Solifenacin 是一种新型的毒蕈碱受体拮抗剂，对M1、M2和M3受体的pKi值分别为 7.6、6.9 和 8.0。

Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist, its pKis for M1, M2 and M3 receptors is of 7.6, 6.9 and 8.0, respectively.

The inhibitory effects of Solifenacin 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). Solifenacin slightly increases saliva secretion at doses of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg). However, 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). 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.

242478-37-1

C23H26N2O2

362.473

索利那新;YM905 free base

DMSO:49 mg/mL (135.18 mM)
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years