人 big-内皮素-1 和内皮素-1 通过激活大鼠灌注肺中的 ET1 受体释放前列环素。
Human big-endothelin-1 and endothelin-1 release prostacyclin via the activation of ET1 receptors in the rat perfused lung.
作者信息
D'Orléans-Juste P, Télémaque S, Claing A, Ihara M, Yano M
机构信息
Department of Pharmacology, Medical School, Université de Sherbrooke, Québec, Canada.
出版信息
Br J Pharmacol. 1992 Apr;105(4):773-5. doi: 10.1111/j.1476-5381.1992.tb09055.x.
Abstract
Although ET1 and ET2 binding sites were found in rat lung membranes, a selective ET1 receptor antagonist, BQ-123 (10 microM), did not displace [125I]-endothelin-1 ([125I]ET-1) from ET2 sites, illustrating the selectivity of the angatonist for ET1 receptors. In rat perfused lungs, BQ-123 (1 microM) markedly reduced the prostacyclin (PGI2) releasing properties of endothelin-1 (ET-1: 5 nM) and human big-ET-1 (100 nM) suggesting that both peptides induce the release of PGI2 via the selective activation of ET1 receptors.
摘要
尽管在大鼠肺膜中发现了ET1和ET2结合位点，但选择性ET1受体拮抗剂BQ - 123（10微摩尔）并未从ET2位点取代[125I] - 内皮素 - 1（[125I]ET - 1），这说明了该拮抗剂对ET1受体的选择性。在大鼠灌注肺中，BQ - 123（1微摩尔）显著降低了内皮素 - 1（ET - 1：5纳摩尔）和人big - ET - 1（100纳摩尔）的前列环素（PGI2）释放特性，这表明这两种肽均通过选择性激活ET1受体诱导PGI2的释放。
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