N-Cyclohexyl-N'-(2-methoxy-5-chlorophenyl)benzamidine Hydrochloride Monohydrate(HG-70)の抗炎症作用

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概要

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• The anti-inflammatory and other related properties of N-cyclohexyl-N'-(2-methoxy-5-chlorophenyl) benzamidine hydrochloride monohydrate (HG-70), which was selected as the most potent anti-edematous and low toxic new compound among 93 amidines, were investigated to determine profile and mode of action. HG-70 showed marked inhibitory activity on scald paw edema (delayed response) in rats. It also possessed non-specific anti-edematous activity more potent than that of well known anti-inflammatory drugs tested on paw edema induced by carrageenin, serotonin, mustard, trauma, formalin, yeast and bradykinin and skin edema with Punch method. Furthermore, HG-70 showed somewhat weaker inhibitory activity on paper disk-induced granuloma test and granuloma pouch test than phenylbutazone. HG-70 markedly inhibited compound 48/80-induced degranulation of rat mesenterium mast cells. HG-70 inhibited heat-induced hemolysis of rat erythrocytes and collagen-induced platelet aggregation and moderately inhibited histamine-induced capillary permeability. On the other hand, the inhibitory activity of HG-70 as well as sodium salicylate, on carrageenin edema was somewhat suppressed by adrenalectomy and hypophysectomy. HG-70 effected a decrease in the adrenal ascorbic acid and an increase in the plasma corticosterone levels in rats. These results suggest that the anti-inflammatory activity of HG-70 may be primarily due to its inhibitory activity on the release of endogenous inflammatory substances in injury tissues because of its membrane stabilizing action and its inhibitory activity on inflammatory substances and increased vascular permeability and to partly involve stimulation of the pituitary-adrenal system.

• 社団法人日本薬学会の論文
• 1979-03-25

著者

• 浜川 博司

  東洋醸造(株)研究部

• 高柳 法康

  東洋醸造(株)研究部

• 中神 啓二

  東洋醸造(株)研究部

• 小針 定美

  東洋醸造(株)研究部

• 清水 武

  東洋醸造(株)研究部

• 高柳 法康

  東洋醸造(株)医薬品研究所

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• N-Cyclohexyl-N'-(2-methoxy-5-chlorophenyl)benzamidine Hydrochloride Monohydrate(HG-70)の抗炎症作用
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