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- Flavoxate hydrochloride 3717-88-2

- Flavoxate hydrochloride 3717-88-2
Flavoxate hydrochloride 3717-88-2
产品描述 描述 Flavoxate Hydrochloride(DW-61 Hydrochloride) is a muscarinic AChR antagonist used in various urinary syndromes and as an antispasmodic.
纯度 99%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 yan酸黄酮哌酯;Rec-7-0040;DW61外观 白色或类白色结晶性粉末可溶性/溶解性 DMSO : 3 mg/mL (7.01 mM)
Water : 10 mg/mL (23.36 mM)生物活性 靶点 mAChRIn vitro(体外研究) Flavoxate displaces nitrendipine on the Ca2+ channels binding sites with IC50 of 254 μM. Flavoxate (>10 μM) suppresses carbachol-induced contractions in isolated rat detrusor strips with pD value of 4.55. Flavoxate (>10 μM) suppresses Ca2+-induced contractions in isolated rat detrusor strips with pIC50 value of 4.92. Flavoxate (0.01 μM −10 μM) inhibits CAMP formation in a concentration-dependent manner in membranes from the rat striatum and cerebral cortex, an action which is completely abolished by pretreating the membranes with pertussis toxin (PTX). Flavoxate causes a concentration-dependent reduction of the K+-induced contraction of human urinary bladder. Flavoxate inhibits the peak amplitude of voltage-dependent nifedipine-sensitive inward Ba2+ currents in a voltage- and concentration-dependent manner with Ki value of 10 μM in human detrusor myocytes. Flavoxate inhibits voltage-dependent nifedipine-sensitive inward Ba2+ currents in human detrusor myocytes at both 30 degrees C (Ki = 5.1 mM) and 37 degrees C (Ki = 4.6 mM).In vivo(体内研究) Flavoxate (10mg/kg) suppresses both the an initial, rapidly rising phasic contraction (phase 1) and the tonic contraction (phase 2) contractions to the same extent in rats. Flavoxate (10mg/kg) abolishes the bladder contractions without causing any change in the amplitude of the contractions in rats. Flavoxate (3 mg/kg) abolishes the efferent neural activity and the associated bladder contractions for about 10 minutes without changing the baseline vesical pressure in rats. ICV-injected (50 to 200 μg/rat) or IT-injected (100 to 200 μg/rat) Flavoxate abolishes rhythmic bladder contractions during and after injection for five to 15 minutes in a dose-dependent manner in rats. Flavoxate (3 mg/kg, i.v.) abolishes rhythmic bladder contractions and the maximal intervals of voiding contractions is 7.20 min.参考文献 参考文献 1. Dansette PM, et al. Exp Toxicol Pathol, 2000, 52(2), 145-148.
2. Kimura Y, et al. Int J Urol, 1996, 3(3), 218-227.
3. Tomoda T, et al. Naunyn Schmiedebergs Arch Pharmacol, 2007, 376(3), 195-203.
研究领域 研究领域 Drug DiscoverySmall Molecule DrugLead Compound DiscoveryFlavoxate hydrochloride 3717-88-2温馨提示:本产品仅作科研实验使用,不支持临床等研究
