Vabicaserin

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Vabicaserin
File:Vabicaserin.png
Systematic (IUPAC) name
(9aR,12aS)-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline
Clinical data
Routes of
administration
Oral
Legal status
Legal status
  • Uncontrolled
Identifiers
CAS Number 620948-34-7
ATC code none
PubChem CID 11658860
Chemical data
Formula C15H21ClN2
Molar mass 264.79 g/mol[[Script error: No such module "String".]]
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Vabicaserin (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.[7][6]

See also

References

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  1. Jump up to: 1.0 1.1 "Search of: vabicaserin - List Results - ClinicalTrials.gov". 
  2. Jump up "Enzyme Inhibition in Drug Discovery ... - Google Books". 
  3. Jump up Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 0-470-51979-7. 
  4. Jump up to: 4.0 4.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  5. Jump up Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  6. Jump up to: 6.0 6.1 "ECNP-2007 CIS". 
  7. Jump up Stahl's essential psychopharmacology: neuroscientific basis and practical applications. Cambridge, UK: Cambridge University Press. 2008. ISBN 0-521-85702-3.