title: Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca)).
abstract: 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.
authors.affiliation: Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, UK. epower@sienabiotech.it
authors.forename: Eoin C
authors.initials: EC
authors.lastname: Power
authors.forename: C Robin
authors.initials: CR
authors.lastname: Ganellin
authors.forename: David C H
authors.initials: DC
authors.lastname: Benton
mesh_terms: D000818:Animals; D002417:Cattle; D004353:Drug Evaluation, Preclinical; D007654:Ketoconazole / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051036:Large-Conductance Calcium-Activated Potassium Channels / Q000187:drug effects*; D049990:Membrane Transport Modulators / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D009131:Muscle, Smooth, Vascular / Q000166:cytology / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D051036:Large-Conductance Calcium-Activated Potassium Channels; D049990:Membrane Transport Modulators; D007654:Ketoconazole