[Anti-edematous action of 1-(m-chlorophenyl)-3-N, N-dimethylcarbamoyl-5-methoxypyrazole (PZ-177)].
From the screening of a number of new pyrazole derivatives, the title compound, PZ-177, was selected as the most significant derivative for analgestic and anti-edematous actions, in this paper, we report the anti-edematous activity of PZ-177 as assessed by detailed analysis. PZ-177 showed a markedly inhibitory effect against rat paw edema induced by various phlogists (carragenin, dextran, egg albumin, serotonin, formalin and bradykinin). It also inhibited edema induced by anti-rat rabbit serum. The activity of PZ-177 was more potent than that of mepirizole and the same as that of phenylbutazone. Though this agent has a central depressive effect, it is considered that the action has actually little influence on anti-edematous effect, as carrageenin-induced edema was inhibited in spinal rats. On the other hand, the anti-edematous effect of PZ-177 was reduced significantly in adrenalectomized rats. It is therefore suggested that the potent anti-edematous action of PZ-177 is exerted partially by a direct action at the inflamed site and mediated partially by stimulation of the hypophysis-adrenal system.
D000818:Animals; D000893:Anti-Inflammatory Agents; D001920:Bradykinin; D002351:Carrageenan; D004353:Drug Evaluation, Preclinical; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D004840:Epirizole / Q000627:therapeutic use; D005557:Formaldehyde; D010047:Ovalbumin; D011720:Pyrazoles / Q000627:therapeutic use*; D051381:Rats; D012701:Serotonin
D000893:Anti-Inflammatory Agents; D011720:Pyrazoles; D005557:Formaldehyde; D012701:Serotonin; D004840:Epirizole; C011584:PZ 177; D002351:Carrageenan; D010047:Ovalbumin; D001920:Bradykinin