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

Authors
Morizawa, Y Okazoe, T Wang, SZ Sasaki, J Ebisu, H Nishikawa, M Shinyama, H
Citation
Y. Morizawa et al., A novel trifluoromethanesulfonamidophenyl-substituted quinoline derivative, GA 0113: synthesis and pharmacological profiles, J FLUORINE, 109(1), 2001, pp. 83-86
Citations number
10
Categorie Soggetti
Inorganic & Nuclear Chemistry
Journal title
JOURNAL OF FLUORINE CHEMISTRY
ISSN journal
00221139 → ACNP
Volume
109
Issue
1
Year of publication
2001
Pages
83 - 86
Database
ISI
SICI code
0022-1139(200106)109:1<83:ANTQD>2.0.ZU;2-#
Abstract
The trifluoromethanesulfonamidophenyl-substituted quineline GA 0113 have be en synthesized from o-nitrobenzoyl chloride via a multistep process. GA 011 3 displaced specific binding of [I-125]-Sar1, Ile(8)-Ang II to AT(1) recept ors in membrane from Sf9 cells. In concious normotensive dogs, GA 0113 inhi bited the Ang II-induced presser response with ID50 of 0.032 mg/kg and dose -dependently increased plasma renin activity for 48 h. (C) 2001 Elsevier Sc ience B.V. All rights reserved.