2,5‐Di(tert‐butyl)‐1,4‐benzohydroquinone — a novel inhibitor of liver microsomal Ca2+ sequestration

Treatment of rat liver microsomes with 2,5‐di(tert‐butyl)‐1,4‐benzohydroquinone caused a dose‐related inhibition (K i⋍1 μM) of ATP‐dependent Ca2+ sequestration. This was paralleled by a similar impairment of the microsomal Ca2+ ‐stimulated ATPase activity. In contrast, the hydroquinone failed to ind...

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Veröffentlicht in:FEBS letters 1987-11, Vol.224 (2), p.331-336
Hauptverfasser: Moore, Gregory A., McConkey, David J., Kass, Georges E.N., O'Brien, Peter J., Orrenius, Sten
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container_end_page 336
container_issue 2
container_start_page 331
container_title FEBS letters
container_volume 224
creator Moore, Gregory A.
McConkey, David J.
Kass, Georges E.N.
O'Brien, Peter J.
Orrenius, Sten
description Treatment of rat liver microsomes with 2,5‐di(tert‐butyl)‐1,4‐benzohydroquinone caused a dose‐related inhibition (K i⋍1 μM) of ATP‐dependent Ca2+ sequestration. This was paralleled by a similar impairment of the microsomal Ca2+ ‐stimulated ATPase activity. In contrast, the hydroquinone failed to induce Ca2+ release from Ca2+ ‐loaded liver mitochondria (supplied with ATP), and inhibited neither the mitochondrial F1F0‐ATPase nor the Ca2+ ‐stimulated ATPase activity of the hepatic plasma membrane fraction. The inhibition of microsomal Ca2+ sequestration was not associated with any apparent alteration of membrane permeability or loss of other microsomal enzyme activities or modification of microsomal protein thiols. These findings suggest that 2,5‐di(tert‐butyl)‐1,4‐benzohydroquinone is a potent and selective inhibitor of liver microsomal Ca2+ sequestration which may be a useful tool in studies of Ca2+ fluxes in intact cells and tissues.
doi_str_mv 10.1016/0014-5793(87)80479-9
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Vitamins ; Hydroquinones - pharmacology ; In Vitro Techniques ; Male ; Medical sciences ; Microsome ; Microsomes, Liver - drug effects ; Microsomes, Liver - metabolism ; Mitochondria, Liver - metabolism ; Pharmacology. 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Vitamins</subject><subject>Hydroquinones - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Microsome</subject><subject>Microsomes, Liver - drug effects</subject><subject>Microsomes, Liver - metabolism</subject><subject>Mitochondria, Liver - metabolism</subject><subject>Pharmacology. 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subjects (Ca2+ + Mg2+)-ATPase
2,5-Di(tert-butyl)-1,4-benzohydroquinone
Animals
Biological and medical sciences
Ca2+ sequestration
Calcium - metabolism
Calcium-Transporting ATPases - metabolism
Cell Compartmentation - drug effects
Cell Membrane - enzymology
Cytochrome P-450 Enzyme System - metabolism
General and cellular metabolism. Vitamins
Hydroquinones - pharmacology
In Vitro Techniques
Male
Medical sciences
Microsome
Microsomes, Liver - drug effects
Microsomes, Liver - metabolism
Mitochondria, Liver - metabolism
Pharmacology. Drug treatments
Rat liver
Rats
title 2,5‐Di(tert‐butyl)‐1,4‐benzohydroquinone — a novel inhibitor of liver microsomal Ca2+ sequestration
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