title: Pharmacological activities of the main metabolite of flavoxate 3-methylflavone-8-carboxylic acid.
abstract: The pharmacological properties of 3-methylflavone-8-carboxylic acid (MFCA), the main metabolite of flavoxate, have been studied in vitro and in vivo. MFCA did not display antispasmodic activity on isolated organs contractions induced by histamine, acetylcholine or CaCl2, nor did it exhibit significant affinity for the rat brain alpha- and beta-adrenergic, serotoninic, muscarinic, D2, opiate and Ca2+ receptors. However, it showed a remarkable phosphodiesterase (PDE) inhibiting activity. Moreover in vivo studies indicate an interesting activity of MFCA which inhibited the rat urinary bladder voiding contractions, increased bladder volume capacity and decreased micturition pressure in the rat cystometric recordings. The activity of MFCA in the two in vivo experimental models, probably related to cAMP-PDE inhibitory properties, suggests that flavoxate's therapeutical potential might be partially sustained by its main metabolite.
authors.affiliation: Research Division, Recordati S.p.a., Milan, Italy.
authors.forename: P
authors.initials: P
authors.lastname: Cazzulani
authors.forename: C
authors.initials: C
authors.lastname: Pietra
authors.forename: G A
authors.initials: GA
authors.lastname: Abbiati
authors.forename: R
authors.initials: R
authors.lastname: Ceserani
authors.forename: D
authors.initials: D
authors.lastname: Oliva
authors.forename: M
authors.initials: M
authors.lastname: Civelli
authors.forename: A
authors.initials: A
authors.lastname: Tajana
authors.forename: D
authors.initials: D
authors.lastname: Nardi
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors; D000818:Animals; D002121:Calcium Channel Blockers; D005260:Female; D005419:Flavonoids / Q000494:pharmacology*; D005422:Flavoxate / Q000031:analogs & derivatives / Q000494:pharmacology*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011955:Receptors, Drug / Q000187:drug effects; D001743:Urinary Bladder / Q000187:drug effects
chemical_list: D002121:Calcium Channel Blockers; D005419:Flavonoids; D011955:Receptors, Drug; D005422:Flavoxate; D015105:3',5'-Cyclic-AMP Phosphodiesterases; C011504:3-methylflavone-8-carboxylic acid