Serotonergic psychedelic
Encyclopedia
Serotonergic psychedelics (also known as serotonergic
hallucinogens) are a class of hallucinogenic
drugs with a method of action strongly tied to the serotonin
neurotransmitter
. Serotonin (often referred to as 5-HT, short for its full chemical name 5-Hydroxy Tryptamine) is a naturally occurring neurotransmitter which is tied to positive mood, certain involuntary muscle control, and countless other functions, many of which are not yet fully understood.
, the major relay for sensory information input to the cortex
. Worth noting is that selective serotonin reuptake inhibitor
s (a class of antidepressants including Paxil, Prozac, and Zoloft) can increase the dosage required for hallucinogenic effects of serotonergic psychedelics, in some people, based on anecdotal reports. Some users, however, have found this to be entirely untrue for them.
, LSD, psilocybin
, and mescaline
. The tryptamine
psychedelics, such as DMT
and psilocybin
structurally resemble serotonin
itself, see Erowid.org's Chem-Compare tool, here shown comparing serotonin and psilocybin. The phenethylamine
psychedelics on the other hand, such as mescaline
(found naturally in Peyote
) and compounds of the 2C
family, more closely resemble the neurotransmitter
dopamine
, as shown here in a comparison of dopamine and mescaline.
known in the common slang as a trip.
or spiritual
role as entheogen
s. In some cases (such as mescaline
and psilocin
) such use has occurred for centuries. Some entheogenic users also engage in or support recreational use
, while others deem it irresponsible or sacrilegious.
Entheogens are also utilised in occult practices as espoused by Peter Carroll in his treatise, Liber Null and Psychonautica. Other occult practitioners, such as Aleister Crowley, used psychedelic substances (mescaline) and other drugs to achieve "chemi-gnosis" (knowledge gained though chemical inebriation).
Serotonergic
Serotonergic or serotoninergic means "related to the neurotransmitter serotonin". A synapse is serotonergic if it uses serotonin as its neurotransmitter...
hallucinogens) are a class of hallucinogenic
Psychedelics, dissociatives and deliriants
This general group of pharmacological agents can be divided into three broad categories: psychedelics, dissociatives, and deliriants. These classes of psychoactive drugs have in common that they can cause subjective changes in perception, thought, emotion and consciousness...
drugs with a method of action strongly tied to the serotonin
Serotonin
Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
neurotransmitter
Neurotransmitter
Neurotransmitters are endogenous chemicals that transmit signals from a neuron to a target cell across a synapse. Neurotransmitters are packaged into synaptic vesicles clustered beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to...
. Serotonin (often referred to as 5-HT, short for its full chemical name 5-Hydroxy Tryptamine) is a naturally occurring neurotransmitter which is tied to positive mood, certain involuntary muscle control, and countless other functions, many of which are not yet fully understood.
Method of action
While the method of action of serotonergic psychedelics is not fully understood, serotonergic psychedelics are known to show affinities for various 5-HT receptors in different ways and levels, and may be classified by their activity at different 5-HT sub-sites, such as 5-HT1A, 5-HT1B, 5-HT2A, etc. Many serotonergic psychedelics, such as the family of tryptamines, have very strong structural similarities to serotonin itself, which partially explains the affinity for certain 5-HT sites. It is almost unanimously agreed that serotonergic psychedelics produce their effect by acting as strong partial agonists at the 5-HT2A receptors. How this produces the psychedelic experience is unclear, but it is likely that it acts by increasing excitation in the cortex, possibly by specifically facilitating input from the thalamusThalamus
The thalamus is a midline paired symmetrical structure within the brains of vertebrates, including humans. It is situated between the cerebral cortex and midbrain, both in terms of location and neurological connections...
, the major relay for sensory information input to the cortex
Cerebral cortex
The cerebral cortex is a sheet of neural tissue that is outermost to the cerebrum of the mammalian brain. It plays a key role in memory, attention, perceptual awareness, thought, language, and consciousness. It is constituted of up to six horizontal layers, each of which has a different...
. Worth noting is that selective serotonin reuptake inhibitor
Selective serotonin reuptake inhibitor
Selective serotonin re-uptake inhibitors or serotonin-specific reuptake inhibitor are a class of compounds typically used as antidepressants in the treatment of depression, anxiety disorders, and some personality disorders. The efficacy of SSRIs is disputed...
s (a class of antidepressants including Paxil, Prozac, and Zoloft) can increase the dosage required for hallucinogenic effects of serotonergic psychedelics, in some people, based on anecdotal reports. Some users, however, have found this to be entirely untrue for them.
Examples
Examples of serotonergic psychedelics include DMTDimethyltryptamine
N,N-Dimethyltryptamine is a naturally occurring psychedelic compound of the tryptamine family. DMT is found in several plants, and also in trace amounts in humans and other mammals, where it is originally derived from the essential amino acid tryptophan, and ultimately produced by the enzyme INMT...
, LSD, psilocybin
Psilocybin
Psilocybin is a naturally occurring psychedelic prodrug, with mind-altering effects similar to those of LSD and mescaline, after it is converted to psilocin. The effects can include altered thinking processes, perceptual distortions, an altered sense of time, and spiritual experiences, as well as...
, and mescaline
Mescaline
Mescaline or 3,4,5-trimethoxyphenethylamine is a naturally occurring psychedelic alkaloid of the phenethylamine class used mainly as an entheogen....
. The tryptamine
Tryptamine
Tryptamine is a monoamine alkaloid found in plants, fungi, and animals. It is based around the indole ring structure, and is chemically related to the amino acid tryptophan, from which its name is derived...
psychedelics, such as DMT
Dimethyltryptamine
N,N-Dimethyltryptamine is a naturally occurring psychedelic compound of the tryptamine family. DMT is found in several plants, and also in trace amounts in humans and other mammals, where it is originally derived from the essential amino acid tryptophan, and ultimately produced by the enzyme INMT...
and psilocybin
Psilocybin
Psilocybin is a naturally occurring psychedelic prodrug, with mind-altering effects similar to those of LSD and mescaline, after it is converted to psilocin. The effects can include altered thinking processes, perceptual distortions, an altered sense of time, and spiritual experiences, as well as...
structurally resemble serotonin
Serotonin
Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
itself, see Erowid.org's Chem-Compare tool, here shown comparing serotonin and psilocybin. The phenethylamine
Phenethylamine
Phenylethylamine or phenethylamine is a natural monoamine alkaloid, trace amine, and also the name of a class of chemicals with many members well known for psychoactive drug and stimulant effects. Studies suggest that phenylethylamine functions as a neuromodulator or neurotransmitter in the...
psychedelics on the other hand, such as mescaline
Mescaline
Mescaline or 3,4,5-trimethoxyphenethylamine is a naturally occurring psychedelic alkaloid of the phenethylamine class used mainly as an entheogen....
(found naturally in Peyote
Peyote
Lophophora williamsii , better known by its common name Peyote , is a small, spineless cactus with psychoactive alkaloids, particularly mescaline.It is native to southwestern Texas and Mexico...
) and compounds of the 2C
2C (psychedelics)
2C is a general name for the family of psychedelic phenethylamines containing methoxy groups on the 2 and 5 positions of the benzene ring. Most of these compounds also carry lipophilic substituents at the 4 position, usually resulting in more potent and more metabolically stable and longer acting...
family, more closely resemble the neurotransmitter
Neurotransmitter
Neurotransmitters are endogenous chemicals that transmit signals from a neuron to a target cell across a synapse. Neurotransmitters are packaged into synaptic vesicles clustered beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to...
dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
, as shown here in a comparison of dopamine and mescaline.
Recreational uses
The most widely known use of serotonergic psychedelics is as recreational drugs, providing the user with a psychedelic experiencePsychedelic experience
The term "psychedelic experience" is vague – characterized by polyvalence or ambiguity due to its nature – however in modern psychopharmacological science as well as philosophical, psychological, neurological, spiritual-religious and most other ideological discourses it is understood as an altered...
known in the common slang as a trip.
Spiritual uses
Serotonergic psychedelics can be used in a religiousReligion
Religion is a collection of cultural systems, belief systems, and worldviews that establishes symbols that relate humanity to spirituality and, sometimes, to moral values. Many religions have narratives, symbols, traditions and sacred histories that are intended to give meaning to life or to...
or spiritual
Spirituality
Spirituality can refer to an ultimate or an alleged immaterial reality; an inner path enabling a person to discover the essence of his/her being; or the “deepest values and meanings by which people live.” Spiritual practices, including meditation, prayer and contemplation, are intended to develop...
role as entheogen
Entheogen
An entheogen , in the strict sense, is a psychoactive substance used in a religious, shamanic, or spiritual context. Historically, entheogens were mostly derived from plant sources and have been used in a variety of traditional religious contexts...
s. In some cases (such as mescaline
Mescaline
Mescaline or 3,4,5-trimethoxyphenethylamine is a naturally occurring psychedelic alkaloid of the phenethylamine class used mainly as an entheogen....
and psilocin
Psilocin
Psilocin , an aromatic compound, sometimes also spelled psilocine, psilocyn, or psilotsin, is a psychedelic mushroom alkaloid. It is found in most psychedelic mushrooms together with its phosphorylated counterpart psilocybin...
) such use has occurred for centuries. Some entheogenic users also engage in or support recreational use
Recreational drug use
Recreational drug use is the use of a drug, usually psychoactive, with the intention of creating or enhancing recreational experience. Such use is controversial, however, often being considered to be also drug abuse, and it is often illegal...
, while others deem it irresponsible or sacrilegious.
Entheogens are also utilised in occult practices as espoused by Peter Carroll in his treatise, Liber Null and Psychonautica. Other occult practitioners, such as Aleister Crowley, used psychedelic substances (mescaline) and other drugs to achieve "chemi-gnosis" (knowledge gained though chemical inebriation).
Medical uses
- There is substantial anecdotal evidence that serotonergic psychedelics may be helpful in the treatment of cluster headacheCluster headacheCluster headache, nicknamed "suicide headache", is a neurological disease that involves, as its most prominent feature, an immense degree of pain in the head. Cluster headaches occur periodically: spontaneous remissions interrupt active periods of pain. The cause of the disease is currently unknown...
s. - There has been research, largely during the 1960s, suggesting that psychedelic drugs may be able to lead to breakthrough experiences during psychotherapyPsychotherapyPsychotherapy is a general term referring to any form of therapeutic interaction or treatment contracted between a trained professional and a client or patient; family, couple or group...
. Most of this research was centered around serotonergic psychedelics. - During the 1960s, some therapists would self-administer LSDLSDLysergic acid diethylamide, abbreviated LSD or LSD-25, also known as lysergide and colloquially as acid, is a semisynthetic psychedelic drug of the ergoline family, well known for its psychological effects which can include altered thinking processes, closed and open eye visuals, synaesthesia, an...
in an attempt to gain insight to the nature of schizophreniaSchizophreniaSchizophrenia is a mental disorder characterized by a disintegration of thought processes and of emotional responsiveness. It most commonly manifests itself as auditory hallucinations, paranoid or bizarre delusions, or disorganized speech and thinking, and it is accompanied by significant social...
and other psychotic disorders, as the effects of LSD and various other similar psychedelic drugs were believed at the time to be psychotomimeticPsychotomimeticA drug with psychotomimetic actions mimics the symptoms of psychosis, including delusions and/or delirium, as opposed to just hallucinations. Some drugs of the opioid class have psychotomimetic effects, such as pentazocine and butorphanol....
. However while psychedelic drug therapy is believed to have some therapeutic effect, psychotomimetic action has not been found to be a direct product of LSD or other psychedelic drug use. Sandoz Laboratories provided most of the LSD for this use under the brand-name Delysid. Timothy LearyTimothy LearyTimothy Francis Leary was an American psychologist and writer, known for his advocacy of psychedelic drugs. During a time when drugs like LSD and psilocybin were legal, Leary conducted experiments at Harvard University under the Harvard Psilocybin Project, resulting in the Concord Prison...
was a noteworthy individual who initially was performing LSD research along these lines. - Also during the 1960s, AMT (Alpha-Methyl-TryptamineAlphamethyltryptamineα-Methyltryptamine , is a psychedelic, stimulant, and entactogen drug of the tryptamine class. It was originally developed as an antidepressant by workers at Upjohn in the 1960s.- History :...
) was prescribed as an antidepressantAntidepressantAn antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...
due to its MAO InhibitoryMonoamine oxidase inhibitorMonoamine oxidase inhibitors are a class of antidepressant drugs prescribed for the treatment of depression. They are particularly effective in treating atypical depression....
properties and slow release of norepinephrine and serotonin, mostly in the former Soviet UnionSoviet UnionThe Soviet Union , officially the Union of Soviet Socialist Republics , was a constitutionally socialist state that existed in Eurasia between 1922 and 1991....
. - PsilocybinPsilocybinPsilocybin is a naturally occurring psychedelic prodrug, with mind-altering effects similar to those of LSD and mescaline, after it is converted to psilocin. The effects can include altered thinking processes, perceptual distortions, an altered sense of time, and spiritual experiences, as well as...
and other 5-HT2A receptor5-HT2A receptorThe mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor . This is the main excitatory receptor subtype among the GPCRs for serotonin , although 5-HT2A may also have an inhibitory effect on certain areas such...
agonists appear to have a rapid and often sustained (after the drug has left the body) therapeutic effect on Obsessive-compulsive disorderObsessive-compulsive disorderObsessive–compulsive disorder is an anxiety disorder characterized by intrusive thoughts that produce uneasiness, apprehension, fear, or worry, by repetitive behaviors aimed at reducing the associated anxiety, or by a combination of such obsessions and compulsions...
.
External resources
- Organization for Understanding Cluster Headaches Research Library - 5HT and Hallucinogens (Archive.org index, Aug 28, 2005)
- Cluster Busters