4R-Hydroxy Solifenacin N-Oxide

Name	Solifenacin
Synonyms	YM 905 Solif·Nacin Solifenacin Unii-A8910sqj1u 4R-Hydroxy Solifenacin Solifenacin intermediate 4R-Hydroxy Solifenacin N-Oxide (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate (3R)-1-azabicyclo[2.2.2]oct-3-yl (1S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate [(8R)-1-azabicyclo[2.2.2]octan-8-yl] (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate 3,4-dihydro-1-phenyl-(1S)-2(1H)-Isoquinolinecarboxylic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester 2(1H)-Isoquinolinecarboxylicacid, 3,4-dihydro-1-phenyl-, (3R)-1-azabicyclo[2.2.2]oct-3-yl ester, (1S)-
CAS	242478-37-1
InChI	InChI=1/C23H26N2O2/c26-23(27-21-16-24-13-10-18(21)11-14-24)25-15-12-17-6-4-5-9-20(17)22(25)19-7-2-1-3-8-19/h1-9,18,21-22H,10-16H2/t21-,22-/m0/s1

Molecular Formula	C23H26N2O2
Molar Mass	362.47
Density	1.24±0.1 g/cm3(Predicted)
Boling Point	505.5±50.0 °C(Predicted)
Flash Point	259.5°C
Vapor Presure	2.41E-10mmHg at 25°C
pKa	9.03±0.33(Predicted)
Storage Condition	2-8℃
Refractive Index	1.648
In vitro study	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.
In vivo study	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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4R-Hydroxy Solifenacin N-Oxide

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