索非那新
中文名称 | 索非那新 |
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中文同义词 | 1-氮杂双环[2.2.2]辛烷-8-基-(1S)-1-苯基-3,4-二氢-1H-异喹啉-2-甲酸酯;索非那新;索利那新-D5;4R-羟基索利那新;4R-羟基SOLIFENACIN N-氧化物;(8R)-1-氮杂双环(2.2.2)辛烷-8-基-(1S)-1-苯基-3,4-二氢-1H-异喹啉-2-甲酸酯 (索非那新);(8R)-1-氮杂双环(2.2.2)辛烷-8-基-(1S)-1-苯基-3,4-二氢-1H-异喹啉-2-甲酸酯;索非那新及其中间体 |
英文名称 | Solifenacin |
英文同义词 | Unii-A8910sqj1u;3,4-dihydro-1-phenyl-(1S)-2(1H)-Isoquinolinecarboxylic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester;YM 905;(1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate;2(1H)-Isoquinolinecarboxylicacid, 3,4-dihydro-1-phenyl-, (3R)-1-azabicyclo[2.2.2]oct-3-yl ester, (1S)-;Solif·Nacin;4R-Hydroxy Solifenacin;4R-Hydroxy Solifenacin N-Oxide |
CAS号 | 242478-37-1 |
分子式 | C23H26N2O2 |
分子量 | 362.46 |
EINECS号 | |
相关类别 | 医药中间体;肠胃泌尿生殖系统类;医药原料;VESICARE |
Mol文件 | 242478-37-1.mol |
结构式 |
索非那新 性质
沸点 | 505.5±50.0 °C(Predicted) |
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密度 | 1.24±0.1 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | DMSO:≥ 50 mg/mL (137.95 mM);水:< 0.1 mg/mL(不溶) |
形态 | 固体 |
酸度系数(pKa) | 9.03±0.33(Predicted) |
颜色 | 白色至米白色 |
pKi: 7.6 (M 1 receptor), 6.9 (M 2 receptor), 8.0 (M 3 receptor)
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-A0034 | Solifenacin | 5 mg | 312元 | |
2024/08/19 | HY-A0034 | 索非那新 Solifenacin | 242478-37-1 | 10mg | 500元 |