Zonampanel (YM 872) 是一种选择性的 AMPA 受体拮抗剂。

Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.

Solid

Zonampanel inhibits the human MRP4-mediated transport of [H]oestradiol 17-D-glucuronide in a concentration-dependent manner. In contrast, Zonampanel (up to 1000 mM) does not inhibit the human MRP2- or BCRP-mediated transport of [H]oestradiol 17-D-glucuronide or [H]methotrexate. Zonampanel inhibits the uptake of typical substrates by Oat1, Oat2, and Oat3 with inhibition constant (Ki) values of 7.02 to 10.4 μM. A time- and saturable concentration-dependent increase in [C]Zonampanel uptake is observed in these cells [Km values: 13.4 to 53.6 μM]. has not independently confirmed the accuracy of these methods. They are for reference only.

In in vivo experiments, probenecid and cimetidine decrease intrinsic clearance for both the renal secretion and biliary excretion of Zonampanel. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[1]. Minematsu T, et al. Characterization of renal tubular apical efflux of zonampanel, an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonist, in humans. Xenobiotica. 2008 Sep;38(9):1191-202.
[2]. Minematsu T, et al. Role of organic anion transporters in the pharmacokinetics of zonampanel, an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonist, in rats. Drug Metab Dispos. 2008 Aug;36(8):1496-504.

In Vitro: DMSO : 50 mg/mL (150.95 mM; ultrasonic and warming and heat to 60°C)配制储备液