Serotonin receptor agonist

Serotonergic psychedelics such as tryptamines (e.g., psilocybin, psilocin, DMTTooltip dimethyltryptamine, 5-MeO-DMT, bufotenin), lysergamides (e.g., LSDTooltip lysergic acid diethylamide, ergine (LSA)), phenethylamines (e.g., mescaline, 2C-B, 25I-NBOMe), and amphetamines (e.g., MDATooltip 3,4-methylenedioxyamphetamine, DOMTooltip 2,5-dimethoxy-4-methylamphetamine) are non-selective agonists of serotonin receptors.

Azapirones such as buspirone, gepirone, and tandospirone are 5-HT1A receptor partial agonists marketed primarily as anxiolytics, but also as antidepressants.

[1] Many atypical antipsychotics, such as aripiprazole, asenapine, clozapine, lurasidone, quetiapine, and ziprasidone, are 5-HT1A receptor partial agonists, and this action is thought to contribute to their beneficial effects on negative symptoms in schizophrenia.

Triptans such as sumatriptan, rizatriptan, and naratriptan are 5-HT1B receptor agonists that are used to abort migraine and cluster headache attacks.

[10] Selective 5-HT2A receptor agonists like the 25-NB compounds, specifically those which can behave as full agonists at this receptor, can cause serotonin syndrome-like adverse effects such as hyperthermia, hyperpyrexia, tachycardia, hypertension, clonus, seizures, agitation, aggression, and hallucinations which has ended in death on numerous occasions despite these particular drugs only being available to drug users for about 2–3 years, being widely in use mostly in the period from 2010-2012.

[8][11] In contrast to the aforementioned drugs's potent, selective, and most importantly, full agonism (meaning the drug can fully activate the receptor to 100% of its activation potential, and does so even with minuscule amounts due to high potency, LSD, like the other "safe" psychedelics which are almost impossible to overdose fatally on, is a partial agonist, and this means it has a limit of how much it can activate the receptor, a limit which is basically impossible to exceed even with exponentially larger amounts of the drug.

[11][12] Antagonists of the 5-HT2A receptor like cyproheptadine and chlorpromazine are able to reverse and mediate recovery from serotonin syndrome.

[16] MDMA has been reported to be both a potent direct agonist[14] and have an indirect effect by increasing plasma serotonin levels.

meta-Chlorophenylpiperazine (mCPP) is a 5-HT2C-preferring serotonin receptor agonist that induces anxiety and depression and can cause panic attacks in susceptible individuals.

Selective 5-HT6 receptor agonists like E-6801, E-6837, EMDT, WAY-181,187, and WAY-208,466 show antidepressant, anxiolytic, antiobsessional, and appetite suppressant effects in animals, but also impair cognition and memory.