Bimetopyrolの抗炎症作用(第3報) : 抗炎症活性成分とその作用部位

概要

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Some pharmacokinetic studies were made on bimetopyrol [2-methyl-4,5-bis (p-methoxyphenyl) pyrrole], a new anti-inflammatory compound, with special reference to the possible quantitative relationship between serum or tissue concentration of this compound and the anti-inflammatory response in rats. Inhibitory effect of bimetopyrol on carrageenininduced rat paw edema was much more efficient by subcutaneous administration into the inflamed paw than by oral medication. On the other hand, the oral activity of bimetopyrol was not affected by adrenalectomy of the animals used. These findings suggest the possibility that bimetopyrol itself and not the metabolites might act directly upon the target at the site of inflamed tissue, even when it was administered orally. In order to prove this hypothesis, rats were at first pretreated with ^<14>C-labeled bimetopyrol orally followed by carrageenin injection in the paw, then both anti-edema activity and content of bimetopyrol in the inflamed paw were estimated. The results summarized below seem to support the hypothesis. (1) Bimetopyrol content (by fluorometry) in the paw was agreed fairly well with that of radioactivity. (2) Either with any dose or with any pretreatment time, the change in bimetopyrol content in the inflamed paw was always parallel to that in percentage inhibition of paw edema.
社団法人日本薬学会の論文
1972-03-25