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180468-39-7

中文名稱 索利那新鹽酸鹽
CAS 180468-39-7
分子式 C23H26N2O2.ClH
分子量 398.931
MOL 文件 180468-39-7.mol
180468-39-7 結(jié)構(gòu)式 180468-39-7 結(jié)構(gòu)式

基本信息

中文別名
索利那新鹽酸鹽
英文別名
Solifenacin Succinate 3
Solifenacin Hydrochloride
(1S)-3,4-Dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic Acid (3R)-1-Azabicyclo-[2.2.2]oct-3-yl Ester Hydrochlorid
(1S)-3,4-Dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic Acid (3R)-1-Azabicyclo-[2.2.2]oct-3-yl Ester Hydrochloride
(1S)-3,4-Dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester hydrochloride (1:1)

物理化學(xué)性質(zhì)

熔點(diǎn)120-122°C
儲存條件Hygroscopic, -20°C Freezer, Under Inert Atmosphere

常見問題列表

生物活性
Solifenacin hydrochloride (YM905 hydrochloride) 是毒蕈堿受體 (muscarinic receptor) 拮抗劑,對 M1,M2 和 M3 受體的 pKi 值分別為 7.6, 6.9 和 8.0。
靶點(diǎn)

Muscarinic receptor

體外研究

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.

體內(nèi)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.

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