Pharm-136, also known as 7-methyl-10-hydroxynoribogaminalog, is a serotonin 5-HT2 receptor agonist and psychedelic drug of the ibogalog family.[1][2]

Pharmacology

Pharmacodynamics

Pharm-136 acts as a potent serotonin 5-HT2 receptor agonist, with EC50Tooltip half-maximal effective concentration (EmaxTooltip maximal efficacy) values of 0.6 nM (102%) at the serotonin 5-HT2A receptor, 3.5 nM (52%) at the serotonin 5-HT2B receptor, and 0.5 nM (101%) at the serotonin 5-HT2C receptor.[1][2] The drug showed far lower agonistic potency or was inactive at all other serotonin receptors.[2] 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.[2]

The drug produces the head-twitch response, a behavioral proxy of psychedelic effects, in rodents.[2] Its median effective dose (ED50) was 3.6 mg/kg, compared to 0.38 mg/kg (9.5-fold lower) in the case of psilocybin.[2]

Pharmacokinetics

The preclinical pharmacokinetics of Pharm-136 have been studied.[2]

Chemistry

Pharm-136 is an ibogalog (azepinoindole) derivative and a cyclized tryptamine analogue of the non-hallucinogenic psychoplastogen 7-methylpsilocin.[1][2]

Synthesis

The chemical synthesis of Pharm-136 has been described.[2]

History

Pharm-136 was patented by Bright Minds Biosciences in 2023.[1][2] There is interest in Pharm-136 for potential therapeutic use.[1][2]

See also

References

  1. 1 2 3 4 5 6 Sabnis RW (August 2025). "Novel Azepinoindoles as 5‑HT2C Agonists for Treating Depression, Drug Addiction, Alcoholism, PTSD, and Neuropathic Pain". ACS Medicinal Chemistry Letters. 16 (8) acsmedchemlett.5c00426: 1507–1508. doi:10.1021/acsmedchemlett.5c00426. PMC 12358981. PMID 40832530.
  2. 1 2 3 4 5 6 7 8 9 10 11 12 WO 2023212811, Kozikowski A, Tueckmantel W, "Azepinoindoles and methods of preparation thereof", published 9 November 2023, assigned to Bright Minds Biosciences Inc.
  3. ↑ "5-HT2C agonist-11 3006787-99-8". www.medchemexpress.com.
source: https://en.wikipedia.org/wiki/Pharm-136