Coronary vasodilatory, spasmolytic and cAMP-phosphodiesterase inhibitory properties of dihydropyranocoumarins and dihydrofuranocoumarins
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Twenty-three dihydropyrano- and dihydrofuranocoumarins, most of plant origin, were examined for their effects on the coronary flow of isolated perfused guinea-pig heart, on the Ba2+-induced spasms in isolated guinea-pig ileum, on the cAMP level in guinea-pig heart homogenate and on the cAMP metabolising activity of purified beef heart cAMP-phosphodiesterase. For certain esters of dihydropyranocoumarin- and dihydrofuranocoumarin alcohols coronary vasodilatory and spasmolytic activities comparable to those of papaverine were observed. A very close correlation between the coronary vasodilatory and the spasmolytic activity was found. The most potent structures maximally increased the cAMP level from 19 pmol/mg protein to about 60 pmol/mg protein and inhibited the cAMP-phosphodiesterase activity with about 90%. The potencies were comparable to those of papaverine. A significant correlation was obtained between the coronary vasodilatory and the cAMP-phosphodiesterase inhibitory activity. The results indicate involvement of cAMP-phosphodiesterase inhibition in coronary vasodilatory effects of acyloxydihydropyrano- and acyloxydihydrofurano-coumarins.
Original language | English |
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Journal | Acta pharmacologica et Toxicologica |
Volume | 52 |
Issue number | 4 |
Pages (from-to) | 246-53 |
Number of pages | 8 |
Publication status | Published - 1983 |
- 3',5'-Cyclic-AMP Phosphodiesterases, Animals, Coronary Circulation, Coumarins, Cyclic AMP, Dose-Response Relationship, Drug, Guinea Pigs, Male, Muscle Contraction, Muscle, Smooth, Myocardium, Parasympatholytics, Vasodilator Agents
Research areas
ID: 43350702