Enhancement of calcium influx in human platelets by CGP 28392, a novel dihydropyridine.
CGP 28392, a novel compound structurally related to the dihydropyridine Ca2+-entry blockers, causes a dose-dependent increase in intracellular free Ca2+ in human platelets, as measured with the Quin-2 Ca2+ indicator, with a semimaximal effective concentration of 2.2 X 10(-7) M. This effect occurs in a concentration range in which CGP 28392 competes for specific [3H]nitrendipine binding in guinea pig heart membranes. It can be inhibited by nitrendipine. The data presented furnish direct evidence of the Ca2+-entry-stimulating properties of CGP 28392 and indicate the presence of dihydropyridine-susceptible structures in human platelets.
D000818:Animals; D001792:Blood Platelets / Q000378:metabolism*; D002118:Calcium / Q000097:blood*; D002121:Calcium Channel Blockers / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006801:Humans; D007473:Ion Channels / Q000187:drug effects; D009206:Myocardium / Q000378:metabolism; D009543:Nifedipine / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D009568:Nitrendipine; D011725:Pyridines / Q000494:pharmacology*
D002121:Calcium Channel Blockers; D007473:Ion Channels; D011725:Pyridines; C040525:CGP 28392; D009568:Nitrendipine; D009543:Nifedipine; D002118:Calcium