Abstract
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 |
|---|---|
| Journal | Acta pharmacologica et Toxicologica |
| Volume | 52 |
| Issue number | 4 |
| Pages (from-to) | 246-53 |
| Number of pages | 8 |
| Publication status | Published - 1983 |
Keywords
- 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