Pesampator (Synonyms: PF-04958242) |
| Catalog No.GC64929 |
Pesampator(PF-04958242)는 EC50이 310nM이고 Ki가 170nM인 AMPA 수용체(AMPA 강화제)의 강력하고 고도로 선택적인 양성 알로스테릭 조절제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1258963-59-5
Sample solution is provided at 25 µL, 10mM.
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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.
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