Pesampator (PF-04958242) is a potent and highly selective positive allosteric modulator of AMPA receptor (an AMPA potentiator) with an EC50 of 310 nM and a Ki of 170 nM[1].
Pesampator (0.1-1 mg/kg; SC) dose-dependently increases CD-1 mouse cerebellum cGMP and Pesampator (0.1-0.32 mg/kg; SC) decreases fall latency in C57BL/6J mice traversing an accelerating rotarod[1].Pesampator (0.001-0.01 mg/kg; male Sprague-Dawley rats) reverses the MK-801-mediated (0.05 mg/kg; IV) reduction in paired-pulse facilitation (PPF) after cumulative or a single (0.01 mg/kg) intravenous dose[1].Pesampator (0.0032-0.032 mg/kg; SC) attenuates ketamine-induced working memory disruptions in rats as determined by mean errors in a radial arm maze[1].In rats, Pesampator (0.027, 0.08, and 0.60 mg/kg; SC) dose-dependently affectes the regional brain uptake of 2-deoxy-2-[18F]fluoro-d-glucose (FDG)[1].
[1]. Shaffer CL, et al. The discovery and characterization of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiator N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242). J Med Chem. 2015;58(10):4291-4308.