Pruvanserin

In this article we are going to explore the fascinating world of Pruvanserin. From its origins to its impact on today's society, Pruvanserin has played a fundamental role in various aspects of daily life. Throughout history, Pruvanserin has been a source of debate and controversy, giving rise to endless opinions and theories. In this sense, it is essential to critically and objectively analyze the influence of Pruvanserin on our culture, politics, economy and daily life. Likewise, it is crucial to examine how Pruvanserin has evolved over time and what the implications are of its presence today. Through this exploration, we hope to shed light on the meaning and impact of Pruvanserin in the contemporary world.

Pruvanserin
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • 7-({4-piperazin-1-yl}carbonyl)-1H-indole-3-carbonitrile
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H21FN4O
Molar mass376.435 g·mol−1
3D model (JSmol)
  • N#Cc2c1cccc(c1c2)C(=O)N4CCN(CCc3ccc(F)cc3)CC4

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. ^ Bartoszyk GD, van Amsterdam C, Böttcher H, Seyfried CA (July 2003). "EMD 281014, a new selective serotonin 5-HT2A receptor antagonist". European Journal of Pharmacology. 473 (2–3): 229–30. doi:10.1016/S0014-2999(03)01992-7. PMID 12892843.
  2. ^ Teegarden BR, Al Shamma H, Xiong Y (2008). "5-HT(2A) inverse-agonists for the treatment of insomnia". Current Topics in Medicinal Chemistry. 8 (11): 969–76. doi:10.2174/156802608784936700. PMID 18673166.
  3. ^ "Efficacy Study of LY2422347 to Treat Insomnia - Full Text View - ClinicalTrials.gov". 24 January 2007.
  4. ^ "Eli Lilly and Company » Research Pipeline".
  5. ^ Monti JM, Jantos H (September 2006). "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. doi:10.1016/j.pnpbp.2006.02.013. PMID 16713054. S2CID 12837755.
  6. ^ Monti JM, Jantos H (December 2006). "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. doi:10.1016/j.ejphar.2006.09.027. PMID 17059817.
  7. ^ Patel JG, Bartoszyk GD, Edwards E, Ashby CR (April 2004). "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. doi:10.1002/syn.10308. PMID 14755634. S2CID 21941333.
  8. ^ Adamec R, Creamer K, Bartoszyk GD, Burton P (November 2004). "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. doi:10.1016/j.ejphar.2004.09.017. PMID 15507224.
  9. ^ Terry AV, Buccafusco JJ, Bartoszyk GD (June 2005). "Selective serotonin 5-HT2A receptor antagonist EMD 281014 improves delayed matching performance in young and aged rhesus monkeys". Psychopharmacology. 179 (4): 725–32. doi:10.1007/s00213-004-2114-1. PMID 15619109. S2CID 30366683.