BMB-201
Serotonergic drug
From Wikipedia, the free encyclopedia
BMB-201 is a serotonin 5-HT2A and 5-HT2C receptor agonist of the tryptamine family described as a non-hallucinogenic psychoplastogen which is under development for the treatment of depression, anxiety, pain, and other indications.[1][2][3][4][5] Its route of administration is unspecified.[1]
administrationUnspecified[1]
| Clinical data | |
|---|---|
| Other names | BMB201; BMB-A39a prodrug |
| Routes of administration | Unspecified[1] |
| Drug class | Non-hallucinogenic serotonin 5-HT2A and 5-HT2C receptor partial agonist, other actions[1][2][3][4][5][6] |
Pharmacology
| Target | Affinity (Ki, nM) |
|---|---|
| 5-HT1F | ND (Ki) 23 (EC50) 92% (Emax) |
| 5-HT2A | ND (Ki) 70–71 (EC50) 68–69% (Emax) |
| 5-HT2B | ND (Ki) ND (EC50) <20% (Emax) |
| 5-HT2C | ND (Ki) 6.7 (EC50) 79% (Emax) |
| 5-HT6 | ND (Ki) 9 (EC50) 48% (Emax) |
| Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs: [4][5] | |
BMB-201 is a prodrug of another compound known as BMB-A39a.[4][5] This active metabolite acts as a biased partial agonist of the serotonin 5-HT2A and 5-HT2C receptors.[2][3][4][5][6] BMB-A39a is slightly less efficacious in activating Gq signaling at the serotonin 5-HT2A and 5-HT2C receptors compared to psilocin (Emax = 68% vs. 82% at 5-HT2A and 79% vs. 95% at 5-HT2C, respectively).[5] It is about 9-fold less potent in activating the serotonin 5-HT2A receptor than psilocin, whereas its potency in activating the serotonin 5-HT2C receptor is similar to that of psilocin.[5] Relatedly, whereas psilocin shows balanced activation of both the serotonin 5-HT2A and 5-HT2C receptors, BMB-A39a is about 11-fold more potent in activating the serotonin 5-HT2C receptor over the serotonin 5-HT2A receptor.[5]
In addition to the serotonin 5-HT2A and 5-HT2C receptors, BMB-A39a is a potent partial agonist of the serotonin 5-HT1F and 5-HT6 receptors.[4][6] On the other hand, it shows minimal or negligible activity in activating the serotonin 5-HT2B receptor (Emax < 20%), and does not activate other serotonin receptors, for instance the serotonin 5-HT1B and 5-HT1D receptors.[4][5][6]
BMB-A39a shows less than 70% efficacy in activating Gq signaling at the serotonin 5-HT2A receptor, which has been associated with absence of hallucinogenic-like activity.[4][7] Accordingly, BMB-201 is said to have minimal or absent psychedelic effects due to its reduced serotonin 5-HT2A receptor intrinsic activity but to potently induce neuroplasticity.[4][5] It has been reported to show effectiveness in animal models of depression, anxiety, pain, and substance use disorder.[4][8][5]
Chemistry
The exact chemical structure of BMB-201 does not yet appear to have been disclosed.[1][2][3][6] However, it is known to be a tryptamine derivative.[6] In addition, Bright Mind Biosciences has patented tryptamines and prodrugs as serotonin 5-HT2 receptor modulators, including for example 7-methylpsilocin and 7-methylpsilocybin.[10][11][12]
Research
BMB-201 is under development by Bright Minds Biosciences.[1][2][3] As of September 2025, it is in the preclinical research stage of development for the treatment of depressive disorders and pain.[1][2][3]