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]
| Clinical data | |
|---|---|
| Other names | BMB201; BMB-A39a prodrug |
| Drug class | Non-hallucinogenic serotonin 5-HT2A and 5-HT2C receptor partial agonist[1][2][3][4] |
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 = 68% vs. 82% at 5-HT2A and 79% vs. 95% at 5-HT2C for BMB-201 and psilocin, respectively).[4] The EC50 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
editReferences
edit- ^ a b c d e f "Delving into the Latest Updates on BMB-201 with Synapse". Synapse. 29 October 2024. Retrieved 30 October 2024.
- ^ a b c d e f "BMB-201 Drug Profile". Ozmosi. Retrieved 30 October 2024.
- ^ a b c d e f g h 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.
- ^ a b c d e f g h i "Bright Minds Investor Deck" (PDF). Bright Minds Biosciences Inc. September 2024.
- ^ "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.