1-Methylpsilocin Explained

1-Methylpsilocin (developmental code names CMY, CMY-16) is a tryptamine derivative developed by Sandoz which acts as a selective agonist of the serotonin 5-HT2C receptor (of 12 nM, vs. 633 nM at 5-HT2A), and an inverse agonist at 5-HT2B (Ki of 38 nM). While 1-methylpsilocin does have higher affinity for 5-HT2C than 5-HT2A, it does produce a head-twitch response in mice that is dependent on 5-HT2A, so it is not entirely free of effects on 5-HT2A in vivo. In contrast to psilocin, 1-methylpsilocin did not activate 5-HT1A receptors in mice.

1-Methylpsilocin has been investigated for applications such as treatment of glaucoma, obsessive–compulsive disorder (OCD), and cluster headaches, as these conditions are amenable to treatment with psychedelic drugs but are not generally treated with such agents due to the hallucinogenic side effects they produce, which are considered undesirable. 1-Methylpsilocin therefore represents a potential alternative treatment to psilocin that may be less likely to produce hallucinogenic effects.[1] [2] [3]

See also

Notes and References

  1. Bryan Roth . Sard H, Kumaran G, Morency C, Roth BL, Toth BA, He P, Shuster L . SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist . Bioorganic & Medicinal Chemistry Letters . 15 . 20 . 4555–4559 . October 2005 . 16061378 . 10.1016/j.bmcl.2005.06.104 .
  2. Sewell RA, Halpern JH, Pope HG . Response of cluster headache to psilocybin and LSD . Neurology . 66 . 12 . 1920–1922 . June 2006 . 16801660 . 10.1212/01.wnl.0000219761.05466.43 . 31220680 .
  3. Halberstadt AL, Koedood L, Powell SB, Geyer MA . Differential contributions of serotonin receptors to the behavioral effects of indoleamine hallucinogens in mice . Journal of Psychopharmacology . 25 . 11 . 1548–1561 . November 2011 . 21148021 . 3531560 . 10.1177/0269881110388326 .