The effects of prenylamine on single ventricular myocytes of guinea-pig.
1. The action of prenylamine, an antianginal drug, was studied in single ventricular guinea-pig myocytes. In concentrations of 10-50 microM, prenylamine significantly (P less than 0.01) shortened action potentials, and significantly (P less than 0.001) reduced the inward calcium current by 29% to 76% (n = 7). This effect was also present in the presence of adrenoceptor-blockade (with phentolamine and propranolol), and was thus not due to indirect changes in endogenous catecholamine action. 2. Prenylamine did not affect the steady state level of current at the end of long pulses, and does therefore not act by changing time-dependent outward currents. Since the resting potential in the unclamped mode is unchanged during gross changes in action potential duration, it is also unlikely that there are any changes in the background, time-independent potassium conductance. 3. It is concluded that prenylamine has a direct effect on cardiac calcium channels, not mediated by adrenoceptor activation.
Shimoni
Y
Y
University Laboratory of Physiology, Oxford.
Posner
P
P
Spindler
A J
AJ
Noble
D
D
D000818:Animals; D002118:Calcium / Q000378:metabolism; D002395:Catecholamines / Q000378:metabolism; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects*; D006352:Heart Ventricles; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D009206:Myocardium / Q000166:cytology; D011299:Prenylamine / Q000494:pharmacology*; D011941:Receptors, Adrenergic / Q000187:drug effects
D002395:Catecholamines; D007473:Ion Channels; D011941:Receptors, Adrenergic; D011299:Prenylamine; D002118:Calcium