アンスラニル酸関連化合物の抗炎症作用(第2報) : アクリジン・モノおよびジカルボン酸, オキソアクリダン・モノカルボン酸誘導体について
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概要
- 論文の詳細を見る
Anti-carrageenin edema activity of compounds related to anthranilic acid was tested in rats by subcutaneous administration. Inhibitory effect of these compounds against heatinduced denaturation of bovine serum albumin and heat-induced hemolysis of dog red blood cells was also tested in vitro. Flufenamic acid and phenylbutazone, among the control drugs used here, demonstrated good correlation between their in vivo and in vitro potencies. Almost all of N-phenylanthranilic acid derivatives showed relatively high activity in both in vitro tests, regardless of their in vivo effectiveness. In both in vitro tests, good agreement was found in the potencies of these derivatives against protein denaturation and hemolysis, except that the compound with either CF_3 plus COOH, COOH, or SO_3H substituent had no effect on hemolysis. Acridine-4-carboxylic acid derivatives generally showing high toxicity in rats had no inhibitory effect on carrageenin edema even at a toxic dose, but significantly high inhibition in vitro was found in these derivatives. Acridine-4,9-dicarboxylic acid derivatives were mostly inactive both in vivo and in vitro. Only the dichloro-substituted compounds slightly inhibited the development of edema in the hind paw of rats following their subcutaneous injection, and showed a marked inhibition in vitro against both protein denaturation and hemolysis. The dichloro-substituted derivative of 9-oxo-acridan-4-carboxylic acid was the most effective in the carrageenin edema test among the compounds related to anthranilic acid tested, except flufenamic acid. This derivative also greatly inhibited both protein denaturation and hemolysis in vitro. The trifluoromethyl substituted derivative was the second in its potency against carrageenin edema. Monochloro or monomethyl substitution resulted in a slight increase of the antiedema activity of 9-oxo-acridan-4-carboxylic acid, but not so much as the dichloro compound in enhancement of the in vitro activities.
- 社団法人日本薬学会の論文
- 1971-02-25
著者
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藤平 榮一
大正製薬株式会社研究部
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小友 進
大正製薬株式会社研究部
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曾田 馨
大正製薬株式会社研究部
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仲沢 政雄
大正製薬株式会社研究部
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小友 進
大正製薬株式会社・健康科学研究所・薬効評価研
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仲沢 政雄
大正製薬研究部薬理研究室
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小友 進
大正製薬株式会社 総合研究所 薬理研究室
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