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Bis-quinolinium cyclophanes: A novel class of potent blockers of the apamin-sensitive Ca2+-activated K+ channel

✍ Scribed by Joaquin Campos Rosa; Bridgitte M Beckwith-Hall; Dimitrios Galanakis; C.Robin Ganellin; Philip M Dunn; Donald H Jenkinson

Publisher: Elsevier Science
Year: 1997
Tongue: English
Weight: 239 KB
Volume: 7
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(96)00568-9

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✦ Synopsis

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 it has been shown (elsewhere) to be selective for the neuronal SKca channel (IC50 = 80 aM) relative to hepatocyte channels.

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