Studies on Antihypertensive Agents with Antithrombotic Activity.2.Syntheses and Pharmacological Evaluation of Pyrrolo[2,3-c]azepine Derivatives

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概要

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• As an extension of our previous investigation, a series of 7-aminoalkylpyrrolo[2,3-c]azepine derivatives was synthesized and evaluated as α_1-adrenergic- and serotonin 2(5-HT_2)-receptor antagonists, with the aim of finding a novel potent antihypertensive agent with both activities. Among the compounds obtained in this study, (E)-1-ethyl-7-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-4-hydroxyimino-1,4,5,6,7,8-hexahydropyrrolo[2,3-c]azepin-8-one (16d) displayed potent α_1-adrenoceptor blocking activity (pA_2=7.83±0.20) and 5-HT_2-receptor blocking activity (pA_2=9.47±0.17) in isolated guinea pig arteries. At 3 mg/kg oral administration, compound 16d exhibited antihypertensive activity more potent than that of doxazosin in deoxycorticosterone acetate (DOCA)-salt hypertensive dogs. Furthermore, this compound reduced the rate of mouse acute pulmonary thromboembolitic death induced by collagen and serotonin at oral doses of 0.3 mg/kg or more, and its effect lasted for at least 6 h at 3 mg/kg.

• 公益社団法人日本薬学会の論文
• 2000-08-01

著者

• Inomata Norio

  Suntory Institute for Biomedical Research

• Yamaki Akira

  Suntory Institute for Biomedical Research

• Mizuno A

  Suntory Institute For Biomedical Research

• Inomata N

  Suntory Institute For Biomedical Research

• Inomata Norio

  Laboratory Of Experimental:molecular Pharmacology Suntory Institute For Biomedical Research

• Shibata M

  Fumakilla Ltd.

• Mizuno Akira

  Suntory Institute For Biomedical Research

• KAMEI Tomoe

  Suntory Institute for Biomedical Research

• SHIBATA Makoto

  Suntory Institute for Biomedical Research

• NAKANISHI Kyoko

  Suntory Institute for Biomedical Research

• TAKIGUCHI Chikako

  Suntory Institute for Biomedical Research

• Mizuno A

  Meiji Pharmaceutical Univ. Tokyo Jpn

• Kamei T

  Suntory Institute For Biomedical Research

• TATSUOKA TOSHIO

  Suntory Institute for Biomedical Research

• Tatsuoka T

  Suntory Institute For Biomedical Research

• Hidaka Toshinori

  Suntory Institute For Biomedical Research

• MIYA Mikiko

  Suntory Institute for Biomedical Research

• Nakanishi K

  Suntory Institute For Biomedical Research

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