PMID: 7334375Dec 1, 1981Paper

Competitive inhibition of rat brain hexokinase by 2-deoxyglucose, glucosamine, and metrizamide

Journal of Neurochemistry
J M Bertoni

Abstract

The effects of metrizamide on the kinetics of rat brain hexokinase were compared in vitro with those of 2-deoxyglucose and glucosamine. Although metrizamide, 2-deoxyglucose, and glucosamine are known to be competitive inhibitors of approximately equal potency for glucose of yeast hexokinase (Ki approximately 0.7 mM for all three), metrizamide is a much weaker competitive inhibitor (Ki about 20 mM) of rat brain hexokinase than either 2-deoxyglucose or glucosamine (Ki about 0.3 mM for both). This indicates a greater active site specificity of rat brain hexokinase than of yeast hexokinase. Rat brain hexokinase activity is enhanced approximately threefold in the presence of 0.05, 0.2, and 0.8 mg/ml bovine serum albumin, while yeast hexokinase is only enhanced by 50% under these conditions. Despite the high Ki value for metrizamide, interference with glucose metabolism may occur whenever metrizamide is present in much higher concentrations than glucose. Myelography in humans is one such situation.

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Citations

Nov 20, 2012·Pharmacology & Therapeutics·Mohita UpadhyayPerumal Vivekanandan
Dec 25, 2008·Annals of Neurology·Sang Won SuhRaymond A Swanson
Feb 1, 1984·Journal of Neurochemistry·J M Bertoni, S T Weintraub
Apr 1, 1984·Acta Neurologica Scandinavica·L BechA Gjedde
Apr 30, 2013·Neurological Research·William A LiYuchuan Ding
Sep 1, 1982·Acta Neurologica Scandinavica·A Gjedde
Oct 1, 1985·Acta Neurologica Scandinavica·L BechA Gjedde
Feb 6, 2017·Journal of Neuroscience Research·Evgeniya SamokhinaYuri Zilberter
Oct 21, 2016·The Journal of Biological Chemistry·Pedro CisternasNibaldo C Inestrosa
Feb 5, 2021·PloS One·Yoko SuwabeTomohiro Nakayama
Feb 24, 2021·Journal of Medicinal Chemistry·Alexandra GlenisterTrevor W Hambley
Aug 1, 1984·The American Journal of Physiology·G EvoniukS Schanberg

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