Lecozotan, formerly known as SRA-333, is a potent and selective 5-HT antagonist potentially for the treatment of Alzheimer's disease. Lecozotan (SRA-333) enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties. Lecozotan significantly potentiated the potassium chloride-stimulated release of glutamate and acetylcholine in the dentate gyrus of the hippocampus. Chronic administration of lecozotan did not induce 5-HT(1A) receptor tolerance or desensitization in a behaviorally bioavailable model indicative of 5-HT(1A) receptor function. Acute lecozotan administration increases learning and memory in rats without affecting anxiety or behaviorally bioavailable depression. References: Parks V, Philipp AW, Raje S, Plotka A, Schechter LE, Connell J, Chalon S. Concomitant blockade of 5-HT(1A) receptor and 5-HT transporter: use of the Hunter Serotonin toxicity criteria in a clinical pharmacology study. Eur Neuropsychopharmacol. 2012 Feb;22(2):92-9. doi: 10.1016/j.euroneuro.2011.06.002. PubMed PMID: 21733663.
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CAS:433282-68-9