BIS-QUINOLINIUM CYCLOPHANES - A NOVEL CLASS OF POTENT BLOCKERS OF THEAPAMIN-SENSITIVE CA2-ACTIVATED K+ CHANNEL()

Authors
ROSA JC BECKWITHHALL BM GALANAKIS D GANELLIN CR DUNN PM JENKINSON DH
Citation
Jc. Rosa et al., BIS-QUINOLINIUM CYCLOPHANES - A NOVEL CLASS OF POTENT BLOCKERS OF THEAPAMIN-SENSITIVE CA2-ACTIVATED K+ CHANNEL(), Bioorganic & medicinal chemistry letters, 7(1), 1997, pp. 7-10
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
1
Year of publication
1997
Pages
7 - 10
Database
ISI
SICI code
0960-894X(1997)7:1<7:BC-ANC>2.0.ZU;2-2
Abstract
Based on the structure-activity analysis of two series of blockers of the small conductance Ca2+-activated K+ (SKCa) channel a novel class o f bis-quinolinium cyclophane blockers has been designed and synthesise d. These compounds exhibit submicromolar activity; UCL 1530 (4) is a u seful agent since it has been shown (elsewhere) to be selective for th e neuronal SKCa channel (IC50 = 80 nM) relative to hepatocyte channels . Copyright (C) 1996 Elsevier Science Ltd