vabicaserin

Vabicaserin is a small molecule drug that was developed as a novel antipsychotic and anorectic agent. It acts primarily as a potent and selective full agonist at the serotonin 2C receptor (5-HT2C) (EC50 = 8 nM; intrinsic activity = 100%), with additional antagonist activity at the serotonin 2B receptor (5-HT2B) (IC50 = 29 nM) and weak antagonism at the serotonin 2A receptor (5-HT2A) (IC50 = 1,650 nM), though this latter effect is not clinically significant. By activating the 5-HT2C receptor, vabicaserin inhibits dopamine release in the mesolimbic pathway—an action believed to underlie its potential efficacy for treating positive symptoms of schizophrenia—and increases acetylcholine and glutamate levels in the prefrontal cortex, suggesting possible benefits for cognitive symptoms. Preclinical studies indicated that it could improve mood disorders and cognitive impairment associated with schizophrenia without causing extrapyramidal side effects or weight gain. Vabicaserin reached phase II clinical trials for schizophrenia but was discontinued after demonstrating only moderate efficacy as monotherapy. It was also investigated for depression but development appears to have been dropped[1][5][6][7].

Other names

vabicaserin hydrochloride