title: Novel openers of Ca2+-dependent large-conductance potassium channels: symmetrical pharmacophore and electrophysiological evaluation of bisphenols.
abstract: Electrophysiological evaluation of symmetrical analogues of the known maxi-K opener NS-004 (1) led to the discovery of bisphenols 2a, 3a and 4a as openers of cloned maxi-K channels expressed in oocytes.
authors.affiliation: Computer-Assisted Drug Design, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. yi.li@bms.com
authors.forename: Yi
authors.initials: Y
authors.lastname: Li
authors.forename: Graham
authors.initials: G
authors.lastname: Johnson
authors.forename: Jeffrey L
authors.initials: JL
authors.lastname: Romine
authors.forename: Nicholas A
authors.initials: NA
authors.lastname: Meanwell
authors.forename: Scott W
authors.initials: SW
authors.lastname: Martin
authors.forename: Steven I
authors.initials: SI
authors.lastname: Dworetzky
authors.forename: Christopher G
authors.initials: CG
authors.lastname: Boissard
authors.forename: Valentin K
authors.initials: VK
authors.lastname: Gribkoff
authors.forename: John E
authors.initials: JE
authors.lastname: Starrett
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000737:chemistry; D002733:Chlorophenols / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D004594:Electrophysiology; D051036:Large-Conductance Calcium-Activated Potassium Channels; D009865:Oocytes / Q000187:drug effects / Q000502:physiology; D018408:Patch-Clamp Techniques; D010636:Phenols / Q000737:chemistry* / Q000494:pharmacology*; D024681:Potassium Channels, Calcium-Activated / Q000819:agonists* / Q000187:drug effects / Q000502:physiology; D014982:Xenopus laevis
chemical_list: D001562:Benzimidazoles; D002733:Chlorophenols; D051036:Large-Conductance Calcium-Activated Potassium Channels; D010636:Phenols; D024681:Potassium Channels, Calcium-Activated; C083230:NS 004