BMB-202 is a serotonin 5-HT<sub>2A</sub> receptor agonist and psychedelic hallucinogen which is under development for the treatment of depressive disorders and post-traumatic stress disorder (PTSD). It is taken orally. However, BMB-202 has also been evaluated by injection in preclinical studies.
BMB-202 acts as a highly selective full agonist of the serotonin 5-HT<sub>2A</sub> receptor. In terms of values, it shows 36- to 40-fold selectivity for activation of the serotonin 5-HT<sub>2A</sub> receptor over the serotonin 5-HT<sub>2C</sub> receptor and 500-fold selectivity for activation of the serotonin 5-HT<sub>2A</sub> receptor over the serotonin 5-HT<sub>2B</sub> receptor. It has been claimed by its developer that BMB-202 is the most selective serotonin 5-HT<sub>2A</sub> 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 doseâÂÂresponse 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.
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-HT<sub>2A</sub> receptor agonists of the N-benzylphenethylamine family have been patented by Bright Minds Biosciences.
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.