Dynamic and kinetic differences of the vascular and myocardial effects of calcium antagonists in the rat heartvan Amsterdam, F. T. M., Haas, M. & Zaagsma, J., May-1987, In : Journal of Cardiovascular Pharmacology. 9, 5, p. 570-577 8 p.
Research output: Contribution to journal › Article › Academic › peer-review
We studied the effects of nifedipine, nimodi-pine, verapamil, D600 (gallopamil), D888 (desmethoxy-verapamil), D890 (quaternized verapamil), bepridil, and diltiazem on the coronary flow and the left ventricular pressure in the retrogradely perfused paced rat heart; in addition, we investigated the time course of onset and recovery of these effects. We found a clear difference in potency order for the vascular and cardiac effects as well as widely different kinetics of coronary flow increase and negative inotropic activity. Furthermore, positive inotropism at low doses of some calcium antagonists seemed to be related to the vascular effects of these compounds. We conclude that the rat heart contains a hydrophylic and readily accessible, vascular “dihydropyridine” site and a more hydrophobic, possibly intramembraneous or intracellular, myocardial “verapamil” site with a lower accessibility for verapamil derivatives and bepridi
|Number of pages||8|
|Journal||Journal of Cardiovascular Pharmacology|
|Publication status||Published - May-1987|