| Clinical data | |
|---|---|
| Other names | BMB202 |
| Routes of administration | Oral[1] |
| Drug class | Serotonin 5-HT2A receptor agonist; Serotonergic psychedelic; Hallucinogen[1][2][3] |
| Pharmacokinetic data | |
| Protein binding | 91–94%[3] |
BMB-202 is a serotonin 5-HT2A receptor agonist and psychedelic hallucinogen which is under development for the treatment of depressive disorders and post-traumatic stress disorder (PTSD).[1][2][3][4][5][6] It is taken by mouth.[1] However, BMB-202 has also been evaluated by injection in preclinical studies.[3]
The drug acts as a highly selective full agonist of the serotonin 5-HT2A receptor.[1][2][3][4][5] In terms of EC50 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 metabolic clearance, 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 2 hours 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]
BMB-202 is the most selective 5-HT2A agonist known so far. [...] BMB-202: The most selective 5-HT2A agonist in development*. [...] *Based on publicly available information as of September 2024.
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
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).
{{cite journal}}: CS1 maint: DOI inactive as of November 2024 (link)