Conti M, Setnikar I
Arch Int Pharmacodyn Ther. 1975 Feb;213(2):186-9.
The c-AMP phosphodiesterase inhibiting properties of flavoxate and of its main metabolite i.e. 3-methylflavone-8-carboxylic acid (MFCA), were assayed in vitro and compared to those of theophylline. Flavoxate and MFCA are competitive phosphodiesterase inhibitors, and are 21 and respectively 5 times more potent than theophylline. The smooth muscle relaxing activity of flavoxate possibly relies on this enzymatic mechanism.
在体外测定了黄酮哌酯及其主要代谢产物即3-甲基黄酮-8-羧酸(MFCA)对环磷酸腺苷磷酸二酯酶的抑制特性,并与茶碱的抑制特性进行了比较。黄酮哌酯和MFCA是竞争性磷酸二酯酶抑制剂,其效力分别比茶碱强21倍和5倍。黄酮哌酯的平滑肌舒张活性可能依赖于这种酶促机制。