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Molecular Pharmacology, Vol 15, 174-178, Copyright © 1979 by the American Society for Pharmacology and Experimental Therapeutics

Inhibition of Sodium Channels by D600

JONAS B. GALPER 1 and WILLIAM A. CATTERALL 1

1 Laboratory of Biochemical Genetics, National Heart, Lung, and Blood Institute, National Institutes of Health, Bethesda, Maryland 20014

D6OO, an inhibitor of the slow inward Ca++/Na+ current during the plateau phase of the cardiac action potential, also inhibits veratridine-activated fast sodium channels in both cultured heart cells and cultured neuroblastoma cells. The inhibition is competitive with respect to veratridine and is antagonized by Ca++. The KI for D600 in the presence of 1.8 mM Ca++ is approximately 3 µM.

Submitted on April 24, 1978
Accepted on September 11, 1978




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