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An effect of ischemia on myocardial dihydropyridine binding sites.

Abstract：

:The [3H]nitrendipine binding activity of sarcolemmal fragments isolated from aerobically perfused or ischemic rat hearts was studied. After 90 min aerobic perfusion, two populations of binding sites were detected--high affinity sites with KD of 0.24 +/- 0.04 nM and Bmax 313 +/- 110 fmol/mg protein, and low affinity sites with KD of 47.6 +/- 8.7 nM and Bmax 12.4 +/- 1.88 pmol/mg protein. Sixty minutes global ischemia significantly reduced the KD of the low (15.8 +/- 2.9 nM, P less than 0.03) but not of the high (0.22 +/- 0.05 nM) affinity sites. Under these same conditions the Bmax of both the high (82.4 +/- 14.5 fmol/mg protein, P less than 0.03) and low (6.1 +/- 1.7 pmol/mg protein, P less than 0.01) affinity binding sites was reduced but the sites retained their selectivity, with nifedipine displacing bound [3H]nitrendipine more potently than D600. Bay K 8644, when added upon reperfusion, promoted a dose-related increase in Ca2+ entry which was reduced by nifedipine, indicating that dihydropyridine binding sites can be activated after 60 min ischemia.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Nayler WG,Dillon JS,Elz JS,McKelvie M

doi

10.1016/0014-2999(85)90587-4

subject

Has Abstract

pub_date

1985-09-10 00:00:00

pages

81-9

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(85)90587-4

journal_volume

115

pub_type

杂志文章

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