Pesampator (PF-04958242) 是一种有效的、高选择性的 AMPA 受体的正变构调节剂 (AMPA 增强剂)，EC₅₀ 为 310 nM，K_i 为 170 nM。

Pesampator (PF-04958242) is a potent and highly selective positive allosteric modulator of AMPA receptor (an AMPA potentiator) with an EC 50 of 310 nM and a K i of 170 nM.

Solid

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.
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.
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.
In rats, Pesampator (0.027, 0.08, and 0.60 mg/kg; SC) dose-dependently affectes the regional brain uptake of 2-deoxy-2-[]fluoro-d-glucose (FDG). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (254.78 mM; Need ultrasonic)配制储备液