Pruvanserin Explained

Pruvanserin (EMD-281,014, LY-2,422,347) is a selective 5-HT_2A 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

• Eplivanserin
• Pimavanserin
• Glemanserin
• Roluperidone
• Volinanserin
• Ziprasidone
• Lenperone
• Lidanserin

Notes and References

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