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Synthesis, Molecular Modeling, and Pharmacological Testing of Bis-Quinolinium Cyclophanes: Potent, Non-Peptidic Blockers of the Apamin-Sensitive Ca 2+ -Activated K + Channel

โœ Scribed by Campos Rosa, Joaquin; Galanakis, Dimitrios; Piergentili, Alessandro; Bhandari, Kalpana; Ganellin, C. Robin; Dunn, Philip M.; Jenkinson, Donald H.


Book ID
127186184
Publisher
American Chemical Society
Year
2000
Tongue
English
Weight
239 KB
Volume
43
Category
Article
ISSN
0022-2623

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Bis-quinolinium cyclophanes: A novel cla
โœ Joaquin Campos Rosa; Bridgitte M Beckwith-Hall; Dimitrios Galanakis; C.Robin Gan ๐Ÿ“‚ Article ๐Ÿ“… 1997 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 239 KB

Based on the structure-activity analysis of two series of blockers of the small conductance Ca 2+activated K + (SKca) channel, a novel class of bis-quinolinium cyclophane blockers has been designed and synthesised. These compounds exhibit submicromolar activity; UCL 1530 ( 4) is a useful agent since