Abstract
Summary
Diftalone and its metabolites 7,14-Dihydroxyphthalazino [2,3-b]phthal-azine-5,12 (7H, 14H)-dione, 7-Hydroxy-phthalazino [2,3-b]phthalazine-5,12 (7H, 14H)-dione and 12 [l(2H)-oxo-2-phthal-azinyl]methylbenzoic acid inhibited pros-taglandin synthesis in bovine seminal vesicle microsome preparations. Diftalone was the most active of these compounds but less active than indomethacin although more active than phenylbutazone or aspirin. The magnitude of the concentration of arachi-donic acid influenced the velocity of the reaction in the synthesis of prostaglandins; the highest concentrations inhibited the rate of reaction.
The results of the in vitro inhibition of prostaglandin synthetase studies correlated well with those obtained in the in vivo car-rageenan edema inhibition studies in the rat. The relative potencies for Diftalone, indomethacin and phenylbutazone were similar with both experimental procedures.
The authors thank Dr. Franco Luzzani, Mr. Alfonso Condo', and Mr. Alfredo Soffientini for assistance in the assay procedures; Dr. Pierfranco Schiatti for the information on the carrageenan edema inhibition studies; and Miss Anna Maria Cuzzoni for typing the manuscript.
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