著者

横尾 信夫 佐藤 文泰 桐原 順子 横山 融 池ケ谷 耕司 永倉 正彦 藤井 節郎

出版者

一般社団法人 日本臨床化学会

雑誌

臨床化学 (ISSN:03705633)

巻号頁・発行日

vol.14, no.1, pp.8-12, 1985-02-25 (Released:2012-11-27)

参考文献数

13

被引用文献数

1

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The effect of chymotrypsin inhibitors on the intestinal absorption of insulin was investigated in conscious and unrestrained rabbits. Insulin at a dose of 25U/kg with 10mg/kg of chymotrypsin inhibitors was administered intraduodenally via an indwelled catheter. The blood glucose level was decreased following an administration of insulin in combination with each chymotrypsin inhibitor. The order of the effect on the intestinal absorption was related with the order of chymotrypsin inhibitory activity. Maximal decrease was observed when insulin was administered with such a strong inhibitor as FK 448, [4-(4-isopropylpipe-radinocarbonyl) phenyl 1, 2, 3, 4-tetrahydro-1-naphthoate methanesulfonate], whose IC50 value was 7×10-7M, and the decrease of the glucose level was 25%, compared with the level before administration. The effect of inhibitors which inhibit both chymotrypsin and trypsin was almost the same with that of chymotrypsin specific inhibitors.

著者

横尾 信夫 服部 英三 平田 光輝 渡辺 好一郎 佐藤 文泰 永倉 正彦 藤井 節郎

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.107, no.9, pp.732-737, 1987-09-25 (Released:2008-05-30)

参考文献数

9

被引用文献数

1 1

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Synthesis of water-soluble chymotrypsin specific inhibitors was attempted to study the roles of chymotrypsin-like enzymes in vivo. Previously we reported that the esters of carboxylic acid containing a condensed ring showed stronger activity than those containing a single ring system. Then we synthesized 4-substituted phenyl esters of carboxylic acid containing a condensed ring, such as tetralin, naphthalene, indole etc., and their inhibitory activities were compared. Among these compounds, esters of tetralin-1-carboxylic acid (FK-448) and 1-naphthylacetic acid showed the strongest activity, and their IC50 values were 8×10-7, 5×10-7 M, respectively. Tetralin-2-carboxylate and 2-naphthylacetate inhibited weaker than 1-analogues. Esters of basic quinoline carboxylic acid and bulky carboxylic acids containing a three-ring system inhibited poorly. Chymotrypsin produced equimolecular 4-substituted phenol rapidly and thereafter the amount of 4-substituded phenol increased slowly, when incubated with FK-448 at 37°C.