| Literature DB >> 6210086 |
J F Renaud, J P Méaux, G Romey, A Schmid, M Lazdunski.
Abstract
The two dihydropyridines Bay K8644 and CGP 28392 increase 45Ca2+ influx in cultured rat cardiac cells with half-maximal effects at 2 nM and 30 nM respectively at a membrane potential of -75 mV. This stimulation of Ca2+ uptake is inhibited by nitrendipine, verapamil and bepridil. Ca2+ channel activation produced by Bay K8644 and CGP 28392 has been compared with Ca2+ channel activation produced by depolarization. There is no addition between the effects of drugs activating the Ca2+ channel and the effects of depolarization suggesting that Bay K8644 and CGP 28392 work preferentially on polarized membranes. 45Ca2+ flux experiments yielded results which are in excellent agreement with electrophysiological and contraction data obtained with the same cells in culture. Dose-response curves for the physiological effects of the drugs are observed over the same range of concentrations as their inhibition of [3H]nitrendipine binding to its receptor.Entities:
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Year: 1984 PMID： 6210086 DOI： 10.1016/s0006-291x(84)80382-4
Source DB: PubMed Journal: Biochem Biophys Res Commun ISSN： 0006-291X Impact factor: 3.575