Catalog No.S4027 Synonyms: NSC-114649
Molecular Weight(MW): 427.92
Flavoxate is a muscarinic AChR antagonist with IC50 of 12.2 μM.
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|Description||Flavoxate is a muscarinic AChR antagonist with IC50 of 12.2 μM.|
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). 
|In vivo||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. |
-  Dansette PM, et al. Exp Toxicol Pathol, 2000, 52(2), 145-148.
-  Kimura Y, et al. Int J Urol, 1996, 3(3), 218-227.
-  Oka M, et al. Brain Res, 1996, 727(1-2), 91-98.
|In vitro||Water||10 mg/mL (23.36 mM)|
|DMSO||3 mg/mL (7.01 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
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