DOWN-REGULATION OF ENDOTHELIN BINDING-SITES IN RAT VASCULAR SMOOTH-MUSCLE CELLS

被引：30

作者：

ROUBERT, P ^{[1
]}

GILLARD, V ^{[1
]}

PLAS, P ^{[1
]}

CHABRIER, PE ^{[1
]}

BRAQUET, P ^{[1
]}

机构：

[1] INST HENRI BEAUFOUR,1 AVE TROP,F-91952 LES ULIS,FRANCE

来源：

AMERICAN JOURNAL OF HYPERTENSION | 1990年 / 3卷 / 04期

关键词：

Down-regulation; Endothelin (ET-1); Receptors;

D O I：

10.1093/ajh/3.4.310

中图分类号：

R6 [外科学];

学科分类号：

1002 ; 100210 ;

摘要：

In cultured rat aortic smooth muscle cells, [125I]en-dothelin (ET-1) bound to an apparent single class of high affinity recognition sites with a dissociation constant of 1.84 ± 0.29 nmol/L and a maximum binding of 62 ± 10.5 fmol/106cells. The binding was not affected by calcium antagonists or vasoac-tive substances, including angiotensin II, arginine vasopressin, atrial natriuretic factor and brady-kinin. Exposure of the cells to ET-1 (0.01 nmol/L to 10 nmol/L) resulted in an apparent dose-dependent reduction of the number of endothelin binding sites with no significant modification of its binding affinity. The time course of the down-regulation of ET-1 binding sites showed that this effect was present after 30 min incubation and persisted after 18 h. This indicates that down-regulation of ET-1 binding sites can modulate the activity of ET-1 and suggests a rapid internalization of ET-1 in vascular cells. © 1990 by the American Journal of Hypertension, Ltd.

引用

页码：310 / 312

页数：3

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