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Antipsychotic
Vabicaserin
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    Vabicaserin

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    Vabicaserin
    Vabicaserin.svg
    Clinical data
    Routes of
    administration    		 By mouth
    ATC code
    • None
    Legal status
    Legal status
    • In general: uncontrolled
    Identifiers
    • (9aR,12aS)-4,5,6,7,9,9a,10,11,12,12a-Decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    CompTox Dashboard (EPA)
    Chemical and physical data
    Formula C15H21ClN2
    Molar mass 264.80 g·mol−1
    3D model (JSmol)
    • C1C[C@H]2CN3CCNCC4=C3C(=CC=C4)[C@H]2C1
    • InChI=1S/C15H20N2/c1-3-11-9-16-7-8-17-10-12-4-2-5-13(12)14(6-1)15(11)17/h1,3,6,12-13,16H,2,4-5,7-10H2/t12-,13-/m0/s1 ☒N
    • Key:NPTIPEQJIDTVKR-STQMWFEESA-N ☒N
     ☒NcheckY (what is this?)  (verify)

    Vabicaserin (codenamed SCA-136) was a novel antipsychotic and anorectic under development by Wyeth. As of 2010 it is no longer in clinical trials for the treatment of psychosis. It was also under investigation as an antidepressant but this indication appears to have been dropped as well.

    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). It is also a very weak antagonist at the 5-HT2A receptor (IC50 = 1,650 nM), though this action is not clinically significant. 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.

    See also


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