BMB-202
| Clinical data | |
|---|---|
| Other names | BMB202 |
| Routes of administration | Oral |
| Drug class | Serotonin 5-HT2A receptor agonist; Serotonergic psychedelic; Hallucinogen |
| Pharmacokinetic data | |
| Protein binding | 91–94% |
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). It is taken by mouth. However, BMB-202 has also been evaluated by injection in preclinical studies.
The drug acts as a highly selective full agonist of the serotonin 5-HT2A receptor. 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. 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.
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 2 hours 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 under development by Bright Minds Biosciences. As of April 2023, it is in preclinical research for depressive disorders and PTSD. The chemical structure of BMB-202 does not yet appear to have been disclosed, but it seems that it may be a phenethylamine. In any case, selective serotonin 5-HT2A receptor agonists have been patented by Bright Minds Biosciences in 2023 and 2024.