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242478-37-1

中文名稱 索非那新
英文名稱 Solifenacin
CAS 242478-37-1
分子式 C23H26N2O2
分子量 362.46
MOL 文件 242478-37-1.mol
更新日期 2024/06/20 21:07:16
242478-37-1 結(jié)構(gòu)式 242478-37-1 結(jié)構(gòu)式

基本信息

中文別名
索非那新
索利那新-D5
4R-羥基索利那新
4R-羥基SOLIFENACIN N-氧化物
1-氮雜雙環(huán)[2.2.2]辛烷-8-基-(1S)-1-苯基-3,4-二氫-1H-異喹啉-2-甲酸酯
(8R)-1-氮雜雙環(huán)(2.2.2)辛烷-8-基-(1S)-1-苯基-3,4-二氫-1H-異喹啉-2-甲酸酯
(8R)-1-氮雜雙環(huán)(2.2.2)辛烷-8-基-(1S)-1-苯基-3,4-二氫-1H-異喹啉-2-甲酸酯 (索非那新)
英文別名
YM 905
Solifenacin
Solif·Nacin
Unii-A8910sqj1u
Solifenacin (YM905)
Solifenacin [inn:ban]
4R-Hydroxy Solifenacin
Solifenacin Succinate 2
4R-Hydroxy Solifenacin N-Oxide
(1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate

物理化學(xué)性質(zhì)

沸點(diǎn)505.5±50.0 °C(Predicted)
密度1.24±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : ≥ 50 mg/mL (137.95 mM);Water : < 0.1 mg/mL (insoluble)
酸度系數(shù)(pKa)9.03±0.33(Predicted)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

常見問題列表

生物活性
Solifenacin (YM905 free base) 是一種新型的毒蕈堿受體 (muscarinic receptor) 拮抗劑,對(duì) M1,M2 和 M3 受體的 pKi 值分別為 7.6, 6.9 和 8.0。
靶點(diǎn)

pKi: 7.6 (M 1 receptor), 6.9 (M 2 receptor), 8.0 (M 3 receptor)

體外研究

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.

體內(nèi)研究

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.

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