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POTENCY AND SELECTIVITY OF METHYL ANALOGUES OF PROSTAGLANDIN E 2 ON RAT GASTROINTESTINAL FUNCTION
Author(s) -
MAIN I.H.M.,
WHITTLE B.J.R.
Publication year - 1975
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1975.tb07570.x
Subject(s) - potency , prostaglandin , prostaglandin e2 , chemistry , in vivo , prostaglandin e , pentagastrin , endocrinology , medicine , pharmacology , gastric acid , in vitro , secretion , biology , biochemistry , microbiology and biotechnology
1 The potency and selectivity of action of prostaglandin E 2 and its (15S)‐ or (15R)‐15 methyl and 16,16 dimethyl analogues on gastrointestinal function have been studied in the rat. 2 The (15S)‐15 methyl and 16,16 dimethyl analogues were 40 times as active as prostaglandin E 2 in inhibiting pentagastrin‐stimulated acid secretion on intravenous administration to the anaesthetized rat, and 100 times as active on subcutaneous injection to the chronic fistula rat. 3 In antisecretory doses, the analogues, like prostaglandin E 2 , caused bile reflux and, in higher doses, profuse diarrhoea. 4 The (15S)‐15 methyl and 16,16 dimethyl analogues were at least 30 times as active as prostaglandin E 2 in causing changes in intestinal intraluminal pressure in vivo , but were equipotent on isolated smooth muscle. 5 In equivalent antisecretory doses, the methyl analogues had little effect on systemic arterial blood pressure and resting mucosal blood flow compared with prostaglandin E 2 . 6 The (15R) methyl epimer administered parenterally had little effect on gastrointestinal function but brief acid incubation greatly increased its activity.