242478-37-1 索非那新

• 生物活性 Solifenacin (YM905 free base) 是一种新型的毒蕈碱受体 (muscarinic receptor) 拮抗剂，对 M1，M2 和 M3 受体的 pKi 值分别为 7.6, 6.9 和 8.0。
• 靶点 pKi: 7.6 (M 1 receptor), 6.9 (M 2 receptor), 8.0 (M 3 receptor)
• 体外研究 Solifenacin is a novel muscarinic receptor antagonist with pK i s of 7.6±0.056, 6.9±0.034 and 8.0±0.021 for M1, M2 and M3 receptors, respectively. In murine submandibular gland cells, the antagonistic effects of 100 nM Solifenacin and oxybutynin on Ca 2+ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin does not shift the CCh dose-activation curve in a parallel manner whereas oxybutynin shows insurmountable antagonism. The pK b values are obtained as 7.4±0.17 for Solifenacin and 8.8±0.21 for oxybutynin.
• 体内研究 Solifenacin reduces bladder responses by 40% at a dose of 210 nmol/kg (0.1 mg/kg) and abolishes them at 2100 nmol/kg (1 mg/kg). In contrast, its inhibitory effects on salivary and cardiac responses are only slight at 630 nmol/kg (0.3 mg/kg), and reach 66% and 49%, respectively, at 2100 nmol/kg (1 mg/kg). At doses of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg), Solifenacin slightly increases saliva secretion. Solifenacin (0.01 to 0.3 mg/kg i.v.) dose-dependently increases bladder capacity and voided volume at doses of 0.03 mg/kg i.v. or more, but does not affect residual volume or micturition pressure at any dose tested.

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