A STUDY OF THE NOVEL ANTI INFLAMMATORY AGENT FLORIFENINE - TOPICAL ANTIINFLAMMATORY ACTIVITY AND INFLUENCE ON ARACHIDONIC-ACID METABOLISM AND NEUTROPHIL FUNCTIONS

We have evaluated the effects of the novel anti-inflammatory agent flo rifenine, 2-(1-Pyrrolidinyl)ethyl N-[7- (trifluoromethyl)-4-quinolyl] anthranilate, on topical inflammation in mice, free radical-mediated r eactions, arachidonic acid metabolism and some neutrophil functions. T opical administration of florifenine produced dose-related anti-inflam matory activity in 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced ear oedema and with a lower potency, in the response induced by arachi donic acid (AA). Florifenine also inhibited neutrophil migration and P GE(2) content in the inflammed ears. In human whole blood, florifenine was a potent and selective inhibitor of TXB(2) generation. This anti- inflammatory agent did not exert antioxidant effects but inhibited ela stase release in human neutrophils without affecting superoxide anion generation. Florifenine administration to mice dose-dependently inhibi ted leukocyte migration and PGE, levels in the air pouch inflammation induced by zymosan. These results demonstrate the topical anti-inflamm atory activity of florifenine and provide a basis for understanding th e mechanisms involved in the inhibitory effects of this agent on infla mmatory responses.