A comparative study of the antiinflammatory activity of fentiazac and its major metabolite, p-hydroxy fentiazac.
Wy-25,110, the p-OH metabolite of fentiazac was approximately 100 times less potent than fentiazac after oral administration in rat carrageenan edema and 100-130 times less potent as an inhibitor of prostaglandin synthesis by mouse peritoneal macrophages. In addition, Wy-25,110 was one twelfth as active as fentiazac against immunologic-induced inflammation on day 16 in rat adjuvant arthritis. Wy-25,110 was also much less potent than fentiazac when administered intravenously, suggesting that inadequate oral absorption does not account for its lack of potency. Thus it seems unlikely that the p-OH metabolite contributes greatly to the antiinflammatory properties of fentiazac.
D000085:Acetates / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology* / Q000627:therapeutic use; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000378:metabolism; D001168:Arthritis / Q000188:drug therapy*; D001169:Arthritis, Experimental / Q000188:drug therapy* / Q000378:metabolism; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013844:Thiazoles / Q000494:pharmacology* / Q000627:therapeutic use
D000085:Acetates; D000893:Anti-Inflammatory Agents; D001095:Arachidonic Acids; D013844:Thiazoles; C006124:fentiazac; D016718:Arachidonic Acid; C044249:Wy 25110