由克隆的ETA内皮素受体介导的Et-1和Et-3作用对BQ-123表现出不同的敏感性。

Et-1 and Et-3 actions mediated by cloned ETA endothelin receptors exhibit different sensitivities to BQ-123.

作者信息

Gresser O, Chayard D, Herbert D, Cousin M A, Le Moullec J M, Bouattane F, Guedin D, Frelin C

机构信息

Institut de Pharmacologie Moléculaire et Cellulaire du CNRS, Valbonne, France.

出版信息

Biochem Biophys Res Commun. 1996 Jul 5;224(1):169-71. doi: 10.1006/bbrc.1996.1002.

DOI:10.1006/bbrc.1996.1002

PMID:8694806

Abstract

Et-1 and Et-3 activate phospholipase C in fibroblasts expressing cloned ETA receptors of bovine, rat and human origins. BQ-123 competitively antagonizes both responses but Et-3 actions are 10 times more sensitive to BQ-123 than Et-1 actions. It is suggested that differential sensitivity to BQ-123 is an intrinsic property of Et-1 and Et-3 activated ETA receptors and that there is no need to postulate the existence of new ETA receptor isoforms to account for singular actions of BQ-123.

摘要

内皮素-1（Et-1）和内皮素-3（Et-3）可激活表达牛、大鼠和人源克隆ETA受体的成纤维细胞中的磷脂酶C。BQ-123竞争性拮抗这两种反应，但Et-3的作用对BQ-123的敏感性比对Et-1的作用高10倍。有人提出，对BQ-123的不同敏感性是Et-1和Et-3激活的ETA受体的固有特性，并且无需假定存在新的ETA受体亚型来解释BQ-123的独特作用。