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当前位置: 首页 > 信号通路研究 > AChR > Flavoxate HCl
Flavoxate HCl
Flavoxate HCl
Flavoxate HCl
商品货号:CL-10811
CAS 号:3717-88-2
英文名字:Flavoxate HCl
质量标准:>98%, AChR 拮抗剂
分子式:C24H25NO4.HCl
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商品信息

质检证书(coa)

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 Flavoxate HCl

分子式:C24H25NO4.HCl   分子量427.92

 

产品描述

Flavoxate 是一种毒蕈碱受体 AChR 拮抗剂, IC50 12.2 μM.

靶点

AChR

         

IC50

12.2 μM

         

体外研究

Flavoxate displaces [3H]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).

体内研究

Flavoxate (10mg/kg) suppresses both the an initial, rapidly rising phasic contraction and the tonic contraction  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.

溶解性

DMSO 3 mg/mL,水 10 mg/mL,乙醇 <1 mg/mL

稳定性

2 -20°C粉状,6-80°C溶于DMSO

特征

         

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