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Wednesday 15 February 2006

Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca)).

By: Power EC, Ganellin CR, Benton DC.

Bioorg Med Chem Lett 2006 Feb 15;16(4):887-90

A series of partial structures of ketoconazole has been synthesized and tested for activity on the large conductance calcium-activated potassium channel (BK) in bovine smooth muscle cells. This has provided openers and blockers of the channel. The results suggest that the phenyl and phenoxy moieties are important for interaction with BK, whereas the imidazole group is unimportant. The properties of the phenoxy moiety seem to determine whether the compounds act to open or block the channel.

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