Imidafenacin(KRP-197; ONO-8025)是一种有效的和选择性的M3受体抑制剂，Kb值为0.317nM，对M2受体Kb值稍弱。

Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3) [1] in vitro: KRP-197 showed equipotent anti-M2 and anti-M3 activity and decreased subtype-selectivity [1]. in vivo: Intraduodenal administration of KRP-197 (0.04±0.30 mg/kg) inhibited bladder contraction dose-dependently, and the ED30 value was 0.11 mg/kg. The inhibitory action of KRP-197 on the bladder contraction was 19 times as potent as that of oxybutynin. KRP-197 showed preventive action against the decrease in bladder capacity induced by carbachol (ED50 0.074 mg/kg, intragastric administration), and the potency of the inhibitory action was 15-fold greater than that of oxybutynin [1]. The learning-inhibitory doses of intravenous oxybutynin hydrochloride and tolterodine tartrate were 0.3 and 3 mg/kg in sham-operated rats and 0.1 and 1 mg/kg

Solid

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Miyachi H, et al. Synthesis and antimuscarinic activity of a series of 4-(1-Imidazolyl)-2,2-diphenylbutyramides: discovery of potent and subtype-selective antimuscarinic agents. Bioorg Med Chem. 1999 Jun;7(6):1151-61.
[2]. Yamazaki T, et al. Imidafenacin has no influence on learning in nucleus basalis of Meynert-lesioned rats. Naunyn Schmiedebergs Arch Pharmacol. 2013 Dec;386(12):1095-102.

In Vitro: DMSO : 31.25 mg/mL (97.84 mM; ultrasonic and warming and heat to 60°C)配制储备液