| Clinical data | |
|---|---|
| Other names | BMB201; BMB-A39a prodrug |
| Drug class | Non-hallucinogenic serotonin 5-HT2A and 5-HT2C receptor partial agonist123456 |
| ATC code |
|
BMB-201 is a serotonin 5-HT2A and 5-HT2C receptor agonist of the tryptamine family described as a non-hallucinogenic psychoplastogen which is under development for the treatment of depression, anxiety, pain, and other indications.12345 Its route of administration is unspecified.1
Pharmacology
| Target | Affinity (Ki, nM) |
|---|---|
| 5-HT1F | ND (Ki) 23 (EC50Tooltip half-maximal effective concentration) 92% (EmaxTooltip maximal efficacy) |
| 5-HT2A | ND (Ki) 70–71 (EC50) 68–69% (Emax) |
| 5-HT2B | ND (Ki) ND (EC50) <20% (Emax) |
| 5-HT2C | ND (Ki) 6.7 (EC50) 79% (Emax) |
| 5-HT6 | ND (Ki) 9 (EC50) 48% (Emax) |
| Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs: 45 | |
BMB-201 is a prodrug of another compound known as BMB-A39a.45 This active metabolite acts as a biased partial agonist of the serotonin 5-HT2A and 5-HT2C receptors.23456 BMB-A39a is slightly less efficacious in activating Gq signaling at the serotonin 5-HT2A and 5-HT2C receptors compared to psilocin (EmaxTooltip Maximal efficacy = 68% vs. 82% at 5-HT2A and 79% vs. 95% at 5-HT2C, respectively).5 It is about 9-fold less potent in activating the serotonin 5-HT2A receptor than psilocin, whereas its potency in activating the serotonin 5-HT2C receptor is similar to that of psilocin.5 Relatedly, whereas psilocin shows balanced activation of both the serotonin 5-HT2A and 5-HT2C receptors, BMB-A39a is about 11-fold more potent in activating the serotonin 5-HT2C receptor over the serotonin 5-HT2A receptor.5
In addition to the serotonin 5-HT2A and 5-HT2C receptors, BMB-A39a is a potent partial agonist of the serotonin 5-HT1F and 5-HT6 receptors.46 On the other hand, it shows minimal or negligible activity in activating the serotonin 5-HT2B receptor (Emax < 20%), and does not activate other serotonin receptors, for instance the serotonin 5-HT1B and 5-HT1D receptors.456
BMB-A39a shows less than 70% efficacy in activating Gq signaling at the serotonin 5-HT2A receptor, which has been associated with absence of hallucinogenic-like activity.47 Accordingly, BMB-201 is said to have minimal or absent psychedelic effects due to its reduced serotonin 5-HT2A receptor intrinsic activity but to potently induce neuroplasticity.45 It has been reported to show effectiveness in animal models of depression, anxiety, pain, and substance use disorder.485
Chemistry
The exact chemical structure of BMB-201 does not yet appear to have been disclosed.1236 However, it is known to be a tryptamine derivative.6 In addition, Bright Mind Biosciences has patented tryptamines and prodrugs as serotonin 5-HT2 receptor modulators, including for example 7-methylpsilocin and 7-methylpsilocybin.101112
Research
BMB-201 is under development by Bright Minds Biosciences.123 As of September 2025, it is in the preclinical research stage of development for the treatment of depressive disorders and pain.123
See also
See also
References
References
- "BMB 201". AdisInsight. 10 September 2025. Retrieved 1 April 2026.
- "Delving into the Latest Updates on BMB-201 with Synapse". Synapse. 29 October 2024. Retrieved 30 October 2024.
- "BMB-201 Drug Profile". Ozmosi. Retrieved 30 October 2024.
- Vasilkevich A, Duan J, Lovera A, McCorvy J, Pedersen JT (October 2024). Novel 5-HT2A/2C mixed and partial agonist and its efficacy in preclinical pain models (PDF). Society for Neuroscience 2024 Annual Meeting, Chicago, October 5-9.
- "Bright Minds Investor Deck" (PDF). Bright Minds Biosciences Inc. September 2024.
- Vasilkevich A, Lovera A, Duan J, McDonald I, Collins SD, Pedersen JT (7 December 2025). Overview of Bright Minds Biosciences: Pioneering Serotonin Pharmacology (PDF). 2025 AES Annual Meeting, December 5–9, Atlanta, Georgia.
- Wallach J, Cao AB, Calkins MM, Heim AJ, Lanham JK, Bonniwell EM, et al. (December 2023). "Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential". Nat Commun. 14 (1): 8221. doi:10.1038/s41467-023-44016-1. PMC 10724237. PMID 38102107.
- "Bright Minds Biosciences proprietary compound, BMB-201, 5-HT2C/2A mixed agonist, demonstrated similar efficacy to morphine in preclinical pain models". BioSpace. 17 October 2024. Retrieved 30 October 2024.
- "3-[2-(Dimethylamino)ethyl]-7-methyl-1H-indol-4-ol". PubChem. Retrieved 2 April 2026.
- "Heterocyclic compounds and methods of preparation thereof". Google Patents. 25 May 2022. Retrieved 2 April 2026.
- Duan W, Cao D, Wang S, Cheng J (January 2024). "Serotonin 2A Receptor (5-HT2AR) Agonists: Psychedelics and Non-Hallucinogenic Analogues as Emerging Antidepressants". Chem Rev. 124 (1): 124–163. doi:10.1021/acs.chemrev.3c00375. PMID 38033123.
A recent patent from Bright Minds Bioscience disclosed a series of psilocin analogues with alkyl substitutions on the indole nitrogen, exemplified by compounds 13−16. 137 Among them, compounds 13−15 showed significantly decreased functional activities (13, EC50 = 196 nM, Emax = 65%; 14, EC50 = 188 nM, Emax = 48%; 15, EC50 = 1803 nM, Emax = 18%) compared to that of psilocin (EC50 = 8.34 nM at 5-HT2AR) in the Gq dissociation BRET assay, although all of them displayed excellent potency at 5-HT2CR and high selectivity against the 5-HT2BR. Compound 16, which contains a cyclopropylmethyl substitution on the indole nitrogen, exhibited potent partial agonist activity (EC50 = 28 nM, Emax = 29%) at the rat 5- HT2AR.137 No animal behavioral data have been reported on these compounds yet.
- "3-(2-(aminoethyl)-indol-4-ol derivatives, methods of preparation thereof, and the use as 5-ht2 receptor modulators". Google Patents. 12 March 2021. Retrieved 1 April 2026.