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ANTAGONISM OF PROSTANOID‐INDUCED CONTRACTIONS OF RAT GASTRIC FUNDUS MUSCLE BY SC‐19220, SODIUM MECLOFENAMATE, INDOMETHACIN OR TRIMETHOQUINOL
Author(s) -
BENNETT A.,
JAROSIK C.,
SANGER G.J.,
WILSON D.E.
Publication year - 1980
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.1476-5381.1980.tb10922.x
Subject(s) - prostanoid , chemistry , antagonism , thromboxane , prostaglandin , antagonist , medicine , endocrinology , prostaglandin antagonist , thromboxane receptor , acetylcholine , prostacyclin , thromboxane a2 , receptor , pharmacology , biochemistry , platelet
1 The effects of SC‐19220, sodium meclofenamate, indomethacin or trimethoquinol were studied on contractions of the rat stomach longitudinal muscle to prostaglandin D 2 (PGD 2 ), PGE 2 , PGF 2α , PGH 2 , epoxymethano PGH 2 analogues, PGI 2 , 6‐keto‐PGF 1α , 6,15‐diketo‐PGF 1α and thromboxane B 2 . All the drugs reduced contractions to all the prostanoids, but the degree of reduction differed widely. Selectivity of blockade was assessed by comparison with acetylcholine (ACh). 2 With SC‐19220 5 μg/ml the effect on thromboxane B 2 , PGD 2 or PGH 2 and its epoxymethano analogues was not significantly different from the small effect on ACh, but the other prostanoids were blocked to greater extents. 3 The effect of the cyclo‐oxygenase inhibitor sodium meclofenamate, 1 or 2 μg/ml, on 6,15‐diketo‐PGF 1α or thromboxane B 2 was similar to the small antagonism of ACh, whereas the other prostanoids were blocked to greater extents. Indomethacin, 1 μg/ml, also reduced contractions to the prostanoids, but antagonism of the PGH 2 epoxymethano analogues was considerably less than with meclofenamate. 4 The β‐adrenoceptor stimulant trimethoquinol, 50 ng/ml, was the most potent prostanoid antagonist tested; all the prostanoids except PGE 2 were antagonized more than ACh.