- 英文名称
- Solifenacin
- 分子式
- C23H26N2O2
- 分子量
- 362.46
- 中文别名
- 索利那新; 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; (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; YM 905; 3,4-dihydro-1-phenyl-(1S)-2(1H)-Isoquinolinecarboxylic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester; (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; (1S)-(3R)- Form; solifenacin; [(8R)-1-azabicyclo[2.2.2]octan-8-yl] (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate; (+)-solifenacin; 1-Azabicyclo[2.2.2]oct-3-yl (1S)-1-phenyl-3,4-dihydro-2(1H)-isoquinolinecarboxylate; (3R)-1-Azabicyclo[2.2.2]oct-3-yl (1S)-1-phenyl-3,4-dihydro-2(1H)-isoquinolinecarboxylate; (1S)-(3R)-1-azabicyclo[2,2,2]oct-3-yl-3,4-dihydro-1-phenyl-2(1H)-isoquinoline carboxylate; (3R)-1-Azabicyclo[2.2.2]oct-3-yl (1S)-3,4-dihydro-1-phenyl-2(1H)-Isoquinolinecarboxylate; Vesicare; 2(1H)-Isoquinolinecarboxylic acid,3,4-dihydro-1-phenyl-,1-azabicyclo(2.2.2)oct-3-yl ester,(R-(R*,S*)); (1S,3'R)-quinuclidin-3'-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate
- 用途
- - 生物活性
Solifenacin (YM905 free base) 是一种新型的毒蕈碱受体 (muscarinic receptor) 拮抗剂，对 M1，M2 和 M3 受体的 pKi 值分别为 7.6, 6.9 和 8.0。
- 靶点
pKi: 7.6 (M
1
receptor), 6.9 (M
2
receptor), 8.0 (M
3
receptor)
- 体外研究
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.
- 体内研究
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.
