Chemistry:Pharm-136

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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 EC50 (Emax) 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. ↑ 1.0 1.1 1.2 1.3 1.4 "Novel Azepinoindoles as 5‑HT2C Agonists for Treating Depression, Drug Addiction, Alcoholism, PTSD, and Neuropathic Pain". ACS Medicinal Chemistry Letters 16 (8): 1507–1508. August 2025. doi:10.1021/acsmedchemlett.5c00426. PMID 40832530. 
  2. ↑ 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 2.10 Kozikowski A, Tueckmantel W, "Azepinoindoles and methods of preparation thereof", WO patent 2023212811, published 9 November 2023



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