著者

木山 竜一 林 邦雄 原 真里子 藤本 正文 川畑 友二 川上 勝 中島 成元 藤下 利夫

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.43, no.6, pp.960-965, 1995-06-15 (Released:2008-03-31)

参考文献数

12

被引用文献数

3 8

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A novel series of 6-alkyl-7-oxo-4, 7-dihydropyrazolo[1, 5-a]pyrimidine-3-carboxylic acid derivatives was prepared as angiotensin II (AII) receptor antagonists. When evaluated in an in vitro binding assay using COS cells transfected with a cDNA encoding a human AT1 angiotensin II receptor, the compounds in this series showed Ki values in the range of 0.4-4.0 nM. In anesthetized spontaneously hypertensive rats (SHRs), administration of the 6-propyl derivative 4d (1 mg/kg, i.v.) reduced the mean blood pressure (MBP) by a maximum of more than 30 mmHg from the normal value.