Specific receptors for endothelin‐3 in cultured bovine endothelial cells and its cellular mechanism of action

FEBS Letters

Hirata, Yukio¹  Marumo, Fumiaki¹  Emori, Toshiaki¹ 

[1] Second Department of Internal Medicine, Tokyo Medical and Dental University, Tokyo 113, Japan

关键词: Endothelin-3;    Endothelial cell;    Vasodilatation;   

DOI  :  10.1016/0014-5793(90)81388-5

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Among three endothelin (ET) isopeptides, ET-3 shows the most potent initial depressor response through the endothelium-dependent mechanism. We studied the presence of specific binding sites for ET-3 in cultured bovine endothelial cells (EC) and its cellular mechanism of action. Binding studies revealed the presence of two distinct subclasses of ET-3 receptors with high and low affinities. ET-3 dose-dependently (10⁻¹⁰−10⁻⁷ M) increased both intracellular Ca²⁺ levels ([Ca⁻²]) and inositol trisphosphate (IP₃) formation. The ET-3-induced increase in [Ca²⁺]_i was not affected by either removal of extracellular Ca²⁺ or Ca²⁺-channel blockers. These data suggest that ET-3 induces phosphoinositide breakdown and increase in [Ca²⁺]_i in ECs, possibly resulting from intracellular Ca²⁺ mobilization, thereby leading to vasodilatation.

【 授权许可】

Unknown