An orally active chymase inhibitor, BCEAB, suppresses heart chymase activity in the hamster

被引：24

作者：

Takai, S ^{[1
]}

Jin, DN ^{[1
]}

Sakaguchi, M ^{[1
]}

Kirimura, K ^{[1
]}

Miyazaki, M ^{[1
]}

机构：

[1] Osaka Med Coll, Dept Pharmacol, Osaka 5698686, Japan

来源：

JAPANESE JOURNAL OF PHARMACOLOGY | 2001年 / 86卷 / 01期

关键词：

chymase; inhibitor; oral administration;

D O I：

10.1254/jjp.86.124

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

We investigated the effects of a novel chymase inhibitor, BCEAB (4-[1-{[bis-(4-methyl-phenyl)methyl]-carbamoyl)-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy]-benzoic acid). The IC50 value of BCEAB for purified human chymase was 5.4 nM, whereas BCEAB did not inhibit the angiotensin-converting enzyme, elastase and tryptase. In isolated dog arteries, the IC50 value of BCEAB for the angiotensin 1-induced contraction in the presence of 1 muM lisinopril was 2.8 muM. In the hamster, the heart chymase activities were significantly suppressed to 42.0% and 26.9% 3 h after oral administration of 100 and 300 mg of BCEAB/kg of body weight, respectively. In conclusion, BCEAB is a useful chymase inhibitor for studying the role of chymase in vivo.

引用

收藏

页码：124 / 126

页数：3

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