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Serotonergic drug

Pharmaceutical compound
BMB-201
Clinical data
Other namesBMB201; BMB-A39a prodrug
Drug classNon-hallucinogenic serotonin 5-HT2A and 5-HT2C receptor partial agonist[2][3][4][5]
ATC code
  • None

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.[2][3][4][5] Its route of administration is unspecified.

Pharmacology

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BMB-A39a activities
TargetAffinity (Ki, nM)
5-HT1FND (Ki)
23 (EC50Tooltip half-maximal effective concentration)
92% (EmaxTooltip maximal efficacy)
5-HT2AND (Ki)
70–71 (EC50)
68–69% (Emax)
5-HT2BND (Ki)
ND (EC50)
<20% (Emax)
5-HT2CND (Ki)
6.7 (EC50)
79% (Emax)
5-HT6ND (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: [4][5]

BMB-201 is a prodrug of another compound known as BMB-A39a.[4][5] This active metabolite acts as a biased partial agonist of the serotonin 5-HT2A and 5-HT2C receptors.[2][3][4][5] 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.[4] 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.[4][5]

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.[4][7] 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.[4][5] It has been reported to show effectiveness in animal models of depression, anxiety, pain, and substance use disorder.[4][8][5]

Chemistry

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7-Methylpsilocin, a lead compound with the same in-vitro pharmacology as BMB-A39a patented by Bright Minds Biosciences.[9][10] 7-Methyl­psilocybin was also patented.[10]

The exact chemical structure of BMB-201 does not yet appear to have been disclosed.[2][3] However, it is known to be a tryptamine derivative. In addition, Bright Mind Biosciences has patented tryptamines and prodrugs as serotonin 5-HT2 receptor modulators, including for example 7-methylpsilocin and 7-methylpsilocybin.[10][11][12]

Research

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BMB-201 is under development by Bright Minds Biosciences.[2][3] As of September 2025, it is in the preclinical research stage of development for the treatment of depressive disorders and pain.[2][3]

See also

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References

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  1. 1 2 3 4 5
  2. "BMB-201 Drug Profile". Ozmosi. Retrieved 30 October 2024.
  3. 1 2 3 4 5 6 7 8 9 10 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.
  4. 1 2 3 4 5 6 7 8 9 10 11 "Bright Minds Investor Deck" (PDF). Bright Minds Biosciences Inc. September 2024.
  5. ↑ 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.
  6. ↑ "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.
  7. ↑ "3-[2-(Dimethylamino)ethyl]-7-methyl-1H-indol-4-ol". PubChem. Retrieved 2 April 2026.
  8. 1 2 3 "Heterocyclic compounds and methods of preparation thereof". Google Patents. 25 May 2022. Retrieved 2 April 2026.
  9. ↑ 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.
  10. ↑ "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.
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