Chemistry:Vabicaserin

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Short description: Chemical compound
Vabicaserin
Vabicaserin.svg
Clinical data
Routes of
administration		By mouth
ATC code
  • None
Legal status
Legal status
  • In general: uncontrolled
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC15H21ClN2
Molar mass264.80 g·mol−1
3D model (JSmol)
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Vabicaserin (codenamed SCA-136) was a novel antipsychotic and anorectic under development by Wyeth.[1] As of 2010 it is no longer in clinical trials for the treatment of psychosis.[1][2] It was also under investigation as an antidepressant but this indication appears to have been dropped as well.[3]

Vabicaserin acts as a selective 5-HT2C receptor full agonist (Ki = 3 nM; EC50 = 8 nM; IA = 100% (relative to 5-HT)) and 5-HT2B receptor antagonist (IC50 = 29 nM).[4][5][6] It is also a very weak antagonist at the 5-HT2A receptor (IC50 = 1,650 nM), though this action is not clinically significant.[4] By activating 5-HT2C receptors, vabicaserin inhibits dopamine release in the mesolimbic pathway, likely underlying its efficacy in alleviating positive symptoms of schizophrenia, and increases acetylcholine and glutamate levels in the prefrontal cortex, suggesting benefits against cognitive symptoms as well.[6][7][8]

See also

References

  1. ↑ 1.0 1.1 "Search of: vabicaserin - List Results". ClinicalTrials.gov. http://clinicaltrials.gov/ct2/results?term=vabicaserin. 
  2. ↑ Enzyme Inhibition in Drug Discovery .... John Wiley & Sons. 26 January 2010. ISBN 9780470538944. https://books.google.com/books?id=GS_98F19H74C&q=vabicaserin&pg=PA655. 
  3. ↑ Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. 2010. ISBN 978-0-470-51979-0. https://books.google.com/books?id=pfY3xcsu6EsC&q=vabicaserin%20antidepressant&pg=PA266. 
  4. ↑ 4.0 4.1 "5-HT2C receptor agonists as an innovative approach for psychiatric disorders". Drug News & Perspectives 20 (9): 565–571. November 2007. doi:10.1358/dnp.2007.20.9.1162244. PMID 18176661. 
  5. ↑ "Species differences in the formation of vabicaserin carbamoyl glucuronide". Drug Metabolism and Disposition 38 (4): 581–590. April 2010. doi:10.1124/dmd.109.028639. PMID 20032194. 
  6. ↑ 6.0 6.1 "Vabicaserin: effects of a novel 5HT2C agonist on medial prefrontal cortex neurotransmission, cognition and sensorimotor gating". The Journal of the European College of Neuropsychopharmacology 17 (Supplement 4): S484. doi:10.1016/S0924-977X(07)70740-X. http://91.142.242.133/07ecnp/index.cfm?fuseaction=CIS2002&hoofdnav=Abstracts&content=abs.details&what=AUTHOR&searchtext=beyer&topicselected=*&selection=ABSTRACT&qryStartRowDetail=1. 
  7. ↑ Stahl's essential psychopharmacology: neuroscientific basis and practical applications. Cambridge, UK: Cambridge University Press. 2008. p. 447. ISBN 978-0-521-85702-4. https://books.google.com/books?id=cWbYxSfKN3cC&q=vabicaserin&pg=PA447. 
  8. ↑ Targets and Emerging Therapies for Schizophrenia (3rd ed.). Hoboken, New Jersey: John Wiley & Sons, Inc. 2012. ISBN 9781118309384. 



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