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Pruvanserin









Pruvanserin


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Pruvanserin
Pruvanserin.png
Clinical data
Routes of
administration		 Oral
ATC code
  • none
Legal status
Legal status

  • In general: uncontrolled
Identifiers
CAS Number

  • 443144-26-1
    443144-27-2 (hydrochloride)

PubChem CID
  • 6433122
ChemSpider
  • 4938310
UNII
  • UL09X1D9EM
ChEMBL
  • ChEMBL1215661
Chemical and physical data
Formula
C22H21FN4O
Molar mass 376.43 g/mol
3D model (JSmol)
  • Interactive image

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[edit]



  • Eplivanserin

  • Pimavanserin

  • Volinanserin



References[edit]





  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..mw-parser-output cite.citation{font-style:inherit}.mw-parser-output q{quotes:"""""""'""'"}.mw-parser-output code.cs1-code{color:inherit;background:inherit;border:inherit;padding:inherit}.mw-parser-output .cs1-lock-free a{background:url("//upload.wikimedia.org/wikipedia/commons/thumb/6/65/Lock-green.svg/9px-Lock-green.svg.png")no-repeat;background-position:right .1em center}.mw-parser-output .cs1-lock-limited a,.mw-parser-output .cs1-lock-registration a{background:url("//upload.wikimedia.org/wikipedia/commons/thumb/d/d6/Lock-gray-alt-2.svg/9px-Lock-gray-alt-2.svg.png")no-repeat;background-position:right .1em center}.mw-parser-output .cs1-lock-subscription a{background:url("//upload.wikimedia.org/wikipedia/commons/thumb/a/aa/Lock-red-alt-2.svg/9px-Lock-red-alt-2.svg.png")no-repeat;background-position:right .1em center}.mw-parser-output .cs1-subscription,.mw-parser-output .cs1-registration{color:#555}.mw-parser-output .cs1-subscription span,.mw-parser-output .cs1-registration span{border-bottom:1px dotted;cursor:help}.mw-parser-output .cs1-hidden-error{display:none;font-size:100%}.mw-parser-output .cs1-visible-error{font-size:100%}.mw-parser-output .cs1-subscription,.mw-parser-output .cs1-registration,.mw-parser-output .cs1-format{font-size:95%}.mw-parser-output .cs1-kern-left,.mw-parser-output .cs1-kern-wl-left{padding-left:0.2em}.mw-parser-output .cs1-kern-right,.mw-parser-output .cs1-kern-wl-right{padding-right:0.2em}


  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".


  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.


  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.


  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.













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