Inhibition by suprofen and other non-narcotic analgesic drugs of the effects of prostaglandin precursor on isolated tissues and platelets.
Contractions caused by Slow Reacting Substance C(SRS-C) and by Arachidonic Acid hydroperoxide (AAP) in the guinea-pig ileum and by AAP in the rat fundus were studied in the presence of suprofen and of 3 reference compounds. The dose-related inhibitions were not due to antagonism of prostaglandins. Other agonists of gastrointestinal smooth muscle were not or only weakly antagonized. For the study of selective inhibition of AAP-induced contractions by non-narcotic analgesics, the rat fundus is the preferred preparation. In this model suprofen had an ED50 of 1.27 x 10(-7) M (0.033 mug/ml), being 1.5, 94 and 2, 020 times more potent than indomethacin, phenybutazone and acetylsalicylic acid, respectively. Suprofen also strongly inhibited malondialdehyde formation by guinea-pig platelets incubated with arachidonic acid. The reported effects point to inhibition by suprofen of prostaglandin biosynthesis. The antagonism of AAP-induced contractions in the rat fundus is a valuable test system for inhibitors of prostaglandin biosynthesis.
D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D001095:Arachidonic Acids / Q000494:pharmacology; D012898:Autacoids / Q000037:antagonists & inhibitors / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects* / Q000201:enzymology; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D008315:Malondialdehyde / Q000097:blood; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D010545:Peroxides / Q000494:pharmacology; D010666:Phenylpropionates / Q000494:pharmacology*; D011448:Prostaglandin Antagonists; D011451:Prostaglandin-Endoperoxide Synthases / Q000097:blood; D011453:Prostaglandins / Q000494:pharmacology*; D051381:Rats; D013876:Thiophenes / Q000494:pharmacology*
D000700:Analgesics; D001095:Arachidonic Acids; D012898:Autacoids; D010545:Peroxides; D010666:Phenylpropionates; D011448:Prostaglandin Antagonists; D011453:Prostaglandins; D013876:Thiophenes; D008315:Malondialdehyde; D011451:Prostaglandin-Endoperoxide Synthases