BMB-202 is a selective serotonin 5-HT2A receptor agonist and psychedelic drug of the N-benzylphenethylamine family which is under development for the treatment of depressive disorders and post-traumatic stress disorder (PTSD). It is taken orally.
Pharmacology Pharmacodynamics + Target Affinity (Ki, nM) 5-HT2A (Ki)4.4 ()101% () 5-HT2B (Ki)2,827 ()94% () 5-HT2C (Ki)223 ()113% () Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs:
BMB-202 acts as a highly selective full agonist of the serotonin 5-HT2A receptor. In terms of values, it shows 36- to 40-fold selectivity for activation of the serotonin 5-HT2A receptor over the serotonin 5-HT2C receptor and 500-fold selectivity for activation of the serotonin 5-HT2A receptor over the serotonin 5-HT2B receptor. It has been claimed by its developer that BMB-202 is the most selective serotonin 5-HT2A receptor agonist yet to be discovered or to be in development, at least as of late 2024.
BMB-202 induces the head-twitch response (HTR), a behavioral proxy of psychedelic effects, in animals. Hence, it is putatively hallucinogenic in humans. As with other psychedelics like psilocybin, the HTR induced by BMB-202 shows a biphasic or inverted U-shaped dose–response curve.
The drug shows a pharmacokinetic profile of high peak levels, rapid metabolic clearance, and a short elimination half-life in animals. It is predicted that BMB-202 will have a short half-life of less than 2hours and short duration of 1 to 2hours in humans. In relation to this, the drug is described as a "fast-on-fast-off" compound. The expected short duration of BMB-202 is analogous to the short duration of dimethyltryptamine (DMT). Short-acting psychedelics like DMT and BMB-202 may be more suitable for use in clinical therapeutic settings. BMB-202 is also described as having rapid absorption and brain distribution, high bioavailability, and significant first-pass metabolism resulting in it being fast-acting and having a short duration.
Chemistry
The exact chemical structure of BMB-202 does not yet appear to have been disclosed. However, it is known to be an N-benzylphenethylamine derivative. In addition, selective serotonin 5-HT2A receptor agonists of the N-benzylphenethylamine family have been patented by Bright Minds Biosciences, for instance lead agent "compound 109" (N-(2-methylthiobenzyl)-2-hydroxy-4-cyanophenethylamine).
Research BMB-202 is under development by Bright Minds Biosciences. As of September 2025, it is in the preclinical research stage of development for treatment of depressive disorders and PTSD.
See also List of investigational hallucinogens and entactogens Substituted N-benzylphenethylamine BMB-101 BMB-105 BMB-201
References
External links Pipeline - Bright Minds Biosciences