Imidafenacin (KRP-197) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors (IC50=4.13 nM). 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[3]. A single oral dose of imidafenacin 0.1 mg or 0.2 mg may contribute to the improvement of pulmonary function with excellent safety and tolerability in patients with chronic obstructive pulmonary disease[4]. 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 in nbM-lesioned rats, respectively[5]. Imidafenacin is a safe drug that may improve the urodynamic parameters of patients with SCI, and it possibly alleviates bladder complications[6].
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