11,15-双脱氧前列腺素E1及其同系物的前列腺素E拮抗剂活性

Prostaglandin E antagonist activity of 11, 15-bisdeoxy prostaglandin E1 and congeners.

作者信息

Tolman E L, Partridge R, Barris E T

出版信息

Prostaglandins. 1977 Jul;14(1):11-9. doi: 10.1016/0090-6980(77)90153-8.

Abstract

d,l-11, 15-bisdeoxy PGE1 and certain of its congeners were shown to inhibit gerbil colon contractions induced by l-PGE1. While some of these compounds were selectively antagonistic of PGE1-induced contractions, others additionally inhibited the gerbil colon agonist activities of l-PGE2alpha and acetylcholine. The PGE1 inhibitory activity was apparently competitive in nature. With relatively weak potencies, the bisdeoxy PGE congeners displaced 3H-PGE1 from a fat cell binding site, suggesting competition for a common, putative receptor. Structure-activity relationships and potential utility of these analogs are discussed.

摘要

已表明d，l-11，15-双脱氧前列地尔（PGE1）及其某些同系物可抑制l-PGE1诱导的沙鼠结肠收缩。虽然其中一些化合物对PGE1诱导的收缩具有选择性拮抗作用，但其他化合物还可抑制l-PGE2α和乙酰胆碱对沙鼠结肠的激动剂活性。PGE1抑制活性在本质上显然是竞争性的。双脱氧PGE同系物以相对较弱的效力从脂肪细胞结合位点取代3H-PGE1，表明对共同的假定受体存在竞争。讨论了这些类似物的构效关系和潜在用途。