CP-615003 is a potent and subtype-selective partial agonist of GABA A receptor ( GABA A receptor ) ( K i = 1.1 μM). CP-615003 is mainly converted into the active metabolite CP-900725 through oxidative deamination in monkeys and humans, and the latter also has GABA A receptor affinity. CP-615003 is a substrate of P-glycoprotein (P-gp/MDR1), resulting in severe limitation of its penetration into the central nervous system (CNS). CP-615003 can be used for the study of CNS-related indications.
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