The anti-inflammatory and analgesic profile of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid (tiopinac)

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W H RooksM B Wallach

Abstract

Tiopinac displayed marked anti-inflammatory activity when given p.o. in rat models of acute and chronic inflammation. It inhibited carrageenan-induced paw edema (40 x phenylbutazone), and cotton-pellet-induced granuloma (0.8 x indomethacin). In an 18-day test, tiopinac prevented the development of adjuvant-induced arthritis (10-15 x naproxen) and had similar activity versus pre-induced arthritis. Tiopinac exhibited antiphlogistic activity in adrenalectomized rats. It did not have corticosteroid activity. Depending upon the type of analgesic test used, the potency of tiopinac varied. When given p.o. it inhibited phenylquinone-induced writhing in the mouse and rat (respectively 16 and 10 x aspirin). In contrast, tiopinac had approximately 10 times the potency of indomethacin in increasing the pain threshold when yeast-inflamed paws were compressed. The pain threshold of the noninflamed paw was not increased. Tiopinac was highly active versus pain induced by flexing the adjuvant arthritic-inflamed paw (greater than or equal to 1000 x aspirin). It was inactive in the mouse hot-plate test in which opiate-like agents are active. Tiopinac, p.o., lowered yeast-induced pyrexia (130 x aspirin). Tiopinac did not have significant cardiovas...Continue Reading

References

Jun 1, 1975·Chemical & Pharmaceutical Bulletin·S Kuzuna, K Kawai
Jan 1, 1956·Proceedings of the Society for Experimental Biology and Medicine·C M PEARSON
Dec 1, 1962·Proceedings of the Society for Experimental Biology and Medicine·C A WINTERG W NUSS

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Citations

May 1, 1984·Journal of Pharmaceutical Sciences·E Cullen
Apr 22, 2021·Journal of Clinical Biochemistry and Nutrition·Yuko ShimamuraShuichi Masuda

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