7-PET
Encyclopedia
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 sedation of large animals such as elephants, giraffes and rhinos. 7-PET itself has a 3-O-methyl ether which reduces potency, but the 3-OH derivative is around 2200x morphine, almost the same potency as etorphine as a μ
agonist
, and unexpectedly the 3-desoxy compound is also around the same potency of 2000x morphine.
Unlike etorphine however, 7-PET is not an illegal drug, and is not controlled under the UN drug conventions, but it might still be considered to be a controlled substance analogue
of etorphine on the grounds of its related chemical structure in some jurisdictions such as the USA, Canada
, Australia
and New Zealand
.
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
drug, 300 times the potency of 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...
by weight. It is related to the more well-known 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...
derivative opioid 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...
, which is used as a very potent veterinary painkiller and anesthetic medication, used primarily for the sedation of large animals such as elephants, giraffes and rhinos. 7-PET itself has a 3-O-methyl ether which reduces potency, but the 3-OH derivative is around 2200x morphine, almost the same potency as etorphine as a μ
Mu Opioid receptor
The μ-opioid receptors are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins. They are also referred to as μ opioid peptide receptors. The prototypical μ receptor agonist is the opium alkaloid morphine; μ refers to morphine...
agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
, and unexpectedly the 3-desoxy compound is also around the same potency of 2000x morphine.
Unlike etorphine however, 7-PET is not an illegal drug, and is not controlled under the UN drug conventions, but it might still be considered to be a controlled substance analogue
Federal Analog Act
The Federal Analog Act, , is a controversial section of the United States Controlled Substances Act which allowed any chemical "substantially similar" to a controlled substance listed in Schedule I or II to be treated as if it were also listed in those schedules, but only if intended for human...
of etorphine on the grounds of its related chemical structure in some jurisdictions such as the USA, Canada
Canada
Canada is a North American country consisting of ten provinces and three territories. Located in the northern part of the continent, it extends from the Atlantic Ocean in the east to the Pacific Ocean in the west, and northward into the Arctic Ocean...
, Australia
Australia
Australia , officially the Commonwealth of Australia, is a country in the Southern Hemisphere comprising the mainland of the Australian continent, the island of Tasmania, and numerous smaller islands in the Indian and Pacific Oceans. It is the world's sixth-largest country by total area...
and New Zealand
New Zealand
New Zealand is an island country in the south-western Pacific Ocean comprising two main landmasses and numerous smaller islands. The country is situated some east of Australia across the Tasman Sea, and roughly south of the Pacific island nations of New Caledonia, Fiji, and Tonga...
.
See also
- 14-Cinnamoyloxycodeinone14-Cinnamoyloxycodeinone14-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...
- 14-Phenylpropoxymetopon14-Phenylpropoxymetopon14-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...
- N-PhenethylnormorphineN-PhenethylnormorphineN-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...
- N-Phenethyl-14-ethoxymetoponN-Phenethyl-14-ethoxymetoponN-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....
- PhenomorphanPhenomorphanPhenomorphan 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....
- RAM-378RAM-378RAM-378 is an opiate analgesic drug. It is the N-phenethyl derivative of hydromorphinol.-See also:* 14-Cinnamoyloxycodeinone* 14-Phenylpropoxymetopon* 7-PET* N-Phenethylnormorphine...
- Ro4-1539Ro4-1539Ro4-1539 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...