Inhibition of sodium pump by bepridil. An in vitro and microcalorimetric study.

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Kovacic H, Gallice P, Crevat A

Inhibition of sodium pump by bepridil. An in vitro and microcalorimetric study.

Biochem Pharmacol. 1992 Oct 20;44(8):1529-34.

PubMed ID

1329768 [ View in PubMed

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Abstract

The effects of diltiazem, verapamil, bepridil, nicardipine and nifedipine were studied in vitro on Na+,K(+)-ATPase from dog kidney (EC 3.6.1.37). Except diltiazem, all the drugs tested showed an inhibitory effect on Na+,K(+)-ATPase activity in a dose-dependent manner. Among these drugs bepridil is far more effective than the others (IC50 approximately 10(-4) M). Competition studies showed that bepridil acted in a non-competitive manner with the ATP-Mg2+ complex and in a partially competitive manner with K+. Since ouabain acted similarly under the same experimental conditions, we tested the interaction of bepridil and ouabain on Na+,K(+)-ATPase. With low doses of ouabain, the enzyme inhibition corresponded to a potentiated synergy of the two drugs. We then studied the action of bepridil on the sodium pump activity of intact red blood cells by an ex vivo microcalorimetric technique. At 10(-5) M bepridil caused a significant decrease in sodium pump activity (33 +/- 8%).

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Bepridil	Sodium/potassium-transporting ATPase subunit alpha-1	Protein	Humans	Unknown	Inhibitor	Details