This is a list of opioid

Opioid

An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...

s, opioid antagonist

Opioid antagonist

An opioid antagonist is a receptor antagonist that acts on opioid receptors.Naloxone and naltrexone are commonly used opioid antagonist drugs which are competitive antagonists that bind to the opioid receptors with higher affinity than agonists but do not activate the receptors...

s and inverse agonist

Inverse agonist

In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist....

s.

Opium

Opium

Opium is the dried latex obtained from the opium poppy . Opium contains up to 12% morphine, an alkaloid, which is frequently processed chemically to produce heroin for the illegal drug trade. The latex also includes codeine and non-narcotic alkaloids such as papaverine, thebaine and noscapine...

 and poppy straw derivatives

Crude opiate extracts whole opium products

Polish heroin

Polish heroin

Polish heroin is a crude preparation of heroin made from poppy straw. Like heroin derived from opium, it is an addictive opiate psychoactive drug, used recreationally. Poppy straw and opium are both harvested from the opium poppy...

 (Compote, Kompot) •
Diascordium

Diascordium

In pre-modern medicine, diascordium , or diascord, is a kind of electuary, or opiate, first described by Fracastorius, and denominated from the dried leaves of scordium, which is an ingredient therein...

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B & O Supprettes •
Dover's powder

Dover's powder

Dover's powder was a traditional medicine against cold and fever. It is no longer in use in modern medicine, but may have been in use at least through the 1960s.A 1958 source describes Dover's Powder as follows:...

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Kendal Black Drop

Kendal Black Drop

Kendal Black Drop was a drug based on opium. Named after Kendal in the Lake District, England, it is associated with the romantic poet, Samuel Taylor Coleridge....

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Laudanum

Laudanum

Laudanum , also known as Tincture of Opium, is an alcoholic herbal preparation containing approximately 10% powdered opium by weight ....

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Mithridate

Mithridate

Mithridate, also known as mithridatium, mithridatum, or mithridaticum, is a semi-mythical remedy with as many as 65 ingredients, used as an antidote for poisoning, and said to be created by Mithradates VI Eupator of Pontus in the 1st century BC...

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Opium

Opium

Opium is the dried latex obtained from the opium poppy . Opium contains up to 12% morphine, an alkaloid, which is frequently processed chemically to produce heroin for the illegal drug trade. The latex also includes codeine and non-narcotic alkaloids such as papaverine, thebaine and noscapine...

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Paregoric

Paregoric

Paregoric, or camphorated tincture of opium, also known as tinctura opii camphorata, is a medication known for its antidiarrheal, antitussive, and analgesic properties.-History:...

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Poppy straw concentrate

Poppy straw concentrate

Poppy straw is opium poppy that is harvested when fully mature and dry, minus the ripe poppy seeds...

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Poppy tea

Poppy tea

Poppy tea is an infusion brewed from poppy straw or seeds of several species of poppy. The species most commonly used for this purpose is Papaver somniferum, which contains opium....

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Smoking opium •
Theriac

Theriac

Theriac or theriaca was a medical concoction originally formulated by the Greeks in the 1st century AD and became popular throughout the ancient world as far away as China and India via the trading links of the Silk Route...

Opium alkaloids

Codeine

Codeine

Codeine or 3-methylmorphine is an opiate used for its analgesic, antitussive, and antidiarrheal properties...

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Morphine

Morphine

Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was first isolated in 1804 by Friedrich Sertürner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more...

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Oripavine

Oripavine

Oripavine is an opiate and the major metabolite of thebaine. It is the parent compound from which a series of semi-synthetic opioids are derived, which includes the compounds etorphine and buprenorphine...

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Pseudomorphine

Pseudomorphine

Pseudomorphine is a natural dimerisation product of the morphine molecule in tandem and thus a common impurity in morphine concentrations...

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Thebaine

Thebaine

Thebaine , its name coming from the Greek Θῆβαι, Thēbai, an ancient city in Upper Egypt, is an opiate alkaloid. A minor constituent of opium, thebaine is chemically similar to both morphine and codeine, but has stimulatory rather than depressant effects, causing convulsions similar to strychnine...

Alkaloid salts mixtures

Pantopon

Pantopon

Pantopon is a preparation of opiates made up of all of the alkaloids present in opium in their natural proportions as hydrochloride salts. It can sometimes be tolerated by persons who are allergic to morphine....

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Papaveretum

Papaveretum

Papaveretum is a preparation containing a mixture of hydrochloride salts of opium alkaloids. Since 1993, papaveretum has been defined in the British Pharmacopoeia as a mixture of 253 parts morphine hydrochloride, 23 parts papaverine hydrochloride, and 20 parts codeine hydrochloride...

 (Omnopon) •
Tetrapon

Morphine family

2-(p-Nitrophenyl)-4-isopropylmorphine •
14-Hydroxymorphine •
14β-Hydroxymorphine •
2,4-Dinitrophenylmorphine

2,4-Dinitrophenylmorphine

2,4-Dinitrophenylmorphine is an analog of morphine in which a hydroxyl group is substituted with a dinitro phenyl group.-Properties:Being an analog of morphine, it would be expected to have the same effects on the body as a typical opiate/opioid....

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6-Methyldihydromorphine •
6-Methylenedihydrodesoxymorphine

6-Methylenedihydrodesoxymorphine

6-Methylenedihydrodesoxymorphine is an opiate analogue that is a derivative of hydromorphone, where the 6-ketone group has been replaced by methylene. It has sedative and analgesic effects....

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6-Acetyldihydromorphine •
Acetyldihydromorphine •
Azidomorphine

Azidomorphine

Azidomorphine is an opiate analogue that is a derivative of morphine, where the 7,8 double bond has been saturated and the 6-hydroxy group has been replaced by an azide group....

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Chlornaltrexamine

Chlornaltrexamine

Chlornaltrexamine is an irreversible mixed agonist-antagonist for μ-opioid receptors, which forms a covalent bond to the active site. It is 22 times more potent than morphine...

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Chloroxymorphamine •
Desomorphine

Desomorphine

Desomorphine is an opiate analogue invented in 1932 in the United States that is a derivative of morphine, where the 6-hydroxyl group has been removed and the 7,8 double bond has been saturated. It has sedative and analgesic effects, and is around 8-10 times more potent than morphine...

 (dihydrodesoxymorphine) •
Dihydromorphine

Dihydromorphine

Dihydromorphine is a semi-synthetic opioid invented in Germany in 1900. In structure, it is very similar to morphine, the only difference being the reduction of the double bond between positions 7 and 8 in morphine to a single bond...

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Ethyldihydromorphine •
Hydromorphinol

Hydromorphinol

Hydromorphinol is an opiate analogue that is a derivative of morphine, where the 14-position has been hydroxylated and the 7,8- double bond saturated. It has similar effects to morphine such as sedation, analgesia and respiratory depression, but is more potent and has a steeper dose-response curve...

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Methyldesorphine

Methyldesorphine

Methyldesorphine is an opioid analgesic. First synthesized in Germany in 1940 and patented in the USA in 1952, it has a high potential for abuse as with any potent opioid agonist, and is sometimes found along with desomorphine as a component of the home-made opioid mixture known as "Krokodil" used...

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N-Phenethylnormorphine

N-Phenethylnormorphine

N-Phenethylnormorphine is an opiate analgesic drug derived from morphine by replacing the N-methyl group with β-phenethyl. It is around eight to fourteen times more potent than morphine as a result of this modification, in contrast to most other N-substituted derivatives of morphine which are...

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Pseudomorphine

Pseudomorphine

Pseudomorphine is a natural dimerisation product of the morphine molecule in tandem and thus a common impurity in morphine concentrations...

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RAM-378

RAM-378

RAM-378 is an opiate analgesic drug. It is the N-phenethyl derivative of hydromorphinol.-See also:* 14-Cinnamoyloxycodeinone* 14-Phenylpropoxymetopon* 7-PET* N-Phenethylnormorphine...

3,6-diesters of morphine

6-acetyl-1-iodocodeine •
6-nicotinoyldihydromorphine •
Acetylpropionylmorphine

Acetylpropionylmorphine

Acetylpropionylmorphine is an opiate analogue that is a derivative of morphine. It was developed in the early 1900s after first being synthesised in Great Britain in 1875 but shelved along with heroin and various other esters of morphine, but was never used medically, instead being widely sold as...

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Acetylbutyrylmorphine •
Diacetyldihydromorphine

Diacetyldihydromorphine

Diacetyldihydromorphine is a potent opiate derivative developed in Germany in 1929 which is rarely used in some countries for the treatment of severe pain such as that caused by terminal cancer, as a more potent form of diamorphine...

 (dihydroheroin, acetylmorphinol) •
Diacetyldibenzoylmorphine •
Dibutyrylcodeine •
Dibutyrylmorphine •
Dibenzoylmorphine

Dibenzoylmorphine

Dibenzoylmorphine is an opiate analogue that is a derivative of morphine. It was developed in the early 1900s after first having been synthesised in 1875 in the UK, along with various other esters of morphine, but was never used medically, instead being widely sold as one of the first "designer...

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Diformylmorphine •
Dipropanoylmorphine

Dipropanoylmorphine

Dipropanoylmorphine is an opiate derivative, the 3,6-dipropanoyl ester of morphine. It was developed in 1974 as an analgesic...

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Heroin (diacetylmorphine) •
Nicomorphine

Nicomorphine

Nicomorphine is the 3,6-dinicotinate ester of morphine. It is a strong opioid agonist analgesic two to three times as potent as morphine with a side effect profile similar to that of dihydromorphine, morphine, and diamorphine. Nicomorphine was patented as Vilan by Lannacher Heilmittel Ges. m.b.H...

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Tetrabenzoylmorphine •
Tetrabutyrylmorphine

Codeine-dionine family

6-Monoacetylcodeine

6-Monoacetylcodeine

6-Monoacetylcodeine is a toxic acetate ester of codeine in which the hydroxyl group on the 6 position has been acetylated. It is occasionally present as an impurity in street heroin and is typically created when attempting to create heroin from a solution of morphine in which some of the codeine...

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Benzylmorphine

Benzylmorphine

Benzylmorphine is a semi-synthetic opiate narcotic introduced to the international market in 1896 and that of the United States very shortly thereafter...

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Codeine methylbromide

Codeine methylbromide

Codeine methylbromide is the bromomethane salt of codeine. Its possession is prohibited in many jurisdictions. It is considered a Schedule I controlled substance in the United States....

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Desocodeine •
Dimethylmorphine (methocodeine) •
Dihydroethylmorphine •
Methyldihydromorphine

Methyldihydromorphine

Methyldihydromorphine is a semi-synthetic opioid drug developed in Germany in 1936, controlled under both domestic law and UN conventions because of its possible potential for abuse...

 (dihydroheterocodeine) •
Ethylmorphine

Ethylmorphine

Ethylmorphine is an opiate narcotic analgesic .Ethylmorphine was invented in Germany at Merck in 1884 and was used as a weaker alternative to heroin for all indications. Chemically, ethylmorphine is a morphine molecule with a -25 group substituted for the aromatic 3- group...

 (dionine) •
Heterocodeine

Heterocodeine

Heterocodeine is an opiate derivative, the 6-methyl ether of morphine, and a structural isomer of codeine. Heterocodeine was first synthesised in 1932, and can be made from morphine by selective methylation. Codeine is the natural mono-methyl ester, so methylated where it must be metabolized to...

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Isocodeine •
Isopropylmorphine •
Pholcodine

Pholcodine

Pholcodine is a drug which is an opioid cough suppressant . It helps suppress unproductive coughs and also has a mild sedative effect, but has little or no analgesic effects. It is also known as morpholinylethylmorphine....

 (morpholinylethylmorphine) •
Myrophine

Myrophine

Myrophine is an opiate analogue that was developed in 1952. It is a derivative of morphine.Myrophine is substituted with a 3-benzyl group and a 6-myristyl chain. It is metabolised to form benzylmorphine and then further to morphine, and so is a long-acting prodrug for morphine, but with a slow...

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Nalodeine (N-allyl-norcodeine) •
Transisocodeine

Morphinones and morphols

1-Bromohydrocodone •
1-Bromooxycodone •
1-Chlorohydrocodone •
1-Chlorooxycodone •
1-Iodohydrocodone •
1-Iodooxycodone •
14-Cinnamoyloxycodeinone

14-Cinnamoyloxycodeinone

14-Cinnamoyloxycodeinone is an opiate analgesic drug discovered in the 1960s, with around 100 times the potency of morphine. It is a derivative of oxycodeinone, being the 14-cinnamate ester.-See also:* 14-Phenylpropoxymetopon* 7-PET...

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14-Ethoxymetopon

14-Ethoxymetopon

14-Ethoxymetopon is an opiate analogue that is a derivative of metopon which has been substituted with an ethoxy group at the 14-position. It is a highly potent analgesic drug several hundred times stronger than morphine....

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14-Methoxymetopon

14-Methoxymetopon

14-Methoxymetopon is an opiate analogue that is a derivative of metopon which has been substituted with a methoxy group at the 14-position. It is a highly potent analgesic drug that is around 500x stronger than morphine when administered systemically; however, when given spinally or supraspinally,...

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14β-Hydroxymorphone •
14-Hydroxymorphone •
14-O-Methyloxymorphone •
14-Phenylpropoxymetopon

14-Phenylpropoxymetopon

14-Phenylpropoxymetopon is an opiate analogue that is an derivative of metopon which has been substituted with a γ-phenylpropoxy group at the 14-position. It is a highly potent analgesic drug several thousand times stronger than morphine, with a similar in vivo potency to etorphine...

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7-Spiroindanyloxymorphone

7-Spiroindanyloxymorphone

7-Spiroindanyloxymorphone is a drug which is used in scientific research. It is a selective δ-opioid agonist....

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8,14-Dihydroxydihydromorphinone •
Acetylcodone •
Acetylmorphone

Acetylmorphone

Acetylmorphone is an opiate analogue that is an acetylated derivative of hydromorphone which was developed in the early 1900s as a potential cough suppressant and analgesic. It is prepared by the acetylation of hydromorphone using either acetyl chloride or acetic anhydride...

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α-hydrocodol •
Bromoisopropropyldihydromorphinone •
Codeinone

Codeinone

Codeinone is 1/3 as active as codeine as an analgesic but it is an important intermediate in the production of hydrocodone, a painkiller about 3/4 the potency of morphine.-Chemical structure:...

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Codorphone

Codorphone

Codorphone is an opioid analgesic drug. It is an analogue of hydrocodone substituted with an 8-ethyl group and an N-cyclopropylmethyl group. It is a mixed agonist-antagonist at the μ-opioid receptor, and is slightly more potent than codeine in analgesic effects but associated with somewhat greater...

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Codol •
Codoxime

Codoxime

Codoxime is an opiate analogue that is a derivative of hydrocodone, where the 6-ketone group has been replaced by carboxymethyloxime. It has primarily antitussive effects and was found to have moderate potential to cause dependence in animal studies....

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Thebacon (acetyldihydrocodeinone, dihydrocodeinone enol acetate) •
Ethyldihydromorphinone •
Hydrocodol •
Hydrocodone

Hydrocodone

Hydrocodone or dihydrocodeinone is a semi-synthetic opioid derived from either of two naturally occurring opiates: codeine and thebaine. It is an orally active narcotic analgesic and antitussive...

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Hydromorphinone •
Hydromorphol •
Hydromorphone

Hydromorphone

Hydromorphone, a more common synonym for dihydromorphinone, commonly a hydrochloride is a very potent centrally-acting analgesic drug of the opioid class. It is a derivative of morphine, to be specific, a hydrogenated ketone thereof and, therefore, a semi-synthetic drug...

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Hydroxycodeine •
Isopropropyldihydrocodeinone •
Isopropropyldihydromorphinone •
Methyldihydromorphinone •
Metopon

Metopon

Metopon is an opiate analogue that is a methylated derivative of hydromorphone which was invented in 1948 as an analgesic....

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Morphenol •
Morphinol •
Morphinone

Morphinone

Morphinone is itself not a very potent opioid but it is the intermediate when morphine is being converted to hydromorphone which is 4-6 times as potent as morphine.- Chemical structure :...

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Morphol •
N-Phenethyl-14-ethoxymetopon

N-Phenethyl-14-ethoxymetopon

N-Phenethyl-14-ethoxymetopon is a drug which is a derivative of metopon. It is a potent analgesic, around 60 times stronger than morphine and produces significantly less constipation....

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Oxycodone

Oxycodone

Oxycodone is an opioid analgesic medication synthesized from opium-derived thebaine. It was developed in 1916 in Germany, as one of several new semi-synthetic opioids in an attempt to improve on the existing opioids: morphine, diacetylmorphine , and codeine.Oxycodone oral medications are generally...

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Oxymorphol

Oxymorphol

Oxymorphol is oxymorphone which has been hydroxylated at the 6-position. It is produced by the human body as an active metabolite of oxymorphone and some bacteria as an intermediate in turning morphine into hydromorphone...

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Oxymorphinol •
Oxymorphone

Oxymorphone

Oxymorphone or 14-Hydroxydihydromorphinone is a powerful semi-synthetic opioid analgesic first developed in Germany circa 1914, patented in the USA by Endo Pharmaceuticals in 1955 and introduced to the United States market in January 1959 and other countries around the same time...

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Pentamorphone

Pentamorphone

Pentamorphone is a semi-synthetic opiate derivative related to compounds such as morphine, hydromorphone and oxymorphone. Developed in 1984, it is a potent opioid analgesic several times stronger than fentanyl, and with a similarly fast onset of effects and short duration of action...

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Semorphone

Semorphone

Semorphone is an opiate analogue that is an N-substituted derivative of oxymorphone.Semorphone is a partial agonist at μ-opioid receptors...

Morphides

α-chlorocodide (alphachlorocodide, chlorocodide) •
α-chloromorphide •
3-Bromomorphide •
Bromocodide •
Bromomorphide (8-bromomorphide) •
Chlorocodide •
Chloromorphide

Chloromorphide

Chloromorphide is an opiate analogue that is a derivative of morphine, where the 6-hydroxy group has been replaced by chlorine. Developed in 1933 in Germany, it has approximately ten times the potency of morphine...

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Codide •
Fluorocodide (8-fluorocodide) •
Fluormorphide •
Iodocodide •
Iodomorphide (8-iodomorphide) •
Morphide

Dihydrocodeine series

14-Hydroxydihydrocodeine

14-Hydroxydihydrocodeine

14-Hydroxydihydrocodeine is an opiate analgesic drug, which is also an active metabolite of oxycodone....

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Acetyldihydrocodeine

Acetyldihydrocodeine

Acetyldihydrocodeine is an opiate derivative discovered in Germany in 1914 and was used as as a cough suppressant and analgesic. It is not commonly used, but has activity similar to other opiates...

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Dihydrocodeine

Dihydrocodeine

Dihydrocodeine, also called DHC, Drocode, Paracodeine and Parzone and known by the brand names of Synalgos DC, Panlor DC, Panlor SS, Contugesic, New Bron Solution-ACE, Huscode, Drocode, Paracodin, Codidol, Didor Continus, Dicogesic, Codhydrine, Dekacodin, DH-Codeine,...

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Dihydrodesoxycodeine (desocodeine) •
Dihydroisocodeine •
Nicocodeine

Nicocodeine

Nicocodeine is an opiate derivative, closely related to dihydrocodeine and the codeine analogue of nicomorphine developed as a cough suppressant and analgesic. It is not commonly used in most countries, but has activity similar to other opiates. Nicocodeine and nicomorphine were introduced in the...

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Nicodicodeine

Nicodicodeine

Nicodicodeine is an opiate derivative developed as a cough suppressant and analgesic. Synthesized in 1904, it is not commonly used, but has activity similar to other opiates. Nicodicodeine is metabolised in the liver by demethylation to produce 6-nicotinoyldihydromorphine, and subsequently further...

Nitrogen morphine derivatives

1-Nitrocodeine •
2-Nitrocodeine •
1-Nitromorphine •
2-Nitromorphine •
Codeine-N-oxide •
Heroin-N-oxide •
Hydromorphone-N-oxide •
Morphine-N-oxide

Morphine-N-oxide

Morphine-N-oxide is an active opioid metabolite of morphine. Morphine itself, in trials with rats, acts 11–22 times more potent than morphine-N-oxide subcutaneously and 39–89 times more potent intraperitoneally...

Hydrazones

Acetylmorphazone •
Hydromorphazone •
Morphazone •
Oxymorphazone

Oxymorphazone

Oxymorphazone is an opioid analgesic drug related to oxymorphone. Oxymorphazone is a potent and long acting μ-opioid agonist which binds irreversibly to the receptor, forming a covalent bond which prevents it from detaching once bound...

 

Halogenated morphine derivatives

1-Bromocodeine •
2-Bromocodeine •
1-Bromodiacetylmorphine •
2-Bromodiacetylmorphine •
1-Bromodihydrocodeine •
2-Bromodihydrocodeine •
1-Bromodihydromorphine •
2-Bromodihydromorphine •
1-Bromomorphine •
2-Bromomorphine •
1-Chlorocodeine •
2-Chlorocodeine •
1-Chlorodiacetylmorphine •
2-Chlorodiacetylmorphine •
1-Chlorodihydrocodeine •
2-Chlorodihydrocodeine •
1-Chlorodihydromorphine •
2-Chlorodihydromorphine •
1-Chloromorphine •
2-Chloromorphine •
1-Fluorocodeine •
2-Fluorocodeine •
1-Fluorodiacetylmorphine •
2-Fluorodiacetylmorphine •
1-Fluorodihydrocodeine •
2-Fluorodihydrocodeine •
1-Fluorodihydromorphine •
2-Fluorodihydromorphine •
1-Fluoromorphine •
2-Fluoromorphine •
3-Fluoromorphine •
1-Iodocodeine •
2-Iodocodeine •
1-Iododiacetylmorphine •
2-Iododiacetylmorphine •
1-Iododihydrocodeine •
2-Iododihydrocodeine •
1-Iododihydromorphine •
2-Iododihydromorphine •
1-Iodomorphine

1-Iodomorphine

1-Iodomorphine is a semi-synthetic narcotic analgesic formed by halogenation of the 1 position on the morphine carbon skeleton. Halogenated morphine derivatives were first synthesised in Germany, Austria/Austria-Hungary, the United Kingdom and the United States in the period 1890 to 1930. Use of...

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2-Iodomorphine •
Chlorethylmorphine

Active opiate metabolites

Codeine-N-oxide (genocodeine) •
Dihydromorphine-6-glucuronide •
Hydromorphone-N-oxide •
Heroin-7,8-oxide •
Morphine-6-glucuronide

Morphine-6-glucuronide

Morphine-6-glucuronide is a major active metabolite of morphine, and as such is the molecule responsible for much of the pain-relieving effects of morphine . M6G is formed from morphine by the enzyme UDP-Glucuronosyltransferase-2B7...

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6-Monoacetylmorphine •
Morphine-N-oxide

Morphine-N-oxide

Morphine-N-oxide is an active opioid metabolite of morphine. Morphine itself, in trials with rats, acts 11–22 times more potent than morphine-N-oxide subcutaneously and 39–89 times more potent intraperitoneally...

 (genomorphine) •
Naltrexol •
Norcodeine

Norcodeine

Norcodeine is an opiate analogue that is the N-demethylated derivative of codeine.Norcodeine has relatively little opioid activity in its own right, but is formed as a metabolite of codeine following ingestion....

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Normorphine

Normorphine

Normorphine is an opiate analogue that is derived from the N-demethylated derivative of morphine first described in the 1950s when a large group of N-substituted morphine analogues were characterized for activity....

Morphinan series

4-chlorophenylpyridomorphinan •
Cyclorphan

Cyclorphan

Cyclorphan is a hallucinogenic opioid mixed agonist-antagonist related to levorphanol discovered in the late 1960s. It is not marketed as an analgesic because of side effects related to its impact on the kappa opioid receptor, but has found some use as a research chemical on and off since its...

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Dextrallorphan

Dextrallorphan

Dextrallorphan is a drug of the morphinan class known in scientific research. It acts as a σ1 receptor agonist, κ-opioid receptor agonist, and NMDA receptor antagonist. It has no significant affinity for the σ2, μ-opioid, or δ-opioid receptor, or for the serotonin or norepinephrine transporter...

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Levargorphan •
Levorphanol

Levorphanol

Levorphanol is an opioid medication used to treat severe pain. It is the levorotatory stereoisomer of the synthetic morphinan and a pure opioid agonist, first described in Germany in 1948 as an orally active morphine-like analgesic...

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Levorphan •
Levophenacylmorphan

Levophenacylmorphan

Levophenacylmorphan is a morphinan derivative that acts as an opioid agonist. It has potent analgesic effects and is around 10x more potent than morphine. Adverse effects associated with its use are those of the opioids as a whole, including pruritus, nausea, respiratory depression, euphoria and...

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Levomethorphan

Levomethorphan

Levomethorphan is the l-stereoisomer of methorphan. The effects of the two isomers are quite different. Dextromethorphan is an antitussive at low doses and a dissociative at much higher doses, whereas levomethorphan is an opioid analgesic...

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Norlevorphanol

Norlevorphanol

Norlevorphanol is an opioid analgesic of the morphinan class. It was never marketed....

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N-Methylmorphinan •
Oxilorphan

Oxilorphan

Oxilorphan is an opioid antagonist from the morphinan family of drugs.Oxilorphan is a non-selective opioid which is a μ antagonist but a κ partial agonist. It has similar effects to naloxone, and around the same potency as an antagonist....

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Phenomorphan

Phenomorphan

Phenomorphan is an opioid analgesic. It is not currently used in medicine, but has similar side effects to other opiates, which include itching, nausea and respiratory depression....

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Methorphan

Methorphan

Methorphan comes in two isomeric forms, each with differing pharmacology and effects:* Dextromethorphan - An over-the-counter cough suppressant, as well as dissociative hallucinogen....

 (racemethorphan) •
Morphanol

Morphanol

Racemorphan is the racemic mixture of the two stereoisomers of 17-methylmorphinan-3-ol, each with differing pharmacology and effects:* Dextrorphan - A dissociative hallucinogen and cough suppressant....

 (racemorphanol) •
Ro4-1539

Ro4-1539

Ro4-1539 is an opioid analgesic drug from the morphinan series, which was developed by the pharmaceutical company Hoffmann–La Roche in the 1950s. It acts as a potent μ-opioid agonist, and was found to be around 30-60x more potent than the related drug levorphanol in animal experiments...

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Stephodeline •
Xorphanol

Xorphanol

Xorphanol is an opioid analgesic from the morphinan family of drugs. It is a mixed agonist-antagonist at the μ-opioid receptor and produces potent analgesic effects with little potential for dependence or abuse....

Others

1-Nitroaknadinine •
14-episinomenine •
5,6-Dihydronorsalutaridine •
6-Ketonalbuphine •
Aknadinine •
Butorphanol

Butorphanol

Butorphanol is a morphinan-type synthetic opioid analgesic developed by Bristol-Myers. Brand name Stadol was recently discontinued by the manufacturer. It is now only available in its generic formulations, manufactured by Novex, Mylan, Apotex and Ben Venue Laboratories. Butorphanol is most...

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Cephakicine •
Cephasamine •
Cyprodime

Cyprodime

Cyprodime is an opioid antagonist from the morphinan family of drugs.Cyprodime is a selective opioid antagonist which blocks the μ-opioid receptor, but without affecting the δ-opioid or κ-opioid receptors...

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Drotebanol

Drotebanol

Drotebanol is a morphinan derivative that acts as an opioid agonist. It was invented by Sankyo Company in Japan during the 1970s. It is synthesised from thebaine....

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Fenfangjine G •
Nalbuphine

Nalbuphine

Nalbuphine is a semi-synthetic opioid used commercially as an analgesic under a variety of trade names, including Nubain. It is noteworthy in part for the fact that at low dosages, it is found much more effective by women than by men, and may even increase pain in men, leading to its...

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Sinococuline •
Sinomenine

Sinomenine

Sinomenine or Cocculine is an alkaloid found in the root of the climbing plant Sinomenium acutum which is native to Japan and China. It is traditionally used in herbal medicine in these countries, as a treatment for rheumatism and arthritis. However its analgesic action against other kinds of pain...

 (cocculine) •
Tannagine

Benzomorphan

Benzomorphan

Benzomorphan is a chemical compound.It is the base for a series of drugs which variably act on the opioid and sigma receptors, including, but not limited to, the following compounds:...

s

5,9 alpha-diethyl-2-hydroxybenzomorphan (5,9-DEHB) •
8-Carboxamidocyclazocine

8-Carboxamidocyclazocine

8-Carboxamidocyclazocine is an opioid analgesic drug related to cyclazocine, invented by the chemist Mark P. Wentland and co-workers. Similarly to cyclazocine, 8-CAC acts as an agonist at both the μ and κ opioid receptors, but has a much longer duration of action than cyclazocine, and does not...

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Alazocine •
Anazocine •
Bremazocine

Bremazocine

Bremazocine is a κ-opioid receptor agonist related to pentazocine. It has potency and long-lasting analgesic and diuretic effects....

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Cogazocine

Cogazocine

Cogazocine is an opioid analgesic of the benzomorphan family which was never marketed....

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Dezocine

Dezocine

Dezocine was developed by American Home Products and is an opioid analgesic related to pentazocine, with a similar profile of effects that include analgesic action and euphoria at low doses, but produces dysphoria and hallucinations at high doses, most likely due to action at κ-opioid...

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Eptazocine

Eptazocine

Eptazocine is an opioid analgesic of the benzomorphan family which was introduced in Japan by Morishita in 1987. It acts as a mixed κ-opioid receptor agonist and μ-opioid receptor antagonist....

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Etazocine •
Ethylketocyclazocine •
Fluorophen •
Ketazocine

Ketazocine

Ketazocine , also known as ketocyclazocine, is a benzomorphan derivative used in opioid receptor research. Ketocyclazocine is an exogenous opioid that binds to the kappa opioid receptor....

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Metazocine

Metazocine

Metazocine is an opioid analgesic related to pentazocine. While metazocine has significant analgesic effects, mediated through a mixed agonist-antagonist action at the mu opioid receptor, its clinical use is limited by dysphoric and hallucinogenic effects which are most likely caused by activity at...

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Pentazocine

Pentazocine

Pentazocine is a synthetically prepared prototypical mixed agonist-antagonist narcotic drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain...

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Phenazocine

Phenazocine

Phenazocine is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects....

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Quadazocine •
Thiazocine •
Tonazocine

Tonazocine

Tonazocine is an opioid analgesic of the benzomorphan family which made it to phase II clinical trials for the treatment of postoperative pain, but development was apparently ceased and ultimately it was never marketed...

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Volazocine

Volazocine

Volazocine is an opioid analgesic of the benzomorphan class which was never marketed....

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Zenazocine

Pethidine

Pethidine

Pethidine or meperidine Pethidine (INN) or meperidine (USAN) Pethidine (INN) or meperidine (USAN) (commonly referred to as Demerol but also referred to as: isonipecaine; lidol; pethanol; piridosal; Algil; Alodan; Centralgin; Dispadol; Dolantin; Mialgin (in Indonesia); Petidin Dolargan (in Poland);...

s (meperidines)

4-Fluoromeperidine

4-Fluoromeperidine

4-Fluoropethidine is a drug that is a derivative of pethidine , which combines pethidine's opioid analgesic effects with increased monoamine reuptake inhibition...

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Allylnorpethidine

Allylnorpethidine

Allylnorpethidine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine .Allylnorpethidine is an analogue of pethidine where the N-methyl group has been replaced by allyl...

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Anileridine

Anileridine

Anileridine is a synthetic analgesic drug and is a member of the piperidine class of analgesic agents developed by Merck & Co. in the 1950s...

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Benzethidine

Benzethidine

Benzethidine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine .Benzethidine is not currently used in medicine and is a Class A/Schedule I drug which is controlled under UN drug conventions...

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Carperidine

Carperidine

Carperidine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine .Carperidine is not currently used in medicine...

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Difenoxin

Difenoxin

Difenoxin is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine and more distantly related to alphaprodine and piritramide, and it is an active metabolite of the anti-diarrhoea drug diphenoxylate. Difenoxin et al...

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Diphenoxylate

Diphenoxylate

Diphenoxylate is an opioid agonist used for the treatment of diarrhea that acts by slowing intestinal contractions and peristalsis allowing the body to consolidate intestinal contents and prolong transit time, thus allowing the intestines to draw moisture out of them at a normal or higher rate and...

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Etoxeridine

Etoxeridine

Etoxeridine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine ....

 (carbetidine) •
Furethidine

Furethidine

Furethidine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine .Furethidine is not currently used in medicine and is a Class A/Schedule I drug which is controlled under UN drug conventions. It has similar effects to other opioid derivatives, such as analgesia,...

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Hydroxypethidine

Hydroxypethidine

Hydroxypethidine is an opioid analgesic that is an analogue of pethidine . Hydroxypethidine is significantly less potent than meperidine as an analgesic, although it also has NMDA antagonist properties like its close relative ketobemidone.Hydroxypethidine has similar effects to other opioids, and...

 (bemidone) •
Hydroxymethoxypethidine •
Morpheridine

Morpheridine

Morpheridine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine...

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Oxpheneridine

Oxpheneridine

Oxpheneridine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine .Oxpheneridine is not currently used in medicine...

 (carbamethidine) •
Meperidine-N-oxide •
Pethidine

Pethidine

Pethidine or meperidine Pethidine (INN) or meperidine (USAN) Pethidine (INN) or meperidine (USAN) (commonly referred to as Demerol but also referred to as: isonipecaine; lidol; pethanol; piridosal; Algil; Alodan; Centralgin; Dispadol; Dolantin; Mialgin (in Indonesia); Petidin Dolargan (in Poland);...

 (meperidine) •
Pethidine intermediate A

Pethidine Intermediate A

Pethidine intermediate A is a 4-phenylpiperidine derivative that is a precursor to the opioid analgesic drug pethidine . It is not known to have any analgesic activity in its own right, however other derivatives of pethidine with a 4-cyano group in place of the carboxylate ethyl ester have been...

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Pethidine intermediate B (norpethidine) •
Pethidine intermediate C (pethidinic acid) •
Pheneridine

Pheneridine

Pheneridine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine .Pheneridine is not currently used in medicine...

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Phenoperidine

Phenoperidine

Phenoperidine was discovered by Janssen Pharmacutica 1960. Marketed as its hydrochloride as Operidine or Lealgin, is an opioid used as a general anesthetic. It is a derivative of isonipecotic acid, like pethidine, and is metabolized in part to norpethidine. It is 20-200 times as potent as pethidine...

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Piminodine

Piminodine

Piminodine is an opioid analgesic that is an analogue of pethidine . It was used in medicine briefly during the 1960s and 70s, but has largely fallen out of clinical use. It was used particularly for obstetric analgesia and in dental procedures and, like pethidine, could be combined with...

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Properidine

Properidine

Properidine is an opioid analgesic and the isopropyl analog of pethidine....

 (ipropethidine) •
Sameridine

Sameridine

Sameridine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine .Sameridine has an unusual pharmacological profile, being both a local anaesthetic and a μ-opioid partial agonist. It is currently under development for use in surgical anasthesia, mainly...

Prodine

Prodine

Prodine is an opioid analgesic that is an analogue of pethidine .There are two isomers of prodine, Alphaprodine and Betaprodine. Betaprodine is some 5x more potent than alphaprodine, but is metabolised more rapidly, and only alphaprodine was developed for medicinal use...

s

Allylprodine

Allylprodine

Allylprodine is an opioid analgesic that is an analogue of prodine. It was discovered in by Hoffman-La Roche in 1957 during research into the related drug pethidine...

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Isopromedol •
(α/β)-Meprodine

Meprodine

Meprodine is an opioid analgesic that is an analogue of pethidine . It is closely related to the drug prodine, the only difference being that meprodine has an ethyl group rather than a methyl at the 3-position of the piperidine ring....

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Desmethylprodine (MPPP) •
PEPAP

PEPAP

PEPAP is an opioid analgesic that is an analog of pethidine .It is related to the drug MPPP, with an N-phenethyl group in place of the N-methyl substitution and an acetate ester rather than propionate. PEPAP is approximately 6-7 times more potent than morphine in laboratory rats...

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(α/β)-Prodine

Prodine

Prodine is an opioid analgesic that is an analogue of pethidine .There are two isomers of prodine, Alphaprodine and Betaprodine. Betaprodine is some 5x more potent than alphaprodine, but is metabolised more rapidly, and only alphaprodine was developed for medicinal use...

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Prosidol

Prosidol

Prosidol is an opioid analgesic that is an analogue of prodine. It was originally discovered by J.F. MacFarlan and Co. in the 1950s. It was further developed in Russia in the 1990s during research into the related drug pethidine....

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Trimeperidine

Trimeperidine

Trimeperidine is an opioid analgesic that is an analogue of prodine. It was developed in or around 1954 in the USSR during research into the related drug pethidine....

 (promedol)

Ketobemidone

Ketobemidone

Ketobemidone is a powerful opioid analgesic. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties imparted by it's metabolite norketobemidone. This makes it useful for some types of pain that don't respond well to other opioids...

s

Acetoxyketobemidone

Acetoxyketobemidone

Acetoxyketobemidone is an opioid analgesic that is an acetylated derivative of ketobemidone. It was developed in the 1950s during research into analogues of pethidine and was assessed by the United Nations Office on Drugs and Crime but was not included on the list of drugs under international...

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Droxypropine

Droxypropine

Droxypropine is a cough suppressant....

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Ketobemidone

Ketobemidone

Ketobemidone is a powerful opioid analgesic. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties imparted by it's metabolite norketobemidone. This makes it useful for some types of pain that don't respond well to other opioids...

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Methylketobemidone

Methylketobemidone

Methylketobemidone is an opioid analgesic that is an analogue of ketobemidone. It was developed in the 1950s during research into analogues of pethidine and was assessed by the United Nations Office on Drugs and Crime but was not included on the list of drugs under international control, probably...

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Propylketobemidone

Propylketobemidone

Propylketobemidone is an opioid analgesic that is an analogue of ketobemidone. It was developed in the 1950s during research into analogues of pethidine and was assessed by the United Nations Office on Drugs and Crime but was not included on the list of drugs under international control, probably...

Amidones

Dextromethadone •
Dextroisomethadone •
Dipipanone

Dipipanone

Dipipanone is a strong opioid analgesic drug, used for very severe pain in cases where other analgesics are unsuitable, for instance where morphine is indicated but cannot be used due to the patient being allergic to morphine.-Dosage forms:...

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Isomethadone •
Levoisomethadone •
Levomethadone •
Methadone

Methadone

Methadone is a synthetic opioid, used medically as an analgesic and a maintenance anti-addictive for use in patients with opioid dependency. It was developed in Germany in 1937...

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Methadone intermediate •
Normethadone

Normethadone

Normethadone is a cough suppressant. It is a desmethyl derivative of methadone....

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Norpipanone •
Phenadoxone

Phenadoxone

Phenadoxone is an opioid analgesic of the open chain class invented in by Hoechst in 1947...

 (heptazone) •
Pipidone

Methadols

Dimepheptanol

Dimepheptanol

Dimepheptanol is an opioid analgesic that is an analogue of methadone.Dimepheptanol is a mixture of two isomers, α-methadol and β-methadol. These are also available separately, and this drug has three separate entries in many national and international lists of illegal drugs, which refer to the...

 (racemethadol) •
Levacetylmethadol

Levacetylmethadol

Levacetylmethadol , levomethadyl acetate , Orlaam or levo-α-acetylmethadol is a synthetic opioid similar in structure to methadone. It has a long duration of action due to its active metabolites. It was approved in 1993 by the U.S. Food and Drug Administration for use in the treatment of opioid...

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Noracetylmethadol

Moramides

Dextromoramide

Dextromoramide

Dextromoramide is a powerful opioid analgesic approximately three times more potent than morphine but shorter acting. It is subject to drug prohibition regimes, both internationally through UN treaties, and by the criminal law of individual states...

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Levomoramide

Levomoramide

Levomoramide is the inactive isomer of the opioid analgesic dextromoramide, invented by the chemist Paul Janssen in 1956. Unlike dextromoramide, which is a potent analgesic with high abuse potential, levomoramide is virtually without activity....

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Moramide intermediate •
Racemoramide

Racemoramide

Racemoramide , or simply moramide, is a opioid analgesic and a racemic mixture of the substances dextromoramide and levomoramide , two enantiomers of a chiral molecule....

Thiambutene

Thiambutene

The Thiambutenes are a family of opioid analgesic drugs developed at the British research laboratory of Burroughs-Wellcome in the late 1940s.The parent compound thiambutene has no analgesic effects, but several compounds from this group are analgesics with around the same potency as...

s

Diallylthiambutene •
Diethylthiambutene

Diethylthiambutene

Diethylthiambutene is an opioid analgesic drug developed in the 1950s which was mainly used as an anesthetic in veterinary medicine and continues, along with the other two thiambutenes dimethylthiambutene and ethylmethylthiambutene to be used for this purpose, particularly in Japan...

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Dimethylthiambutene

Dimethylthiambutene

Dimethylthiambutene is an opioid analgesic drug, most often used in veterinary medicine in Japan and to a lesser extent in other countries in the region and around the world...

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Ethylmethylthiambutene

Ethylmethylthiambutene

Ethylmethylthiambutene is an opioid analgesic drug from the thiambutene family, around 1.3x the potency of morphine. It is under international control under Schedule I of the UN Single Convention On Narcotic Drugs 1961, presumably due to high abuse potential....

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Methylisopropylthiambutene •
Methylpropylthiambutene •
Morpholinylthiambutene •
Piperidylthiambutene

Piperidylthiambutene

Piperidylthiambutene is an opioid analgesic drug from the thiambutene family, which has around the same potency as morphine. It would be considered an illegal controlled substance analogue in some countries such as the USA, Australia and New Zealand, but is legal in the rest of the world....

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Pyrrolidinylthiambutene

Pyrrolidinylthiambutene

Pyrrolidinylthiambutene is an opioid analgesic drug from the thiambutene family with around 3/4 of the potency of morphine. It would be considered an illegal controlled substance analogue in some countries such as the USA, Australia and New Zealand, but is legal in countries not possessing a...

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Thiambutene

Thiambutene

The Thiambutenes are a family of opioid analgesic drugs developed at the British research laboratory of Burroughs-Wellcome in the late 1940s.The parent compound thiambutene has no analgesic effects, but several compounds from this group are analgesics with around the same potency as...

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Tipepidine

Tipepidine

Tipepidine was discovered in the 1950s. Under the trade-names is used as a centrally-acting cough suppressant of the opioid type...

Phenalkoxams

Dextropropoxyphene

Dextropropoxyphene

Dextropropoxyphene, manufactured by Eli Lilly and Company, is an analgesic in the opioid category. It is intended to treat mild pain and has, in addition, anti-tussive and local anesthetic effects. It has been taken off the market in Europe and the US due to concerns of fatal overdoses and...

 (propoxyphene) •
Dimenoxadol

Dimenoxadol

Dimenoxadol , or dimenoxadole , is an opioid analgesic which is a diphenylacetic acid derivative, related to other drugs such as dextropropoxyphene....

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Dioxaphetyl butyrate

Dioxaphetyl Butyrate

Dioxaphetyl butyrate is an opioid analgesic which is a diphenylacetic acid derivative, related to other open-chain opioid drugs such as dextropropoxyphene, levacetylmethadol , lefetamine and dimenoxadol.It produces similar effects to other opioids, including dependence, euphoria, analgesia,...

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Levopropoxyphene

Levopropoxyphene

Levopropoxyphene is an antitussive. It is an optical isomer of dextropropoxyphene. The racemic mixture is called propoxyphene. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert only an antitussive effect. It was formerly marketed in the U.S. by Eli Lilly under the...

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Norpropoxyphene

Norpropoxyphene

Norpropoxyphene is a major metabolite of the opioid analgesic drug dextropropoxyphene, and is responsible for many of the side effects associated with use of this drug, especially the unusual toxicity seen during dextropropoxyphene overdose...

Anilidopiperidines

3-Allylfentanyl

3-Allylfentanyl

3-Allylfentanyl is an opioid analgesic that is an analogue of fentanyl.3-Allylfentanyl has similar effects to fentanyl. Side effects of fentanyl analogues are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression which can be...

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3-Methylfentanyl

3-Methylfentanyl

3-Methylfentanyl is an opioid analgesic that is an analogue of fentanyl. 3-Methylfentanyl is one of the most potent drugs that has been widely sold on the black market, estimated to be between 400-6000 times stronger than morphine depending on which isomer is used .3-Methylfentanyl was first...

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3-Methylthiofentanyl

3-Methylthiofentanyl

3-Methyl-thiofentanyl is an opioid analgesic that is an analogue of fentanyl.3-Methyl-thiofentanyl was sold briefly on the black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their...

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4-Phenylfentanyl

4-Phenylfentanyl

4-Phenylfentanyl is an opioid analgesic that is a derivative of fentanyl. It was developed during the course of research that ultimately resulted in super-potent opioid derivatives such as carfentanil, though it is a substantially less potent analogue...

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Alfentanil

Alfentanil

Alfentanil is a potent but short-acting synthetic opioid analgesic drug, used for anaesthesia in surgery. It is an analogue of fentanyl with around 1/4 the potency of fentanyl and around 1/3 of the duration of action, but with an onset of effects 4x faster than fentanyl...

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Alphamethylacetylfentanyl

Alphamethylacetylfentanyl

α-methylacetylfentanyl is an opioid analgesic that is an analogue of fentanyl.α-methylacetylfentanyl was sold briefly on the black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their...

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Alphamethylfentanyl

Alphamethylfentanyl

α-Methylfentanyl is an opioid analgesic that is an analogue of fentanyl.α-Methylfentanyl was invented in 1976 and appeared on the black market under the name "China White"...

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Alphamethylthiofentanyl

Alphamethylthiofentanyl

α-methyl-thiofentanyl is an opioid analgesic that is an analogue of fentanyl.α-methyl-thiofentanyl was sold briefly on the black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their...

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Benzylfentanyl •
Betahydroxyfentanyl

Betahydroxyfentanyl

β-hydroxyfentanyl is an opioid analgesic that is an analogue of fentanyl.β-hydroxyfentanyl was sold briefly on the black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their structural...

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Betahydroxythiofentanyl

Betahydroxythiofentanyl

β-hydroxythiofentanyl is an opioid analgesic that is an analogue of fentanyl.β-hydroxythiofentanyl was sold briefly on the black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their...

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Betamethylfentanyl

Betamethylfentanyl

β-Methylfentanyl is an opioid analgesic that is an analogue of fentanyl.β-Methylfentanyl was sold briefly on the black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their structural...

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Brifentanil

Brifentanil

Brifentanil is an opioid analgesic that is an analogue of fentanyl and was developed in the early 1990s.Brifentanil is most similar to highly potent, short-acting fentanyl analogues such as alfentanil...

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Carfentanil

Carfentanil

Carfentanil or carfentanyl is an analogue of the popular synthetic opioid analgesic fentanyl, and is one of the most potent opioids known . Carfentanil was first synthesized in 1974 by a team of chemists at Janssen Pharmaceutica which included Paul Janssen...

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Fentanyl •
Lofentanil

Lofentanil

Lofentanil is one of the most potent opioid analgesics known and is an analogue of fentanyl, which was developed in 1960. It is most similar to the highly potent opioid carfentanil , only slightly more potent. Lofentanil can be described as 3-methylcarfentanil, or 3-methyl-4-carbomethoxyfentanyl...

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Mirfentanil

Mirfentanil

Mirfentanil is a fentanyl derivative with strong selectivity for the μ opioid receptor. At lower doses, it antagonizes the analgesic effects of alfentanil and substitutes for naloxone in morphine-treated monkeys; however, it also reverses naloxone-precipitated withdrawal in pigeons trained to...

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Ocfentanil

Ocfentanil

Ocfentanil is an opioid analgesic that is an analogue of fentanyl and was developed in the early 1990s. It is similar to fentanyl in effects, producing strong analgesia and sedation, but is slightly more potent, with 3μg/kg of ocfentanil being equivalent to 5μg/kg of fentanyl.Side effects of...

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Ohmefentanyl

Ohmefentanyl

Ohmefentanyl was discovered in 1995 and is an extremely potent analgesic drug which selectively binds to the µ-opioid receptor....

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Parafluorofentanyl

Parafluorofentanyl

Para-fluorofentanyl is an opioid analgesic that is an analogue of fentanyl.Para-fluorofentanyl was sold briefly on the black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their structural...

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Phenaridine

Phenaridine

Phenaridine is an opioid analgesic that is an analogue of fentanyl. It was developed in 1972, and is used for surgical anasthesia.Phenaridine has similar effects to fentanyl. It is slightly less potent than fentanyl in rats...

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Remifentanil

Remifentanil

Remifentanil is a potent ultra short-acting synthetic opioid analgesic drug. It is given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is used for sedation as well as combined with other medications for use in general anesthesia...

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Sufentanil

Sufentanil

Sufentanil is a powerful synthetic opioid analgesic drug, approximately 5 to 10 times more potent than its analog, fentanyl. Sufentanil is marketed for use by specialist centres under different trade names, such as Sufenta and Sufentil...

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Thenylfentanyl •
Thiofentanyl

Thiofentanyl

Thiofentanyl is an opioid analgesic that is an analogue of fentanyl.Thiofentanyl was sold briefly on the black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their structural similarity...

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Trefentanil

Trefentanil

Trefentanil is an opioid analgesic that is an analogue of fentanyl and was developed in 1992.Trefentanil is most similar to short-acting fentanyl analogues such as alfentanil. In comparative studies, trefentanil was slightly more potent and shorter acting than alfentanil as an analgesic, but...

Oripavine

Oripavine

Oripavine is an opiate and the major metabolite of thebaine. It is the parent compound from which a series of semi-synthetic opioids are derived, which includes the compounds etorphine and buprenorphine...

 derivatives

6,14-Endoethenotetrahydrooripavine •
7-PET

7-PET

7-PET was discovered by K.W. Bentley and is a potent analgesic drug, 300 times the potency of morphine by weight. It is related to the more well-known oripavine derivative opioid etorphine, which is used as a very potent veterinary painkiller and anesthetic medication, used primarily for the...

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Acetorphine

Acetorphine

Acetorphine is a potent analgesic drug, up to 8700 times stronger than morphine by weight. It is a derivative of the more well-known opioid etorphine, which is used as a very potent veterinary painkiller and anesthetic medication, primarily for the sedation of large animals such as elephants,...

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Alletorphine

Alletorphine

Alletorphine , or N-allylnoretorphine, is an opioid analgesic of the oripavine series which was never marketed....

 (N-allyl-noretorphine) •
BU-48

BU-48

BU-48 is a drug which is used in scientific research. It is from the oripavine family, related to better known drugs such as etorphine and buprenorphine....

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Buprenorphine

Buprenorphine

Buprenorphine is a semi-synthetic opioid that is used...

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Butorphine •
Cyprenorphine

Cyprenorphine

Cyprenorphine is a drug which is an opioid derivative. It is related to more well-known opioids such as buprenorphine, which is used as an analgesic and for the treatment of opioid addiction, and diprenorphine, which is used as an antidote to reverse the effects of other opioids.Cyprenorphine has...

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Dihydroetorphine

Dihydroetorphine

Dihydroetorphine was developed by K.W.Bentley at McFarlan-Smith in the 1960s and is a potent analgesic drug , which is used mainly in China...

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Etorphine

Etorphine

Etorphine is a semi-synthetic opioid possessing an analgesic potency approximately 200 times that of morphine. It was first prepared in 1960 from oripavine, which does not generally occur in opium poppy extract but rather in "poppy straw" and in related plants, Papaver orientale and Papaver...

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18,19-Dehydrobuprenorphine (HS-599) •
N-cyclopropylmethyl-noretorphine •
Nepenthone •
Norbuprenorphine

Norbuprenorphine

Norbuprenorphine is the primary active metabolite of buprenorphine. Norbuprenorphine acts as a μ-opioid, δ-opioid, and nociceptin receptor full agonist, as well as a κ-opioid receptor partial agonist. Norbuprenorphine crosses the blood-brain-barrier similarly to buprenorphine and likely contributes...

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N-phenethyletorphine •
Thevinone •
Thienorphine

Phenazepanes

Ethoheptazine

Ethoheptazine

Ethoheptazine is an opioid analgesic from the phenazepine family. It was invented in the 1950s and is related to other drugs such as proheptazine....

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Meptazinol

Meptazinol

Meptazinol is an opioid analgesic for use with moderate to severe pain, most commonly used to treat pain in obstetrics . A partial µ-opioid receptor agonist, its mixed agonist/antagonist activity affords it a lower risk of dependence and abuse than full µ agonists like morphine...

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Metheptazine

Metheptazine

Metheptazine is an opioid analgesic from the phenazepine family.Metheptazine produces similar effects to other opioids, including analgesia, sedation, dizziness and nausea....

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Metethoheptazine

Metethoheptazine

Metethoheptazine is an opioid analgesic from the phenazepine family. It was invented in the 1960s.Metethoheptazine produces similar effects to other opioids, including analgesia, sedation, dizziness and nausea....

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Proheptazine

Proheptazine

Proheptazine is an opioid analgesic from the phenazepine family. It was invented in the 1960s.Proheptazine produces similar effects to other opioids, including analgesia, sedation, dizziness and nausea....

Indole

Indole

Indole is an aromatic heterocyclic organic compound. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered nitrogen-containing pyrrole ring. Indole is a popular component of fragrances and the precursor to many pharmaceuticals. Compounds that contain an...

s

18-Methoxycoronaridine

18-Methoxycoronaridine

-18-Methoxycoronaridine is a derivative of ibogaine invented in 1996 by the research team around the pharmacologist Stanley D. Glick from the Albany Medical College and the chemist Martin E. Kuehne from the University of Vermont...

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7-Acetoxymitragynine •
7-Hydroxymitragynine

7-Hydroxymitragynine

7-Hydroxymitragynine , an indole, is an active alkaloid in the plant Mitragyna speciosa, commonly known as Kratom. It has opioid agonistic activity. "The potency, calculated using pD values, was 30- and 17-fold higher than that of mitragynine and morphine, respectively...

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Akuammidine •
Akuammine

Akuammine

Akuammine, an indole alkaloid, is the most abundant active alkaloid found in the seeds from the tree Picralima nitida, commonly known as Akuamma....

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Eseroline

Eseroline

Eseroline is a drug which acts as an opioid agonist. It is a metabolite of the acetylcholinesterase inhibitor physostigmine but unlike physostigmine, the acetylcholinesterase inhibition produced by eseroline is weak and easily reversible, and it produces fairly potent analgesic effects mediated...

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Hodgkinsine

Hodgkinsine

Hodgkinsine is an alkaloid found in plants of the Psychotria genus, particularly Psychotria colorata, although it is also found in Psychotria lyciiflora and probably other species in this family, as well as in the related species Calycodendron milnei.Hodgkinsine has antiviral, antibacterial and...

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Mitragynine

Mitragynine

Mitragynine, an indole alkaloid, is the most abundant active alkaloid in the plant Mitragyna speciosa, commonly known as Kratom.-Pharmacology:...

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Pericine

Pericine

Pericine is one of a number of indole alkaloids found in the tree Picralima nitida, commonly known as Akuamma. The dried seeds from this plant are used in traditional medicine throughout West Africa, particularly in Ghana as well as in the Ivory Coast and Nigeria...

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Pseudoakuammigine

Diphenylmethylpiperazine

Diphenylmethylpiperazine

1-piperazine, also known as benzhydrylpiperazine, is a chemical compound and piperazine derivative. It features a piperazine ring with a benzhydryl group bound to one of the nitrogens....

s

BW373U86

BW373U86

BW373U86 is an opioid analgesic drug used in scientific research.BW373U86 is a selective agonist for the δ-opioid receptor, with approximately 15x stronger affinity for the δ-opioid than the μ-opioid receptor...

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DPI-221

DPI-221

DPI-221 is a drug which is used in scientific research. It is a highly selective agonist for the δ-opioid receptor which produces less convulsions than most drugs from this family....

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DPI-287

DPI-287

DPI-287 is a drug that is used in scientific research. It is a highly selective agonist for the δ-opioid receptor, which produces less convulsions than most drugs from this family. It has antidepressant effects....

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DPI-3290

DPI-3290

DPI-3290 was discoverd by Delta Pharmacutical and is a drug that is used in scientific research. It is a potent analgesic drug, which produces little respiratory depression....

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SNC-80

SNC-80

SNC-80 is an opioid analgesic drug used in scientific research. It was invented in 1994.SNC-80 was the first non-peptide drug developed that is a highly selective agonist for the δ-opioid receptor....

Endorphin

Endorphin

Endorphins are endogenous opioid peptides that function as neurotransmitters. They are produced by the pituitary gland and the hypothalamus in vertebrates during exercise, excitement, pain, consumption of spicy food, love and orgasm, and they resemble the opiates in their abilities to produce...

 

Beta-endorphin

Beta-endorphin

β-endorphin is an endogenous opioid peptide neurotransmitter found in the neurons of both the central and peripheral nervous system.The amino acid sequence is:...

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Alpha-endorphin

Alpha-endorphin

Alpha-endorphin is an endogenous opioid peptide whose amino acid sequence is: Tyr-Gly-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr....

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Gamma-endorphin

Gamma-endorphin

Gamma-endorphin is an endorphin....

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α-neo-endorphin

Α-neo-endorphin

α-Neoendorphin is an endogenous opioid peptide with a decapeptide structure and the amino acid sequence Tyr-Gly-Gly-Phe-Leu-Arg-Lys-Tyr-Pro-Lys....

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β-neo-endorphin

Β-neo-endorphin

β-Neoendorphin is an endogenous opioid peptide with a nonapeptide structure and the amino acid sequence Tyr-Gly-Gly-Phe-Leu-Arg-Lys-Tyr-Pro....

Enkephalin

Enkephalin

An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, or specifically endorphins, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephalin were revealed, one...

 

DADLE •
DAMGO

DAMGO

DAMGO is a synthetic opioid peptide with high μ-opioid receptor specificity. It was synthesized as a biologically stable analog of δ-opioid receptor-preferring endogenous opioids, leu- and met-enkephalin....

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Dermenkephalin •
Met-enkephalin

Met-enkephalin

[Met]enkephalin, sometimes referred to as opioid growth factor , is a naturally-occurring, endogenous opioid peptide that has opioid effects of a relatively short duration. It is one of the two forms of enkephalin, the other being [leu]enkephalin...

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Leu-enkephalin

Leu-enkephalin

Leu-enkephalin is an endogenous opioid peptide neurotransmitter with the amino acid sequence Tyr-Gly-Gly-Phe-Leu that is found naturally in the brains of many animals, including humans. It is one of the two forms of enkephalin; the other is met-enkephalin. The tyrosine residue at position 1 is...

Others / unknown

Adrenorphin

Adrenorphin

Adrenorphin, also sometimes referred to as metorpham​ide, is an endogenous, C-terminally amidated, opioid octapeptide that is produced from proteolyic cleavage of proenkephalin A and is widely distributed throughout the mammalian brain...

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Amidorphin

Amidorphin

Amidorphin is an endogenous, C-terminally amidated, opioid peptide generated as a cleavage product of proenkephalin A that is widely distributed in the mammalian brain, with particularly high concentrations found in the adrenal medulla, posterior pituitary, and striatum...

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Casomorphin

Casomorphin

Casomorphins are peptides, i.e., protein fragments, derived from the digestion of milk protein casein. The distinguishing characteristic of casomorphins is that they have an opioid effect....

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DALDA

Dalda

Dalda is a brand of hydrogenated vegetable oil popular in South Asia. Hindustan Lever Limited wanted to brand it, the trader, who still retained a commercial connection with the product, said it had to be named after his company. HLL wanted to include the letter 'L' in it for Lever , and thus was...

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Deltorphin •
Dermorphin •
DPDPE •
Endomorphin

Endomorphin

Endomorphins are two endogenous opioid peptides. Endomorphin-1 and endomorphin-2 are tetrapeptides with the highest known affinity and specificity for the μ opioid receptor...

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Gliadorphin

Gliadorphin

Gliadorphin is an opioid peptide that is formed during digestion of the gliadin component of the gluten protein. It is usually broken down into amino acids by digestion enzymes. It has been hypothesized that children with autism have abnormal leakage from the gut of this compound, which then...

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Morphiceptin

Morphiceptin

Morphiceptin is a tetrapeptide that is aselective μ-opioid receptor agonist. It is derived from β-casomorphin and has over 1,000 times selectivity for μ- over δ-opioid receptors. When administered intracerebroventricularly, morphiceptin had an analgesic ED50 of 1.7 nmol per animal...

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Nociceptin

Nociceptin

Nociceptin or orphanin FQ, a 17 amino acid neuropeptide, is the endogenous ligand for the nociceptin receptor . It is derived from the prepronociceptin protein, as are a further 2 peptides, nocistatin & NocII...

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Octreotide

Octreotide

Octreotide is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone...

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Opiorphin

Opiorphin

Opiorphin is an endogenous chemical compound first isolated from human saliva. Initial research with mice shows the compound has a painkilling effect greater than that of morphine. It works by stopping the normal breakdown of enkephalins, natural pain-killing opioids in the spinal cord...

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Rubiscolin

Rubiscolin

The rubiscolins are a group of opioid peptides which are formed during digestion of the ribulose bisphosphate carboxylase/oxygenase protein from spinach leaves. Rubiscolins mimic the effects of opiates and therefore influence the brain...

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TRIMU 5

TRIMU 5

TRIMU 5 is a selective agonist of the mu-2 mu opioid receptor....

Others

3-(3-Methoxyphenyl)-3-ethoxycarbonyltropane •
AD-1211

AD-1211

AD-1211 is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4-prenyl-piperazine derivative, which is structurally unrelated to most other opioid drugs...

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AH-7921

AH-7921

AH-7921 was discovered in the 1970s and is an opioid analgesic drug selective for the mu opioid receptor, and having around the same potency as morphine....

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Azaprocin

Azaprocin

Azaprocin is a drug which is an opioid analgesic with approximately 10x the potency of morphine, and a fast onset and short duration of action. It was discovered in 1963, but has never been marketed....

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BDPC

BDPC

4--4--1-cyclohexanol is a potent narcotic analgesic with a distinctive chemical structure. It was developed by Daniel Lednicer at Upjohn in the 1970s...

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Bisnortilidine •
BRL-52537

BRL-52537

BRL-52537 is a drug which acts as a potent and highly selective κ-opioid agonist. It has neuroprotective effects in animal studies, and is used for research into potential treatments for stroke and heart attack as well as more general brain research....

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Bromadoline

Bromadoline

Bromadoline is an opioid analgesic selective for the mu-opioid receptor....

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C-8813

C-8813

C-8813 is a potent μ-opioid agonist with a distinctive chemical structure which is not closely related to other established families of opioid drugs. The trans isomer was found to be around 591x more potent than morphine in animal studies...

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Ciramadol

Ciramadol

Ciramadol is an opioid analgesic that was developed in the late 1970s and is related to tramadol, tapentadol and venlafaxine. It is a mixed agonist-antagonist for the μ-opioid receptor with relatively low abuse potential and a ceiling on respiratory depression which makes it a relatively safe drug...

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Doxpicomine

Doxpicomine

Doxpicomine is a mild opioid analgesic drug.. The drug acts as a mu-opioid receptor agonist. It is of fairly low potency, with a 400 mg dose of doxpicomine approximately equivalent in pain-killing effect to 8 mg morphine or 100 mg pethidine...

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Enadoline

Enadoline

Enadoline is a drug which acts as a highly selective κ-opioid agonist.In human studies, it produced visual distortions and feelings of dissociation, reminiscent of the effects of Salvinorin A....

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Faxeladol

Faxeladol

Faxeladol is an opioid analgesic. It is related to tramadol and ciramadol.Just like tramadol, it is believed faxeladol would have pain-relieving, and potent anti-depressant effects, due to its action on serotonin and noradrenaline....

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GR-89696

GR-89696

GR-89696 is a drug which acts as a highly selective κ-opioid agonist. It shows selective effects in different animal models and it is thought it may be a subtype-selective agonist for the κ2 subtype...

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Herkinorin

Herkinorin

Herkinorin is an opioid analgesic that is an analogue of the natural product Salvinorin A. It was discovered in 2005 during structure-activity relationship studies into neoclerodane diterpenes, the family of chemical compounds of which Salvinorin A is a member.Unlike Salvinorin A which is a...

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ICI-199,441

ICI-199,441

ICI-199,441 is a drug which acts as a potent and selective κ-opioid agonist, and has analgesic effects....

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ICI-204,448

ICI-204,448

ICI-204,448 is a drug which acts as a potent and periperhally selective κ-opioid agonist, with possible uses in the treatment of heart attack as well as anti-itching effects. It is used in research to distinguish centrally from peripherally mediated kappa opioid receptor effects....

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J-113,397

J-113,397

J-113,397 is an opioid analgesic drug which was the first compound found to be a highly selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor...

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JTC-801

JTC-801

JTC-801 is an opioid analgesic drug used in scientific research.JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. This was the fourth opioid receptor to be discovered, and is still the least understood...

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Ketamine

Ketamine

Ketamine is a drug used in human and veterinary medicine. Its hydrochloride salt is sold as Ketanest, Ketaset, and Ketalar. Pharmacologically, ketamine is classified as an NMDA receptor antagonist...

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KNT-42 •
LPK-26

LPK-26

LPK-26 is a drug which acts as a potent and selective κ-opioid agonist, and has analgesic effects....

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Methopholine

Methopholine

Methopholine is an opioid analgesic drug discovered in the 1950s by a team of Swiss researchers at Hoffmann-La Roche.Methopholine is an isoquinoline derivative which is not structurally related to most other opioids. It has around the same efficacy as an analgesic as codeine, and was evaluated for...

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MT-45

MT-45

MT-45 is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4-piperazine derivative, which is structurally unrelated to most other opioid drugs...

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Desmethylclozapine

Desmethylclozapine

N-Desmethylclozapine , or norclozapine, is a major active metabolite of the atypical antipsychotic drug clozapine. Interestingly, unlike clozapine, it possesses intrinsic activity at the D2/D3 receptors, and acts as a weak partial agonist at these sites similarly to aripiprazole and bifeprunox...

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NNC 63-0532

NNC 63-0532

NNC 63-0532 is an nociceptoid drug used in scientific research. It acts as a potent and selective agonist for the nociceptin receptor, also known as the ORL-1 receptor...

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Nortilidine

Nortilidine

Nortilidine is the active metabolite of the drug Tilidine. It is formed from Tilidine by demethylation in the liver. The racemate has opioid analgesic effects roughly equivalent in potency to that of morphine but virtually all of the activity resides in the isomer....

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O-Desmethyltramadol

O-Desmethyltramadol

O-Desmethyltramadol is an opioid analgesic and the main active metabolite of tramadol.-O-Desmethyltramadol is the most important metabolite of tramadol produced in the liver after tramadol is consumed...

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Phenadone •
Phencyclidine

Phencyclidine

Phencyclidine , commonly initialized as PCP and known colloquially as angel dust, is a recreational dissociative drug...

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Prodilidine

Prodilidine

Prodilidine is an opioid analgesic which is a ring-contracted analogue of prodine. It has around the same efficacy as codeine, but is only around 1/3 the potency, and has little abuse potential....

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Profadol

Profadol

Profadol is an opioid analgesic which was developed in the 1960s by Parke-Davis. It acts as a mixed agonist-antagonist of the μ-opioid receptor. The analgetic potency is about the same as of meperidine, the antagonistic effect is 1/50 of Nalorphine....

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Ro64-6198

Ro64-6198

Ro64-6198 is an nociceptoid drug used in scientific research. It acts as a potent and selective agonist for the nociceptin receptor, also known as the ORL-1 receptor, with over 100x selectivity over other opioid receptors...

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Salvinorin A

Salvinorin A

Salvinorin A is the main active psychotropic molecule in Salvia divinorum, a Mexican plant which has a long history of use as an entheogen by indigenous Mazatec shamans...

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SB-612,111

SB-612,111

SB-612,111 is an opioid receptor ligand which is a potent and selective antagonist for the nociceptin receptor , several times more potent than the older drug J-113,397. It does not have analgesic effects in its own right, but prevents the development of hyperalgesia, and also shows antidepressant...

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SC-17599

SC-17599

SC-17599 is a steroid derivative drug discovered in 1968 which acts as a selective μ-opioid receptor agonist, with little or no affinity for the δ-opioid or κ-opioid receptors. It is an active analgesic in vivo, more potent than codeine or pethidine but slightly less potent than morphine, and...

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RWJ-394,674

RWJ-394,674

RWJ-394674 is a drug which is used in scientific research. It is a potent, orally active analgesic drug, which produces little respiratory depression. RWJ-394674 itself is a potent and selective agonist for δ-opioid receptors, with a Ki of 0.24 nM at δ and 72 nM at μ...

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TAN-67

TAN-67

TAN-67 is a drug which is used in scientific research, which is a potent and selective δ-opioid agonist, selective for the δ1 subtype. It has analgesic properties and induces dopamine release in the brain...

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Tapentadol

Tapentadol

Tapentadol is a centrally acting analgesic with a dual mode of action as an agonist at the μ-opioid receptor and as a norepinephrine reuptake inhibitor. While its analgesic actions have been compared to tramadol and oxycodone, its general potency is somewhere between tramadol and morphine in...

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Tecodine •
Tifluadom

Tifluadom

Tifluadom is a benzodiazepine derivative with an unusual activity profile. Unlike most benzodiazepines, tifluadom has no activity as a GABAA agonist, but instead is a selective agonist for the κ-opioid receptor...

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Tilidine

Tilidine

Tilidine , or tilidate is a synthetic opioid analgesic, used mainly in Germany, Switzerland and Belgium for treatment of moderate to severe pain, both acute and chronic.-Pharmacology:...

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Tramadol

Tramadol

Tramadol hydrochloride is a centrally acting synthetic opioid analgesic used in treating moderate pain. The drug has a wide range of applications, including treatment for restless legs syndrome and fibromyalgia...

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Trimebutine

Trimebutine

Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects. The maleic acid salt of trimebutine is marketed under the trademark of Debridat, Recutin, Polybutin, or Modulon for treatment of irritable bowel syndrome and other gastrointestinal disorders...

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U-50,488 •
U-69,593

U-69,593

U-69,593 is a drug which acts as a potent and selective κ1-opioid receptor agonist. In animal studies it has been shown to produce antinociception, anti-inflammation, anxiolysis , respiratory depression, and diuresis, while having little effect on gastrointestinal motility. It also inhibits the...

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Viminol

Viminol

Viminol is an opioid analgesic developed by the drugs company Zambon in the 1960s. It has an unusual chemical structure that is not similar to other opioids....

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1-(4-Nitrophenylethyl)piperidylidene-2-(4-chlorophenyl)sulfonamide

1-(4-Nitrophenylethyl)piperidylidene-2-(4-chlorophenyl)sulfonamide

1-piperidylidene-2-sulfonamide is a potent μ-opioid agonist with a distinctive chemical structure which is not closely related to other established families of opioid drugs...

 (W-18)

Opioid antagonists

Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...

 and inverse agonist

Inverse agonist

In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist....

s

5'-Guanidinonaltrindole

5'-Guanidinonaltrindole

5'-Guanidinonaltrindole is an opioid antagonist used in scientific research which is highly selective for the κ opioid receptor. It is 5x more potent and 500 times more selective than the commonly used κ-opioid antagonist norbinaltorphimine. It has a slow onset and long duration of action, and...

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β-Funaltrexamine •
6β-Naltrexol •
Alvimopan

Alvimopan

Alvimopan is a drug which behaves as a peripherally acting μ-opioid antagonist. With limited ability to cross the blood-brain barrier, many of the undesirable side-effects of the opioid agonists such as constipation are minimized without affecting analgesia or precipitating withdrawals...

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Binaltorphimine •
Chlornaltrexamine

Chlornaltrexamine

Chlornaltrexamine is an irreversible mixed agonist-antagonist for μ-opioid receptors, which forms a covalent bond to the active site. It is 22 times more potent than morphine...

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Clocinnamox •
Cyclazocine

Cyclazocine

Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs is called the benzomorphans or benzazocines.- Use :...

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Cyprodime

Cyprodime

Cyprodime is an opioid antagonist from the morphinan family of drugs.Cyprodime is a selective opioid antagonist which blocks the μ-opioid receptor, but without affecting the δ-opioid or κ-opioid receptors...

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Diprenorphine

Diprenorphine

Diprenorphine is an opioid antagonist used to reverse the effects of the super-potent opioid analgesics such as etorphine and carfentanil that are used for tranquilizing large animals in veterinary medicine....

 (M5050) •
Fedotozine •
JDTic

JDTic

JDTic is a drug that acts as an opioid antagonist, which is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- or δ-opioid receptors...

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Levallorphan

Levallorphan

Levallorphan is a drug of the morphinan family which is used as an opioid antidote or antagonist. It acts as an antagonist on μ-opioid receptor and agonist on kappa receptors [hence called [partial agonist]], Levallorphan (Lorfan, Naloxiphan) is a drug of the morphinan family which is used as an...

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Methocinnamox •
Methylnaltrexone

Methylnaltrexone

Methylnaltrexone is one of the newer agents of peripherally-acting μ-opioid antagonists that act to reverse some of the side effects of opioid drugs such as constipation without affecting analgesia or precipitating withdrawals...

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Nalfurafine

Nalfurafine

Nalfurafine is a κ-opioid receptor agonist marketed as a treatment for uremic pruritus in people undergoing hemodialysis....

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Nalmefene

Nalmefene

Nalmefene is an opioid receptor antagonist developed in the early 1970s, and used primarily in the management of alcohol dependence, and also has been investigated for the treatment of other addictions such as pathological gambling and addiction to shopping.Nalmefene is an opiate derivative...

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Nalmexone •
Naloxazone

Naloxazone

Naloxazone is an irreversible μ opioid receptor antagonist which is selective for the μ1 receptor subtype. Naloxazone produces very long lasting antagonist effects as it forms a covalent bond to the active site of the mu-opioid receptor, thus making it impossible for the molecule to unbind and...

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Naloxonazine

Naloxonazine

Naloxonazine is a potent irreversible mu opioid antagonist. Naloxonazine forms spontaneously in acidic solutions of naloxazone, and may be responsible for much or all of the irreversible μ opioid receptor binding displayed by the latter.-See also:...

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Naloxone

Naloxone

Naloxone is an opioid antagonist drug developed by Sankyo in the 1960s. Naloxone is a drug used to counter the effects of opiate overdose, for example heroin or morphine overdose. Naloxone is specifically used to counteract life-threatening depression of the central nervous system and respiratory...

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Naloxone benzoylhydrazone •
Nalorphine

Nalorphine

Nalorphine trade names Lethidrone and Nalline. Nalorphine acts at two opioid receptors, at the mu receptor it has antagonistic effects and at the kappa receptors it exerts agonistic characteristics. It is used to reverse opioid overdose and in a challenge test to determine opioid dependence....

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Naltrexone

Naltrexone

Naltrexone is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. It is marketed in generic form as its hydrochloride salt, naltrexone hydrochloride, and marketed under the trade names Revia and Depade...

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Naltriben

Naltriben

Naltriben is a potent and selective antagonist for the delta opioid receptor, which is used in scientific research. It has similar effects to the more widely used δ antagonist naltrindole, but with different binding affinity for the δ1 and δ2 subtypes, which makes it useful for distinguishing the...

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Naltrindole

Naltrindole

Naltrindole is a highly potent, highly selective delta opioid receptor antagonist used in biomedical research.-Drug design:Since peptide compounds are unable to cross the blood brain barrier, researchers developed naltrindole to be a non-peptide antagonist analog of the delta-preferring endogenous...

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Norbinaltorphimine

Norbinaltorphimine

Norbinaltorphimine is an opioid antagonist used in scientific research. It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- or δ-opioid receptors, although it has less selectivity in vivo than when...

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Oxilorphan

Oxilorphan

Oxilorphan is an opioid antagonist from the morphinan family of drugs.Oxilorphan is a non-selective opioid which is a μ antagonist but a κ partial agonist. It has similar effects to naloxone, and around the same potency as an antagonist....

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S-allyl-3-hydroxy-17-thioniamorphinan (SAHTM)