Endothelin‐induced intracellular Ca2+ mobilization through its specific receptors in murine peritoneal macrophages

FEBS Letters

Kato, Toshiyuki¹  Hanasaki, Kohji¹  Arita, Hitoshi¹  Kishino, Junji¹ 

[1] Shionogi Research Laboratories, Shionogi and Co. Ltd., Fukushima-ku, Osaka 553, Japan

关键词: Endothelin;    Receptor binding;    Cytosolic free Ca2+;    Peritoneal macrophages;    Mouse;    ET;    endothelin;    [Ca2+]i;    intracellular free Ca2+ concentration;   

DOI  :  10.1016/0014-5793(91)80214-N

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

We studied the presence of specific binding sites for endothelin (ET) and the effect of ET on cytosolic free Ca²⁺ concentration ([Ca²⁺]_i) in murine thiogylcolate-activated peritoneal macrophages. Scatchard analysis for binding experiments using [¹²⁵I]ET-1 or [¹²⁵I]ET-3 revealed the existence of a single class of binding sites. The binding parameters (K??? and B???) for [¹²⁵I]ET-1 were almost identical to those for [¹²⁵I]ET-3. In addition, unlabeled 3 ET isopeptides (ET-1, ET-2 and ET-3) inhibited the specific binding of both ET-1 and ET-3 with similar inhibitory potencies. All 3 ET isopeptides caused an increase in [Ca²⁺]_i in the same dose-dependent manner (0.01–100nM). These results demonstrate the existence of an ET receptor with the same affinity for all isoforms that mediates the ET-induced intracellular Ca²⁺ mobilization in murine peritoneal macrophages.

【 授权许可】

Unknown