内皮素ETA受体与人类右心房中肌醇磷酸的形成及腺苷酸环化酶的抑制相关联。
Endothelin ETA-receptors couple to inositol phosphate formation and inhibition of adenylate cyclase in human right atrium.
作者信息
Vogelsang M, Broede-Sitz A, Schäfer E, Zerkowski H R, Brodde O E
机构信息
Biochemical Research Laboratory, Medizinische Klinik and Poliklinik, University of Essen, Germany.
出版信息
J Cardiovasc Pharmacol. 1994 Feb;23(2):344-7.
To study signal transduction pathways of endothelin (ET) in human heart, we assessed, in isolated human right atria, the effects of ET-1 and ET-3 on inositol phosphate (IP) formation and on the adenylate cyclase/cyclic AMP system. In right atrial slices, ET-1 (10(-10)-10(-6)M) concentration-dependently increased [3H]IP accumulation and decreased 10-microM isoprenaline-induced or 1-microM forskolin-induced increases in cyclic AMP content. ET-3 was approximately 100 times less potent. The cyclic AMP-decreasing effect of ET-1 (10(-11)-10(-6)M) could also be demonstrated directly in adenylate cyclase assays in right atrial membranes; again, ET-3 was approximately 100 times less potent. We conclude that in human right atrium, ETA receptors couple to two different signal-transduction pathways: IP formation and inhibition of adenylate cyclase.
为研究内皮素（ET）在人心脏中的信号转导途径，我们在离体的人右心房中评估了ET-1和ET-3对肌醇磷酸（IP）生成以及对腺苷酸环化酶/环磷酸腺苷（cAMP）系统的影响。在右心房切片中，ET-1（10⁻¹⁰ - 10⁻⁶M）浓度依赖性地增加[³H]IP积累，并降低10μM异丙肾上腺素或1μM福斯高林诱导的cAMP含量增加。ET-3的效力约低100倍。ET-1（10⁻¹¹ - 10⁻⁶M）降低cAMP的作用也可在右心房膜的腺苷酸环化酶测定中直接证明；同样，ET-3的效力约低100倍。我们得出结论，在人右心房中，ETA受体与两种不同的信号转导途径偶联：IP生成和腺苷酸环化酶抑制。
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