Pesampator (PF-04958242) is a potent, highly selective positive allosteric modulator of the AMPA receptor, also known as an AMPA potentiator, demonstrating an EC50 of 310 nM and a Ki of 170 nM [1].

Pesampator administered subcutaneously (0.1-1 mg/kg) dose-dependently enhances cerebellum cGMP levels in CD-1 mice and at a dosage of 0.1-0.32 mg/kg, it shortens fall latency in C57BL/6J mice on an accelerating rotarod [1]. Furthermore, at dosages ranging from 0.001 to 0.01 mg/kg in male Sprague-Dawley rats, Pesampator counteracts the MK-801-induced (0.05 mg/kg; IV) decrease in paired-pulse facilitation (PPF) whether given cumulatively or as a single dose of 0.01 mg/kg intravenously [1]. At concentrations between 0.0032 and 0.032 mg/kg, it mitigates ketamine-caused disturbances in working memory in rats, evidenced by reduced errors in a radial arm maze [1]. Additionally, Pesampator exhibits a dose-dependent influence on the regional brain absorption of 2-deoxy-2-[18F]fluoro-D-glucose (FDG) in rats at dosages of 0.027, 0.08, and 0.60 mg/kg [1].