Interactions of cryptosin with mammalian cardiac dihydropyridine-specific calcium channels

Cryptosin -a new cardenolide was found to be a potent inhibitor of cardiac Na+ and K+ dependent Adenosinetri-phosphatase (7). In experiments with dog heart ex vivo, development of inotropic and toxic effect correlated with changes in the cardiac dihydropyridine-specific calcium channels as measured by the binding of 3[H]PN 200-110. A significant change in the PN 200-110 binding was observed when guinea pig and dog heart sarcolemmal membranes were pre-incubated with cryptosin in vitro. Binding analysis of 3[H]PN 200-110 (Isradipine) - -a 1,4-dihydropyridine analog with very specific calcium channel binding properties - in both in vitro and ex vivo studies were consistent and indicated a non-specific type of interaction of cryptosin with mammalian cardiac 1,4-dihydropyridine-specific calcium channels.