Identification of high and low (GTP-sensitive) affinity [3H]glibenclamide binding sites in cardiac ventricular membranes

Biochemical and Biophysical Research Communications
J F FrenchJ G Sarmiento

Abstract

Glibenclamide is an antagonist of the ATP-modulated K+ channel in cardiac tissue. This study showed glibenclamide to bind to high (0.2 nM) and low (40 nM) affinity binding sites in canine ventricular membranes. Gpp [NH]p significantly altered the binding characteristics of the low affinity site, while those of the high affinity site were unchanged. This indicates independence of the two sites and suggests the low affinity site may be coupled to a G-binding protein. Although we have identified two [3H]glibenclamide binding sites, the importance of these sites to the cardiac effects of glibenclamide remains to be determined.

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Citations

Jul 1, 1992·Biulleten' eksperimental'noĭ biologii i meditsiny·A P BabenkoV Kh Khavinson
Feb 22, 1991·Brain Research·S ZiniY Ben-Ari
Dec 15, 1992·Biochimica Et Biophysica Acta·S J Ashcroft, F M Ashcroft
Jan 1, 1991·Neuroscience·J M Treherne, M L Ashford
May 25, 1991·European Journal of Pharmacology·J F FrenchJ G Sarmiento
Aug 8, 2002·Journal of Pharmacological and Toxicological Methods·K L WhiteakerM Gopalakrishnan
Mar 1, 1997·British Journal of Pharmacology·R B JonesW R Buckett
Aug 17, 2002·British Journal of Pharmacology·Laurent GrosPhilippe Blache
Feb 1, 1993·Journal of Cardiovascular Electrophysiology·C RipollC G Nichols
Apr 20, 1999·Biochemical and Biophysical Research Communications·L GrosP Blache

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