Solifenacin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Solifenacin (YM905 free base) 是一种新型毒蕈碱受体拮抗剂，其对 M1、M2 和 M3 受体的 pK 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.

Solifenacin is a novel muscarinic receptor antagonist with pKis 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 Ca2+ 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 pKb values are obtained as 7.4±0.17 for Solifenacin and 8.8±0.21 for oxybutynin.

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.

YM905 free base

Endocrinology/Hormones

AChR

muscarinic receptor

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242478-37-1

362.46

C23H26N2O2

>98% (HPLC)

DMSO : 49 mg/mL (135.18 mM); H2O : < 0.1 mg/mL (insoluble)

O=C(N(CC1)[C@@H](c2ccccc2)c2c1cccc2)O[C@@H]1C(CC2)CCN2C1

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(-20℃)

With Ice Pack

≥ 2 years