Chemistry:Bexicaserin

From HandWiki

Bexicaserin (INN; developmental code names LP352 and AN352) is a selective serotonin 5-HT2C receptor agonist which is under development for the treatment of Dravet syndrome and Lennox-Gastaut syndrome.[1][2][3] It is taken by mouth.[3][1]

The drug is highly selective for the serotonin 5-HT2C receptor, with negligible affinity for the serotonin 5-HT2A and 5-HT2B receptors.[3] Because it does not activate the serotonin 5-HT2B receptor, bexicaserin is not expected to pose a risk of cardiac valvulopathy, unlike the existing agent fenfluramine.[3]

The activation of serotonin 5-HT2C receptors has been shown to reduce epileptic seizure activity by inhibiting T-type calcium channels (Cav3).[4] These calcium channels facilitate high frequency burst firing in principal neurons of the subiculum. This firing pattern is upregulated following status epilepticus, with these hyperactive neurons often serving as the initiation point for seizures.[5][6][7]

As of October 2024, bexicaserin is in phase 3 clinical trials for treatment of developmental disabilities.[1][2] It is being developed by Longboard Pharmaceuticals.[1][2]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 "Bexicaserin - Longboard Pharmaceuticals". 16 October 2024. https://adisinsight.springer.com/drugs/800061058. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on Bexicaserin with Synapse". 28 October 2024. https://synapse.patsnap.com/drug/b88ffdb0306a4c40bf7b0aa58f256e2c. 
  3. ↑ 3.0 3.1 3.2 3.3 "Evaluating bexicaserin for the treatment of developmental epileptic encephalopathies". Expert Opinion on Pharmacotherapy 25 (9): 1121–1130. June 2024. doi:10.1080/14656566.2024.2373350. PMID 38916481. 
  4. ↑ "Serotonin Regulates the Firing of Principal Cells of the Subiculum by Inhibiting a T-type Ca2+ Current". Frontiers in Cellular Neuroscience 11: 60. 2017. doi:10.3389/fncel.2017.00060. PMID 28326015. 
  5. ↑ "Synaptic contributions to focal and widespread spatiotemporal dynamics in the isolated rat subiculum in vitro". The Journal of Neuroscience 24 (24): 5525–36. June 2004. doi:10.1523/JNEUROSCI.0309-04.2004. PMID 15201325. 
  6. ↑ "Upregulation of a T-type Ca2+ channel causes a long-lasting modification of neuronal firing mode after status epilepticus". The Journal of Neuroscience 22 (9): 3645–55. May 2002. doi:10.1523/JNEUROSCI.22-09-03645.2002. PMID 11978840. 
  7. ↑ "On the origin of interictal activity in human temporal lobe epilepsy in vitro". Science 298 (5597): 1418–1421. 2002. doi:10.1126/science.1076510. PMID 12434059. Bibcode: 2002Sci...298.1418C. 



Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:Bexicaserin&oldid=4243458"