An Orally Active Chymase Inhibitor, BCEAB, Suppresses Heart Chymase Activity in the Hamster

The Japanese Journal of Pharmacology

Shinji Takai¹  Kazuyoshi Kirimura¹  Masato Sakaguchi¹  Mizuo Miyazaki¹  Denan Jin¹ 

[1] Department of Pharmacology, Osaka Medical College

关键词: Chymase;    Inhibitor;    Oral administration;   

DOI  :  10.1254/jjp.86.124

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(11)Cited-By(11)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 I-induced contraction in the presence of 1 μM lisinopril was 2.8 μM. 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.

【 授权许可】

Unknown