首页> 外文期刊>British Journal of Pharmacology >Involvement of ET_A and ET_B receptors in the activation of phospholipase D by endothelins in cultured rat cortical astrocytes
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Involvement of ET_A and ET_B receptors in the activation of phospholipase D by endothelins in cultured rat cortical astrocytes

机译:ET_A和ET_B受体参与内皮素在培养的大鼠皮质星形胶质细胞中激活磷脂酶D的作用

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摘要

This study was performed to characterize the receptor subtypes involved in the endothelin stimulation of phospholipase D(PLD) in rat cortical astrocytes in primary culture. PLD activity was determined by measuring the formation of [~32P]phosphatidylbutanol in [~32P]orthophosphate prelabelled cells stimulated in the presence of 25 mM butanol. The agonists enothelin-1 (ET-1), endothelin-3(ET-3), sarafotoxin 6c (S6c) and IRL 1620 elicited PLD activation in a concentration-dependent manner. The potencies of ET-1, ET-3 and S6c were Similar. The maximal effect evoked by the ET_B-preferring agonists, ET-3, S6c and IRL 1620, were Significantly lower than the maximal response to the non-selective agonist ET-1.
机译:进行这项研究来表征参与原代培养的大鼠皮质星形胶质细胞中内皮素刺激磷脂酶D(PLD)的受体亚型的特征。通过测量在25 mM丁醇存在下刺激的[〜32P]正磷酸预标记细胞中[〜32P]磷脂酰丁醇的形成来确定PLD活性。激动剂enothelin-1(ET-1),内皮素-3(ET-3),sarafotoxin 6c(S6c)和IRL 1620以浓度依赖的方式引起PLD活化。 ET-1,ET-3和S6c的效力相似。 ET_B优先激动剂ET-3,S6c和IRL 1620引起的最大作用明显低于对非选择性激动剂ET-1的最大反应。

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