BMB-201

Last updated

BMB-201
Clinical data
Other namesBMB201; BMB-A39a prodrug
Drug class Non-hallucinogenic serotonin 5-HT2A and 5-HT2C receptor partial agonist [1] [2] [3] [4]

BMB-201 is a serotonin 5-HT2A and 5-HT2C receptor agonist described as a non-hallucinogenic psychoplastogen which is under development for the treatment of depression, anxiety, pain, and other indications. [1] [2] [3] [4]

Contents

The drug is a prodrug of another compound called BMB-A39a. [3] [4] It acts as a partial agonist of the serotonin 5-HT2A and 5-HT2C receptors. [1] [2] [3] [4] BMB-A39a is less efficacious in activating Gq signaling at the serotonin 5-HT2A and 5-HT2C receptors compared to psilocin (Emax Tooltip Maximal efficacy = 68% vs. 82% at 5-HT2A and 79% vs. 95% at 5-HT2C for BMB-201 and psilocin, respectively). [4] The EC50 Tooltip half-maximal effective concentration value of BMB-A39a in activating the serotonin 5-HT2C receptor is around 10-fold higher than for activating the 5-HT2A receptor (EC50 = 6.7 nM and 71.2 nM, respectively). [4] 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. [3] Conversely, BMB-A39a shows minimal or negligible activity in activating the serotonin 5-HT2B receptor (Emax < 20%) and does not activate other serotonin receptors. [3] [4]

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. [3] [4] It has been reported to show effectiveness in animal models of depression, anxiety, pain, and substance use disorder. [3] [5] [4]

BMB-201 is under development by Bright Minds Biosciences. [1] [2] As of October 2024, its highest developmental phase is preclinical research. [1] [2] The chemical structure of BMB-201 does not yet appear to have been disclosed. [1] [2]

See also

References

  1. 1 2 3 4 5 6 "Delving into the Latest Updates on BMB-201 with Synapse". Synapse. 29 October 2024. Retrieved 30 October 2024.
  2. 1 2 3 4 5 6 "BMB-201 Drug Profile". Ozmosi. Retrieved 30 October 2024.
  3. 1 2 3 4 5 6 7 8 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 "Bright Minds Investor Deck" (PDF). Bright Minds Biosciences Inc. September 2024.
  5. ↑ "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.
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