BMB-202 explained

Routes Of Administration:Oral
Class:Serotonin 5-HT2A receptor agonist; Serotonergic psychedelic; Hallucinogen
Protein Bound:91–94%
Synonyms:BMB202

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. 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 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, a behavioral proxy of psychedelic effects, in animals. Hence, it is putatively hallucinogenic in humans. 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 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).[7] [8] 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.[9] [10]

See also

External links

Notes and References

  1. Web site: BMB 202 . AdisInsight . 24 April 2023 . 30 October 2024.
  2. Web site: Delving into the Latest Updates on BMB-202 with Synapse . Synapse . 29 October 2024 . 30 October 2024.
  3. Vasilkevich A, Halberstadt AL, Duan J, Merritt CR, Cunningham KA, McCorvy J, Kozikowski A, Pedersen J . Novel 5-HT2A selective agonists with well-characterized PK profile and short duration of action . Society for Neuroscience 2024 Annual Meeting (Chicago), October 5-9 . October 2024 .
  4. Web site: Bright Minds Biosciences Provides Clinical Program Updates and Outlines Anticipated Milestones for 2023 . BioSpace . 27 February 2023 . 30 October 2024.
  5. Web site: Bright Minds Biosciences Receives a Favorable Written Opinion from the International Searching Authority for BMB-202 . BioSpace . 19 April 2023 . 30 October 2024.
  6. Web site: Bright Minds Biosciences . Bright Minds Novel Drugs for Targeted Treatment of CNS & Neuropsychiatric Disorders September 2024 (BMB Investor Deck) . September 2024 . 30 October 2024 . 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..
  7. Cameron LP, Olson DE . Dark Classics in Chemical Neuroscience: N, N-Dimethyltryptamine (DMT) . ACS Chem Neurosci . 9 . 10 . 2344–2357 . October 2018 . 30036036 . 10.1021/acschemneuro.8b00101 . 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.
  8. Chaves C, Dos Santos RG, Dursun SM, Tusconi M, Carta MG, Brietzke E, Hallak JE . Why N, N-Dimethyltryptamine (DMT) Matters: Unique Features and Therapeutic Potential Beyond Classical Psychedelics . Frontiers in Psychiatry . 2024 . 15 . 1485337 . 10.3389/fpsyt.2024.1485337 . free . 39568756 . 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).. 11576444 .
  9. Web site: 3-(2-(Aminoethyl)-Indol-4-ol Derivatives, Methods of Preparation Thereof, and the Use as 5-HT2 Receptor Modulators . Google Patents . 5 May 2023 . 30 October 2024.
  10. Web site: Heterocyclic compounds and methods of preparation thereof . Google Patents . 10 April 2024 . 30 October 2024.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "BMB-202".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2025, A B Cryer, All Rights Reserved. Cookie policy.