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使用犬壁细胞富集制剂和[3H]米索前列醇游离酸对特定E型前列腺素受体的证明。

Demonstration of specific E-type prostaglandin receptors using enriched preparations of canine parietal cells and [3H]misoprostol free acid.

作者信息

Tsai B S, Kessler L K, Schoenhard G, Collins P W, Bauer R F

出版信息

Am J Med. 1987 Jul 27;83(1A):9-14. doi: 10.1016/0002-9343(87)90572-9.

Abstract

High-affinity, E-type prostaglandin binding sites in enriched canine parietal cell preparations were identified with [3H] misoprostol free acid, a prostaglandin E1 analogue. Saturable, reversible, and highly stereospecific binding was identified, with approximately 8,000 binding sites per cell. Prostaglandin I and F bound weakly, and cimetidine and histamine did not bind. The results indicate that [3H] misoprostol free acid binds to E-type prostaglandin receptors, which suggests that the ulcer-healing inhibition of gastric acid secretion by misoprostol results from its interaction with a specific E-type prostaglandin receptor.

摘要

利用前列腺素E1类似物[3H]米索前列醇游离酸,在富集的犬壁细胞制剂中鉴定出高亲和力的E型前列腺素结合位点。确定了可饱和、可逆且高度立体特异性的结合,每个细胞约有8000个结合位点。前列腺素I和F结合较弱,西咪替丁和组胺不结合。结果表明,[3H]米索前列醇游离酸与E型前列腺素受体结合,这表明米索前列醇对胃酸分泌的溃疡愈合抑制作用是其与特定E型前列腺素受体相互作用的结果。

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