Novel openers of Ca2+-dependent large-conductance potassium channels: symmetrical pharmacophore and electrophysiological evaluation of bisphenols

Yi Li; Graham Johnson; Jeffrey L Romine; Nicholas A Meanwell; Scott W Martin; Steven I Dworetzky; Christopher G Boissard; Valentin K Gribkoff; John E Starrett Jr

doi:10.1016/s0960-894x(03)00156-2

Novel openers of Ca2+-dependent large-conductance potassium channels: symmetrical pharmacophore and electrophysiological evaluation of bisphenols

Bioorg Med Chem Lett. 2003 Apr 17;13(8):1437-9. doi: 10.1016/s0960-894x(03)00156-2.

Authors

Yi Li¹, Graham Johnson, Jeffrey L Romine, Nicholas A Meanwell, Scott W Martin, Steven I Dworetzky, Christopher G Boissard, Valentin K Gribkoff, John E Starrett Jr

Affiliation

¹ Computer-Assisted Drug Design, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. [email protected]

PMID: 12668007
DOI: 10.1016/s0960-894x(03)00156-2

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.

MeSH terms

Animals
Benzimidazoles / chemistry
Chlorophenols / chemistry
Dose-Response Relationship, Drug
Electrophysiology
Large-Conductance Calcium-Activated Potassium Channels
Oocytes / drug effects
Oocytes / physiology
Patch-Clamp Techniques
Phenols / chemistry*
Phenols / pharmacology*
Potassium Channels, Calcium-Activated / agonists*
Potassium Channels, Calcium-Activated / drug effects
Potassium Channels, Calcium-Activated / physiology
Xenopus laevis

Substances

Benzimidazoles
Chlorophenols
Large-Conductance Calcium-Activated Potassium Channels
Phenols
Potassium Channels, Calcium-Activated
NS 004