The drug acts as a highly selectivefull agonist of the serotonin 5-HT2A receptor.[1][2][3][4][5] In terms of EC50Tooltip half-maximal effective concentration values, it shows 36-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.[3][5] It has been claimed by its developer to be the most selective serotonin 5-HT2A receptor agonist yet to be discovered or that is currently under development, at least as of September 2024.[6]
BMB-202 induces the head-twitch response, a behavioral proxy of psychedelic effects, in animals.[3] Hence, it is putatively hallucinogenic in humans.[3] The drug shows a pharmacokinetic profile of high peak levels, rapid metabolicclearance, and a short elimination half-life in animals.[3][5] It is predicted that BMB-202 will have a short half-life of less than 2hours in humans.[3][5] In relation to this, the drug is described as a "fast-on-fast-off" compound.[6][5] The expected short duration of BMB-202 is analogous to the short duration of dimethyltryptamine (DMT).[7][8] Short-acting psychedelics like DMT and BMB-202 may be more suitable for use in clinical therapeutic settings.[3][8]
BMB-202 is under development by Bright Minds Biosciences.[1][2] As of April 2023, it is in preclinical research for depressive disorders and PTSD.[1][2] The chemical structure of BMB-202 does not yet appear to have been disclosed,[1][2] but it seems that it may be a phenethylamine.[5] In any case, selective serotonin 5-HT2A receptor agonists have been patented by Bright Minds Biosciences in 2023 and 2024.[5][9][10]
^Cameron LP, Olson DE (October 2018). "Dark Classics in Chemical Neuroscience: N, N-Dimethyltryptamine (DMT)". ACS Chem Neurosci. 9 (10): 2344–2357. doi:10.1021/acschemneuro.8b00101. PMID30036036. Owing to its rapid onset (a few minutes) and short duration of action (less than an hour) when smoked, the use of DMT in the 1960s became known as a "businessman's lunch." [...] It was not until 1956, 3 years after Twarog's and Page's seminal discovery of serotonin in the brain,170 that Szara and coworkers found ́DMT to be hallucinogenic in humans.171 The acute hallucinogenic effects were rapid (within 5 min) but lasted only for 30−60 min.172,173 The original reports of DMT use were described as "similar to LSD or mescaline, but with a shorter duration of effect."174
^ abChaves C, Dos Santos RG, Dursun SM, Tusconi M, Carta MG, Brietzke E, et al. (2024). "Why N, N-Dimethyltryptamine (DMT) Matters: Unique Features and Therapeutic Potential Beyond Classical Psychedelics". Frontiers in Psychiatry. 15: 1485337. doi:10.3389/fpsyt.2024.1485337. PMC11576444. PMID39568756. DMT's rapid onset and short duration (20-30 minutes when inhaled or injected) (17, 23) make it practical for clinical use compared to longer-acting psychedelics like psilocybin (4-6 hours), MDMA (4-6 hours), and LSD (8-12 hours) (110, 111). Its brief effects reduce supervision needs, and its lack of tolerance allows for repeated dosing. However, its short half-life and intense acute effects could complicate clinical use if frequent administration is needed, increasing demands on personnel and risk of adverse reactions (2, 3).
