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vabicaserin

n. An antipsychotic and anorectic drug.

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Vabicaserin

Vabicaserin (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-HT receptor full agonist (K = 3 nM; EC = 8 nM; IA = 100% (relative to 5-HT)) and 5-HT receptor antagonist (IC = 29 nM). It is also a very weak antagonist at the 5-HT receptor (IC = 1,650 nM), though this action is not clinically significant. By activating 5-HT 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.