Chemistry:Pruvanserin

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Short description: Chemical compound
Pruvanserin
Pruvanserin.png
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC22H21FN4O
Molar mass376.435 g·mol−1
3D model (JSmol)

Pruvanserin (EMD-281,014, LY-2,422,347) is a selective 5-HT2A receptor antagonist which was under development by Eli Lilly and Company for the treatment of insomnia.[1][2] It was in phase II clinical trials in 2008 but appears to have been discontinued as it is no longer in the company's development pipeline.[3][4] In addition to its sleep-improving properties,[5][6] pruvanserin has also been shown to have antidepressant, anxiolytic, and working memory-enhancing effects in animal studies.[7][8][9]

See also

References

  1. ↑ "EMD 281014, a new selective serotonin 5-HT2A receptor antagonist". European Journal of Pharmacology 473 (2–3): 229–30. July 2003. doi:10.1016/S0014-2999(03)01992-7. PMID 12892843. 
  2. ↑ "5-HT(2A) inverse-agonists for the treatment of insomnia". Current Topics in Medicinal Chemistry 8 (11): 969–76. 2008. doi:10.2174/156802608784936700. PMID 18673166. 
  3. ↑ "Efficacy Study of LY2422347 to Treat Insomnia - Full Text View - ClinicalTrials.gov". 24 January 2007. http://clinicaltrials.gov/ct2/show/NCT00259311. 
  4. ↑ "Eli Lilly and Company » Research Pipeline". http://www.lilly.com/research/pipeline/. 
  5. ↑ "Effects of activation and blockade of 5-HT2A/2C receptors in the dorsal raphe nucleus on sleep and waking in the rat". Progress in Neuro-psychopharmacology & Biological Psychiatry 30 (7): 1189–95. September 2006. doi:10.1016/j.pnpbp.2006.02.013. PMID 16713054. 
  6. ↑ "Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat". European Journal of Pharmacology 553 (1–3): 163–70. December 2006. doi:10.1016/j.ejphar.2006.09.027. PMID 17059817. 
  7. ↑ "The highly selective 5-hydroxytryptamine (5-HT)2A receptor antagonist, EMD 281014, significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test". Synapse 52 (1): 73–5. April 2004. doi:10.1002/syn.10308. PMID 14755634. 
  8. ↑ "Prophylactic and therapeutic effects of acute systemic injections of EMD 281014, a selective serotonin 2A receptor antagonist on anxiety induced by predator stress in rats". European Journal of Pharmacology 504 (1–2): 79–96. November 2004. doi:10.1016/j.ejphar.2004.09.017. PMID 15507224. 
  9. ↑ "Selective serotonin 5-HT2A receptor antagonist EMD 281014 improves delayed matching performance in young and aged rhesus monkeys". Psychopharmacology 179 (4): 725–32. June 2005. doi:10.1007/s00213-004-2114-1. PMID 15619109. 



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