Solifenacin succinate

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 Succinate (YM905; Vesicare) 是一种毒蕈碱受体拮抗剂。

Solifenacin Succinate(YM905; Vesicare) is a muscarinic receptor antagonist.(In Vitro):Solifenacin Succinate (YM905) 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 Succinate and oxybutynin on Ca2+ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin Succinate 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 Succinate and 8.8±0.21 for oxybutynin. (In Vivo):Solifenacin Succinate (YM905) 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 Succinate slightly increases saliva secretion. Solifenacin Succinate (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.

Solifenacin Succinate (YM905) 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 Succinate and oxybutynin on Ca2+ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin Succinate 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 Succinate and 8.8±0.21 for oxybutynin.

Solifenacin Succinate (YM905) 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 Succinate slightly increases saliva secretion. Solifenacin Succinate (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.

Isoprenalinoe sulfate | YM-67905

Endocrinology/Hormones

AChR

mAChR

Neurological Disease

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242478-38-2

480.56

C23H26N2O2·C4H6O4

>98% (HPLC)

Ethanol: 5 mg/mL (10.4 mM); Water: 96 mg/mL (199.77 mM); DMSO: 3 mg/mL (6.24 mM)

C1CN2CCC1[C@H](C2)OC(=O)N3CCC4=CC=CC=C4[C@@H]3C5=CC=CC=C5.C(CC(=O)O)C(=O)O

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(-20℃)

With Ice Pack

≥ 2 years