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PINANE THROMBOXANE A 2 ANALOGUES ARE NON‐SELECTIVE PROSTANOID ANTAGONISTS IN RAT AND HUMAN STOMACH MUSCLE
Author(s) -
BENNETT ALAN,
SANGER GARETH J.
Publication year - 1982
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.1476-5381.1982.tb09336.x
Subject(s) - acetylcholine , thromboxane a2 , prostanoid , stomach , contraction (grammar) , endocrinology , medicine , chemistry , gastric fundus , prostaglandin , muscle contraction , thromboxane , thromboxane receptor , smooth muscle , receptor , platelet
1 Pinane thromboxane A 2 (PTxA 2 ) and its epi‐OH isomer were studied on rat and human stomach longitudinal muscle. 2 PTxA 2 (0.5 μg/ml) usually caused a slight contraction of rat gastric fundus. Contractions to PGE 2 , PGF 2α , PGI 2 and expoxymethano analogues of PGH 2 (U‐46619 and U‐44069) were substantially inhibited, whereas those to PGD 2 and acetylcholine were only slightly reduced. 3 In human stomach, PTxA 2 0.5 μg/ml rarely stimulated the muscle. Contractions to PGE 2 , PGF 2α and U‐46619 were antagonized, with little effect on those to acetylcholine. 4 epi‐PTxA 2 (0.5 μg/ml) did not affect rat gastric tone. It was moderately potent against PGI 2 on rat gastric fundus, but was less effective than PTxA 2 against U‐44069.