分离的犬壁细胞中E型前列腺素结合位点：用（3H）米索前列醇游离酸进行阐明

E-type prostaglandin binding sites in isolated canine parietal cells: elucidation with (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

Z Gastroenterol. 1987 Apr;25(4):201-6.

Abstract

(3H) Misoprostol free acid, a prostaglandin E1 analog, was used to identify high affinity binding sites for E-type prostaglandins in enriched canine parietal cell preparations. Saturable, reversible, and highly stereospecific binding, with an estimated number of 8000 binding sites per cell, was demonstrated. The binding sites have high affinity for misoprostol, misoprostol free acid, and other E-type prostaglandins. Prostaglandins of the I- and F-type bind weakly, and chemically unrelated compounds, such as histamine and cimetidine, do not bind. The results indicate that (3H) misoprostol free acid binds to E-type prostaglandin receptors, and that the ulcer-healing drug, misoprostol, inhibits gastric acid secretion through interaction with a specific E-type prostaglandin receptor.

摘要

（3H）米索前列醇游离酸，一种前列腺素E1类似物，用于在富集的犬壁细胞制剂中鉴定E型前列腺素的高亲和力结合位点。已证明存在可饱和、可逆且高度立体特异性的结合，估计每个细胞有8000个结合位点。这些结合位点对米索前列醇、米索前列醇游离酸和其他E型前列腺素具有高亲和力。I型和F型前列腺素结合较弱，而化学上不相关的化合物，如组胺和西咪替丁，则不结合。结果表明，（3H）米索前列醇游离酸与E型前列腺素受体结合，并且溃疡愈合药物米索前列醇通过与特定的E型前列腺素受体相互作用来抑制胃酸分泌。