A novel trifluoromethanesulfonamidophenyl-substituted quinoline derivative, GA 0113: synthesis and pharmacological profiles

…, J Sasaki, H Ebisu, M Nishikawa, H Shinyama

文献索引：Morizawa, Yoshitomi; Okazoe, Takashi; Wang, Shu-Zhong; Sasaki, Jun; Ebisu, Hajime; Nishikawa, Masakuni; Shinyama, Hiroshi Journal of Fluorine Chemistry, 2001 , vol. 109, # 1 p. 83 - 86

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被引用次数: 33

摘要

The trifluoromethanesulfonamidophenyl-substituted quinoline GA 0113 have been synthesized from o-nitrobenzoyl chloride via a multi-step process. GA 0113 displaced specific binding of [125I]-Sar1, Ile8-Ang II to AT1 receptors in membrane from Sf9 cells. In concious normotensive dogs, GA 0113 inhibited the Ang II-induced pressor response with ID50 of 0.032 mg/kg and dose-dependently increased plasma renin activity for 48h.