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胃前列腺素E2受体是黏膜类前列腺素常见的抗分泌靶点。

Gastric prostaglandin E2 receptors are the common antisecretory target of mucosal prostanoids.

作者信息

Hennies S, Beinborn M, Sewing K F

机构信息

Department of General Pharmacology, Medical School, Hannover, Germany.

出版信息

Eur J Pharmacol. 1992 Aug 6;218(2-3):303-10. doi: 10.1016/0014-2999(92)90183-5.

Abstract

The gastric mucosa produces all principal prostaglandin (PG) types, but receptor binding studies in this tissue have as yet been performed exclusively with [3H]PGE2. Therefore we compared the binding of different 3H-labelled prostanoids to fundic mucosal plasma membranes from the porcine stomach. Binding sites for [3H]PGE2, [3H]iloprost and [3H]PGF2 alpha had similar nanomolar dissociation constants with high affinities for unlabelled PGE2. Iloprost and PGF2 alpha were 10- and 100-fold less potent competitors with Hill slopes near unity in all cases. In further [3H]PGE2 competition studies the affinities of prostanoid ligands with selectivity for different PG receptor types correlated closely with their respective antisecretory potencies, as tested by [14C]aminopyrine uptake in isolated porcine parietal cells. We conclude that parietal cell PGE2 receptors are the common antisecretory target for all prostanoid types in the porcine stomach. There was no evidence for other mucosal PG receptors possibly involved in acid secretion.

摘要

胃黏膜可产生所有主要类型的前列腺素(PG),但目前该组织中的受体结合研究仅使用[3H]PGE2进行。因此,我们比较了不同3H标记的前列腺素与猪胃底黏膜质膜的结合情况。[3H]PGE2、[3H]依洛前列素和[3H]PGF2α的结合位点具有相似的纳摩尔解离常数,对未标记的PGE2具有高亲和力。在所有情况下,依洛前列素和PGF2α作为竞争性配体的效力分别低10倍和100倍,希尔系数接近1。在进一步的[3H]PGE2竞争性研究中,对不同PG受体类型具有选择性的前列腺素配体的亲和力与它们各自的抗分泌效力密切相关,这是通过分离的猪壁细胞中[14C]氨基比林摄取试验测得的。我们得出结论,壁细胞PGE2受体是猪胃中所有前列腺素类型共同的抗分泌靶点。没有证据表明存在其他可能参与胃酸分泌的黏膜PG受体。

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