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  • Title: Specific binding of a calcium channel activator, [3H]BAY k 8644, to membranes from cardiac muscle and brain.
    Author: Janis RA, Rampe D, Sarmiento JG, Triggle DJ.
    Journal: Biochem Biophys Res Commun; 1984 May 31; 121(1):317-23. PubMed ID: 6203531.
    Abstract:
    BAY k 8644 is a member of a new class of drugs that directly activates Ca2+ channels. This 1,4-dihydropyridine was found to bind to both high and low affinity sites on rabbit ventricular microsomes and guinea pig brain synaptosomes. The dissociation constant obtained from Scatchard analysis with [3H]BAY k 8644 was 2 to 3 nM for the high affinity binding site, and the estimated maximal number of binding sites was 0.8 and 0.4 pmol/mg protein for heart and brain membranes, respectively, at 15 degrees C. Competition between nitrendipine and [3H]BAY k 8644 indicated a common high affinity binding site for Ca2+ channel activators and antagonists. The results suggest that the 1,4-dihydropyridine Ca2+ channel antagonists do not act as simple channel plugs.
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