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PMID: 2591475 Published · ppublish English Journal Article Research Support, U.S. Gov't, P.H.S.

A Ca2+-activated K+ channel from rabbit aorta: modulation by cromakalim.

European journal of pharmacology ·Vol. 167 ·No. 2 ·1989-08-22 ·Pages 201-10

Gelband CH, Lodge NJ, Van Breemen C

Abstract

A large conductance Ca2+-activated K+ channel from rabbit aorta was incorporated into planar lipid bilayers. This channel had a conductance of 337 +/- 7 pS in symmetrical 250 mM KCl solutions and had a Na+/K+ permeability ratio of less than 0.04. In asymmetrical solutions containing 300 mM KCl cis (intracellular), 100 mM KCl trans (extracellular) or 100 mM KCl cis 500 mM KCl trans, the reversal potentials for the channel were -30 and +46 mV, respectively. This channel possessed voltage-dependent activation and cis (intracellular) Ca2+ sensitivity. Cromakalim (50 nM) added to the trans side of the bilayer significantly increased the Popen by 56% from 0.09 +/- 0.01 to 0.14 +/- 0.01 (P less than 0.01) at -40 mV without altering the single channel conductance. This effect was dose-dependent, increasing at higher cromakalim concentrations. The primary effect of cromakalim was to decrease the tau slow of the channel closed state from 266 +/- 32 to 147 +/- 17 ms which is sufficient to account for the increase in Popen of the channel in the presence of cromakalim.

MeSH Terms
Animals Aorta, Thoracic/drug effects,metabolism Benzopyrans/pharmacology Calcium/pharmacology Cromakalim Drug Interactions In Vitro Techniques Kinetics Lipid Bilayers/analysis Microsomes/drug effects,metabolism Muscle, Smooth, Vascular/drug effects,metabolism Parasympatholytics/pharmacology Potassium Channels/drug effects,metabolism Pyrroles/pharmacology Rabbits
Chemicals
Benzopyrans Lipid Bilayers Parasympatholytics Potassium Channels Pyrroles Cromakalim Calcium
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Gelband C H
Department of Pharmacology, University of Miami School of Medicine, FL 33101.
Lodge N J
Van Breemen C
Article Info
Journal
European journal of pharmacology
Abbr.
Eur J Pharmacol
ISSN
0014-2999
Published
1989-08-22
Pages
201-10
Language
English
Region
Netherlands
NLM ID
1254354
Subset
IM
Grants
NHLBI NIH HHS · HL-07188 · United States
NHLBI NIH HHS · HL-40184 · United States
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