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A possible action of nicardipine on the cardiac sarcolemmal Na+-Ca2+ exchange.

Abstract：

:The effects of nicardipine on sodium-calcium exchange activity of cardiac sarcolemma-enriched vesicles isolated from the rat heart were examined. Sodium-loaded, sarcolemma-enriched vesicles, when exposed to a medium containing 40 microM CaCl2, exhibited about 5 nmoles Ca2+/mg protein of the maximal calcium uptake; the initial rate was 21 nmoles Ca2+/mg protein/min. The calcium uptake was dependent on the extravesicular concentration of calcium ion. Nicardipine at concentrations of 0.1 to 10 microM depressed the rate of calcium uptake activity by 60-90%. The isolated membrane vesicles preloaded with Ca2+ showed a calcium efflux activity, when exposed to a medium containing sodium ion. The rate of calcium efflux was 2.5 nmoles Ca2+/mg protein/min, when measured in a medium containing 6.5 mM NaCl. The efflux rate was facilitated with increased concentrations of sodium ion in the medium. About 75% of the preloaded calcium in the vesicles was released within 3 min of incubation. The rate of calcium efflux was stimulated in the presence of 0.1 to 10 microM nicardipine (2.5- to 4-fold increase). The present results suggest a possible action of nicardipine on the sodium-calcium exchange mechanism at cardiac sarcolemmal sites.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Takeo S,Adachi K,Sakanashi M

doi

10.1016/0006-2952(85)90786-5

subject

Has Abstract

pub_date

1985-07-01 00:00:00

pages

2303-8

issue

13

eissn

0006-2952

issn

1873-2968

pii

0006-2952(85)90786-5

journal_volume

34

pub_type

杂志文章

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