Literature DB >> 897206

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

E L Tolman, R Partridge, E T Barris.   

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.

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Year:  1977        PMID: 897206     DOI: 10.1016/0090-6980(77)90153-8

Source DB:  PubMed          Journal:  Prostaglandins        ISSN: 0090-6980


  1 in total

1.  Pinane thromboxane A2 analogues are non-selective prostanoid antagonists in rat and human stomach muscle.

Authors:  A Bennett; G J Sanger
Journal:  Br J Pharmacol       Date:  1982-12       Impact factor: 8.739

  1 in total

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