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

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概要

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• 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.

• 2001-05-01

著者

• Sakaguchi Minoru

  大阪薬科大学

• Sakaguchi Minoru

  Intensive Grazing Research Team National Agricultural Research Center For Hokkaido Region National A

• JIN Denan

  Department of Pharmacology, Osaka Medical College

• MIYAZAKI Mizuo

  Department of Pharmacology, Osaka Medical College

• Takai Shinji

  Department Of Cardiovascular Medicine Kyoto Prefectural University School Of Medicine

• Takai Shinji

  Department Of Pharmacology Osaka Medical College

• SAKAGUCHI Masato

  Department of Pharmacology, Osaka Medical College

• Jin Denan

  Department Of Pharmacology Osaka Medical College

• Sakaguchi M

  Laboratory Of Cell Biology Osaka University Of Pharmaceutical Sciences

• KIRIMURA Kazuyoshi

  Department of Pharmacology, Osaka Medical College

• Miyazaki Mizuo

  Department Of Pharmacology Osaka Medical College Takatsuki City

• KIRIMURA Kazuyoshi

  Shiga Research Center, Nissei BILIS

• Miyazaki Mizuo

  Department Of Pharmacoldgy Osaka Medical College

• Tanda Syuji

  Division Of Hypertension And Nephrology Department Of Internal Medicine Kyoto Prefectural University

• Kirimura Kazuyoshi

  Shiga Research Center Nissei Bilis

• Sakaguchi Masato

  Department Of Materials Science & Technology Nagoya Institute Of Technology

• Takai Shinji

  Department Of Animal Hygiene School Of Veterinary Medicine And Animal Sciences Kitasato University

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