EFFECT OF ALPHA-(P-THENOYLPHENYL)-PROPIONIC ACID (TN-762) ON ACUTE INFLAMMATORY REACTIONS AND PROSTAGLANDIN BIOSYNTHESIS

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Abstract
A series of compounds with the general structure of phenylpropionic acid was originally synthesized for antiinflammatory screening. TN-762, showed marked antiinflammatory and analgesic activities and was less toxic. This compound was the same as suprofen which was reported to have potent antiinflammatory and antiwrithing activities. Effects of TN-762 on acute inflammatory reactions and prostaglandin [PG] biosynthesis were investigated in animal models and findings compared to those of ketoprofen and indomethacin. TN-762 showed a dose-dependent inhibition at low doses of 5-20 mg/kg, p.o. [per os] on an increased vascular permeability induced by histamine in rats and by acetic acid in mice and carrageenan-induced paw edema in rats. The antiinflammatory activity of TN-762 was much the same as that of ketoprofen and indomethacin. The inhibitory effect of TN-762 on carrageenan-induced paw edema was not affected by successive administration for 14 days and/or by adrenalectomy. The compound was more active than the 2 reference compounds in inhibiting UV erythema in guinea pigs. TN-762 inhibited markedly the arachidonic acid potentiation of carrageenan-induced edema in rat paw, the sudden death following i.v. administration of arachidonic acid to rabbits and the diarrhea produced by endotoxin in mice, all considered to be induced by biosynthetic PG. The activities of TN-762 were the same or were more potent than those of ketoprofen and indomethacin. The ulcerogenic activity of TN-762 on the gastrointestinal tract in rats was significantly less than that of ketoprofen and indomethacin. TN-762 proved to be a potent inhibitor of acutely-induced inflammation and of PG biosynthesis but the ulcerogenic effects were comparatively diminished.

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