In vitro activity: Flavoxate is an anticholinergic agent that binds and inhibits muscarinic receptors, thereby suppressing the micturition reflex and increases urinary bladder capacity by modifying the micturition center in the brain stem. As an anticholinergic, Flavoxate has the potential to be used in various urinary syndromes and as an antispasmodic. Flavoxate (3 mg/kg, i.v.) completely abolished rhythmic bladder contractions in vehicle-pretreated rats, but not in PTX-pretreated rats. These findings suggest that signal transduction via Gi-coupled receptors is involved, at least in part, in the inhibition of the micturition reflex by flavoxate in rats.

Cell Assay: 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).