中文名 | Solifenacin Hydrochloride |
英文名 | Solifenacin Hydrochloride |
别名 | 索利那新盐酸盐 化合物 T23379 |
英文别名 | YM905 hydrochloride YM905 HYDROCHLORIDE YM 905 hydrochloride YM 905 HYDROCHLORIDE YM-905 hydrochloride YM-905 HYDROCHLORIDE VESICARE HYDROCHLORIDE Vesicare hydrochloride Solifenacin Hydrochloride (1S)-3,4-Dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic Acid (3R)-1-Azabicyclo-[2.2.2]oct-3-yl Ester Hydrochlorid |
CAS | 180468-39-7 |
化学式 | C23H27ClN2O2 |
分子量 | 398.93 |
熔点 | 120-122°C |
溶解度 | DMSO (微溶) 、乙醇 (微溶) 、甲醇 (微溶) |
存储条件 | Hygroscopic, -20°C Freezer, Under Inert Atmosphere |
稳定性 | 吸湿性 |
外观 | 固体 |
颜色 | White to Off-White |
体外研究 | Solifenacin hydrochloride (YM905 hydrochloride) 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 hydrochloride and oxybutynin on Ca 2+ mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin hydrochloride 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 hydrochloride and 8.8±0.21 for oxybutynin. |
体内研究 | Solifenacin hydrochloride (YM905 hydrochloride) 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 hydrochloride slightly increases saliva secretion. Solifenacin hydrochloride (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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.507 ml | 12.534 ml | 25.067 ml |
5 mM | 0.501 ml | 2.507 ml | 5.013 ml |
10 mM | 0.251 ml | 1.253 ml | 2.507 ml |
5 mM | 0.05 ml | 0.251 ml | 0.501 ml |
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