On the mechanism of the pharmacological activity of the new nonsteroidal antiinflammatory agent 4'-acetamidophenyl-2-(5'-p-toluyl-1'-methylpyrrole)acetate.
4-Acetamidophenyl-2-(5'-p-toluyl-1'-methylpyrrole)acetate (AU 8001), a tolmetin derivative, prepared by esterification with paracetamol, showed antiinflammatory-antirheumatic activity in animal models. This activity is believed to be largely due to the ability of the drug to inhibit the synthesis of prostaglandins. Furthermore, there is evidence that AU 8001 may also reduce the leucocyte immigration into inflamed tissues. Moreover, AU 8001 had no effects, after oral administration, on histamine- and 5-hydroxytryptamine-induced increase of vascular permeability or lysosome membrane stabilization.
Department of Pharmacology, Universidad de Navarra, Pamplona, Spain.
M
M
Ucelay
B
B
Lasheras
E
E
Cenarruzabeitia
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D002199:Capillary Permeability / Q000187:drug effects; D002351:Carrageenan / Q000494:pharmacology; D002464:Cell Migration Inhibition; D015232:Dinoprostone / Q000096:biosynthesis; D066298:In Vitro Techniques; D007962:Leukocytes / Q000187:drug effects / Q000378:metabolism; D008247:Lysosomes / Q000187:drug effects / Q000378:metabolism; D008297:Male; D011448:Prostaglandin Antagonists; D011758:Pyrroles / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D014046:Tolmetin / Q000031:analogs & derivatives / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011448:Prostaglandin Antagonists; D011758:Pyrroles; C035894:AU 8001; D002351:Carrageenan; D014046:Tolmetin; D015232:Dinoprostone