Chemistry:Cinanserin

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Cinanserin (INN; developmental code name SQ-10643) is a serotonin 5-HT2A and 5-HT2C receptor antagonist which was discovered in the 1960s and was never marketed.[1][2][3] It has about 50-fold higher affinity for the 5-HT2A receptor than for 5-HT2C, and very low affinity for 5-HT1 receptors.[3] The drug also inhibits the 3C-like protease of SARS-CoV-1[4] and SARS-CoV-2,[5] but with much lower affinity.

See also

References

  1. ↑ Elks, J. (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA276. Retrieved 17 January 2026. 
  2. ↑ "Serotonin (5-HT2) receptor mediated enhancement of cortical unit activity". Canadian Journal of Physiology and Pharmacology 70 (12): 1604–9. December 1992. doi:10.1139/y92-230. PMID 1301238. 
  3. ↑ 3.0 3.1 "Central serotonin receptors as targets for drug research". J Med Chem 30 (1): 1–12. January 1987. doi:10.1021/jm00384a001. PMID 3543362. "Table II. Affinities of Selected Phenalkylamines for 5-HT1 and 5-HT2 Binding Sites". 
  4. ↑ "Cinanserin is an inhibitor of the 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro". Journal of Virology 79 (11): 7095–103. June 2005. doi:10.1128/JVI.79.11.7095-7103.2005. PMID 15890949. 
  5. ↑ "Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors". Nature 582 (7811): 289–293. June 2020. doi:10.1038/s41586-020-2223-y. PMID 32272481. "Cinanserin is an inhibitor of SARS-CoV-2 Mpro.". 



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