Pharm-136, also known as 7-methyl-10-hydroxynoribogaminalog, is a serotonin 5-HT2 receptor agonist and psychedelic drug of the ibogalog family.
Pharmacology Pharmacodynamics Pharm-136 acts as a potent serotonin 5-HT2 receptor agonist, with () values of 0.6nM (102%) at the serotonin 5-HT2A receptor, 3.5nM (52%) at the serotonin 5-HT2B receptor, and 0.5nM (101%) at the serotonin 5-HT2C receptor. The drug showed far lower agonistic potency or was inactive at all other serotonin receptors. As an agonist of the serotonin 5-HT2A receptor in vitro, Pharm-136 showed 29-fold greater potency as well as higher efficacy (101% vs. 80%) than psilocin.
The drug produces the head-twitch response, a behavioral proxy of psychedelic effects, in rodents. Its median effective dose (ED50) was 3.6mg/kg, compared to 0.38mg/kg (9.5-fold lower) in the case of psilocybin.
Pharmacokinetics The preclinical pharmacokinetics of Pharm-136 have been studied.
Chemistry Pharm-136 is an ibogalog (azepinoindole) derivative and a cyclized tryptamine analogue of the non-hallucinogenic psychoplastogen 7-methylpsilocin.
Synthesis The chemical synthesis of Pharm-136 has been described.
History Pharm-136 was patented by Bright Minds Biosciences in 2023. There is interest in Pharm-136 for potential therapeutic use.
See also Ibogalog List of investigational hallucinogens and entactogens
References