The drug acts as a highlyselectivefull agonist of the serotonin 5-HT2A receptor.[1][2][3][4][5] In terms ofEC50Tooltip half-maximal effective concentration values, it shows 36-fold selectivity for activation of the serotonin 5-HT2A receptor over the serotonin5-HT2C receptor and 500-fold selectivity for activation of the serotonin 5-HT2A receptor over the serotonin5-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 thehead-twitch response (HTR), a behavioral proxy of psychedelic effects, in animals.[3] Hence, it is putatively hallucinogenic in humans.[3] As with other psychedelics likepsilocybin, the HTR induced by BMB-202 shows a biphasic orinverted U-shapeddose–response curve.[3] The drug shows apharmacokinetic profile of highpeak levels, rapidmetabolicclearance, and a shortelimination 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 shortduration of BMB-202 is analogous to the short duration ofdimethyltryptamine (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 inpreclinical research for depressive disorders and PTSD.[1][2] Thechemical structure of BMB-202 does not yet appear to have been disclosed,[1][2] but it seems that it may be aphenethylamine.[5] In any case, selective serotonin 5-HT2A receptor agonists have beenpatented 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).
