Chemistry:Seganserin

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Seganserin (INN, BAN; developmental code name R-56413) is a selective serotonin 5-HT2 receptor antagonist which was studied for the treatment of insomnia and anxiety but was never marketed.[1][2][3][4][5][6] It acts as a dual serotonin 5-HT2A and 5-HT2C receptor antagonist.[2][4] The drug blocks the head-twitch response induced by serotonin precursor 5-hydroxytryptophan (5-HTP) and the psychedelic drug mescaline in rodents.[7] It has been found to enhance slow wave sleep (SWS) in clinical studies.[2][4][5][8][3] The drug's time to peak levels is 1 hour and its elimination half-life is 26 hours.[3] Seganserin reached phase 2 clinical trials prior to the discontinuation of its development.[1] It was first described in the scientific literature by 1985.[9][10]

See also

References

  1. ↑ 1.0 1.1 "5-HT2 receptor subtypes: a family re-united?". Trends in Pharmacological Sciences 16 (3): 105–110. March 1995. doi:10.1016/s0165-6147(00)88991-9. PMID 7792930. 
  2. ↑ 2.0 2.1 2.2 "Serotonin 5-HT(2A) receptor antagonists in the treatment of insomnia: present status and future prospects". Drugs of Today 46 (3): 183–193. March 2010. doi:10.1358/dot.2010.46.3.1437247. PMID 20467592. 
  3. ↑ 3.0 3.1 3.2 Cite error: Invalid <ref> tag; no text was provided for refs named Dijk_1989
  4. ↑ 4.0 4.1 4.2 "Antagonism of serotonergic 5-HT2A/2C receptors: mutual improvement of sleep, cognition and mood?". The European Journal of Neuroscience 29 (9): 1795–1809. May 2009. doi:10.1111/j.1460-9568.2009.06718.x. PMID 19473234. 
  5. ↑ 5.0 5.1 "Selective Serotonin 5-HT2A Receptor Antagonists and Inverse Agonists Specifically Promote Slow Wave Sleep (Stage N3) in Man". Sleep and Vigilance 2 (1): 23–31. 6 November 2017. doi:10.1007/s41782-017-0024-7. ISSN 2510-2265. https://link.springer.com/10.1007/s41782-017-0024-7. Retrieved 16 January 2026. 
  6. ↑ "The chemical development of selective and specific serotonin S 2 -antagonists". Drug Development Research 8 (1–4): 133–140. 1986. doi:10.1002/ddr.430080116. ISSN 0272-4391. https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/10.1002/ddr.430080116. Retrieved 16 January 2026. 
  7. ↑ "Partial and complete blockade of 5-hydroxytrytophan (5-HTP)-induced head twitches in the rat: A study of ritanserin (R 55 667), risperidone (R 64 766), and related compounds". Drug Development Research 13 (4): 237–244. 1988. doi:10.1002/ddr.430130406. ISSN 0272-4391. https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/10.1002/ddr.430130406. Retrieved 16 January 2026. 
  8. ↑ "Slow-wave sleep deficiency and enhancement: implications for insomnia and its management". The World Journal of Biological Psychiatry 11 Suppl 1: 22–28. June 2010. doi:10.3109/15622971003637645. PMID 20509829. 
  9. ↑ "Pharmacology of potent and selective S2-serotonergic antagonists". Journal of Cardiovascular Pharmacology 7 Suppl 7: S2–11. 1985. doi:10.1097/00005344-198500077-00002. PMID 2412048. 
  10. ↑ "Effects in the X-maze anxiety model of agents acting at 5-HT1 and 5-HT2 receptors". Psychopharmacology 93 (4): 502–506. 1987. doi:10.1007/BF00207243. PMID 3124184. 



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