Prostaglandin E antagonist activity of 11,15-bisdeoxy prostaglandin E1 and congeners |
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Authors: | E.L. Tolman R. Partridge E.T. Barris |
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Affiliation: | Dept. of Biological Research, Metabolic Disease Therapy Research Section, Lederle Laboratories, A Division of American Cyanamid Company, Pearl River, New York 1 965 USA |
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Abstract: | -11,15-bisdeoxy PGE1 and certain of its congeners were shown to inhibit gerbil colon contractions induced by -PGE1. While some of these compounds were selectively antagonistic of PGE1-induced contractions, others additionally inhibited the gerbil colon agonist activities of -PGE2α 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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