Novel openers of Ca2+-dependent large-conductance potassium channels: symmetrical pharmacophore and electrophysiological evaluation of bisphenols.
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.
Li
Yi
Y
Computer-Assisted Drug Design, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. yi.li@bms.com
Johnson
Graham
G
Romine
Jeffrey L
JL
Meanwell
Nicholas A
NA
Martin
Scott W
SW
Dworetzky
Steven I
SI
Boissard
Christopher G
CG
Gribkoff
Valentin K
VK
Starrett
John E
JE
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
D001562:Benzimidazoles; D002733:Chlorophenols; D051036:Large-Conductance Calcium-Activated Potassium Channels; D010636:Phenols; D024681:Potassium Channels, Calcium-Activated; C083230:NS 004