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Title:
Quinine Inhibits Mitochondrial ATP-regulated Potassium Channel from Bovine Heart | The Journal of Membrane Biology
Description:
The mitochondrial ATP-regulated potassium (mitoKATP) channel has been suggested as trigger and effector in myocardial ischemic preconditioning. However, molecular and pharmacological properties of the mitoKATP channel remain unclear. In the present study, single-channel activity was measured after reconstitution of the inner mitochondrial membrane from bovine ventricular myocardium into bilayer lipid membrane. After incorporation, a potassium-selective current was recorded with mean conductance of 103 ± 9 pS in symmetrical 150 mM KCl. Single-channel activity of this reconstituted protein showed properties of the mitoKATP channel: it was blocked by 500 μM ATP/Mg, activated by the potassium-channel opener diazoxide at 30 μM, inhibited by 50 μM glibenclamide or 150 μM 5-hydroxydecanoic acid, and was not affected by the plasma membrane ATP-regulated potassium-channel blocker HMR1098 at 100 μM. We observed that the mitoKATP channel was blocked by quinine in the micromolar concentration range. The inhibition by quinine was additionally verified with the use of 86Rb+ flux experiments and submitochondrial particles. Quinine inhibited binding of the sulfonylurea derivative [3H]glibenclamide to the inner mitochondrial membrane. We conclude that quinine inhibits the cardiac mitoKATP channel by acting on the mitochondrial sulfonylurea receptor.
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Keywords {🔍}
google, scholar, pubmed, article, channel, mitochondrial, potassium, mitochondria, channels, szewczyk, membrane, biol, quinine, atpsensitive, rat, heart, chem, res, biophys, katp, garlid, pharmacol, biochem, liver, openers, commun, nalecz, privacy, cookies, content, journal, research, atpregulated, bednarczyk, mitokatp, activity, access, ion, acta, paucek, intracellular, brain, transport, function, information, publish, search, kicińska, pharmacological, properties,
Topics {✒️}
g-protein-gated inwardly rectifying mitochondrial atp-regulated potassium bilayer lipid membrane month download article/chapter atp-sensitive potassium channel potassium-channel opener diazoxide potassium channel openers ion channel-mediated fluxes sulfonylurea derivative [3h]glibenclamide myocardial katp channels ion-specific channels single-channel activity induced potassium channel opener intracellular ion channels chloride channels 5-ht1a receptor-mediated activation membrane biology aims sarcolemmal katp channels mitochondrial katp channel potassium-selective current myocardial ischemic preconditioning induces membrane depolarization potassium ion privacy choices/manage cookies + channels reconstituted mitochondrial potassium rat liver mitochondria mitochondrial sulfonylurea receptor full article pdf single-channel activity mitochondrial membrane quinine inhibits opening mitochondrial katp related subjects polish state committee superoxide-induced activation uncoupled heart mitochondria beef heart mitochondria 500 μm atp/mg cardiac mitokatp channel alkaline ph biochim mg++ flux biochem thiol reagents biochem bovine heart published european economic area scope submit manuscript 150 μm 5-hydroxydecanoic acid micromolar concentration range 86rb+ flux experiments measuring isotope fluxes
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- Marban (1999) Mitochondria: a new target for potassium channel openers?
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headline:Quinine Inhibits Mitochondrial ATP-regulated Potassium Channel from Bovine Heart
description:The mitochondrial ATP-regulated potassium (mitoKATP) channel has been suggested as trigger and effector in myocardial ischemic preconditioning. However, molecular and pharmacological properties of the mitoKATP channel remain unclear. In the present study, single-channel activity was measured after reconstitution of the inner mitochondrial membrane from bovine ventricular myocardium into bilayer lipid membrane. After incorporation, a potassium-selective current was recorded with mean conductance of 103 ± 9 pS in symmetrical 150 mM KCl. Single-channel activity of this reconstituted protein showed properties of the mitoKATP channel: it was blocked by 500 μM ATP/Mg, activated by the potassium-channel opener diazoxide at 30 μM, inhibited by 50 μM glibenclamide or 150 μM 5-hydroxydecanoic acid, and was not affected by the plasma membrane ATP-regulated potassium-channel blocker HMR1098 at 100 μM. We observed that the mitoKATP channel was blocked by quinine in the micromolar concentration range. The inhibition by quinine was additionally verified with the use of 86Rb+ flux experiments and submitochondrial particles. Quinine inhibited binding of the sulfonylurea derivative [3H]glibenclamide to the inner mitochondrial membrane. We conclude that quinine inhibits the cardiac mitoKATP channel by acting on the mitochondrial sulfonylurea receptor.
datePublished:
dateModified:
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Heart mitochondrial
Potassium channel
Quinine
Glibenclamide
Potassium channel openers
Bilayer lipid membrane
Biochemistry
general
Human Physiology
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headline:Quinine Inhibits Mitochondrial ATP-regulated Potassium Channel from Bovine Heart
description:The mitochondrial ATP-regulated potassium (mitoKATP) channel has been suggested as trigger and effector in myocardial ischemic preconditioning. However, molecular and pharmacological properties of the mitoKATP channel remain unclear. In the present study, single-channel activity was measured after reconstitution of the inner mitochondrial membrane from bovine ventricular myocardium into bilayer lipid membrane. After incorporation, a potassium-selective current was recorded with mean conductance of 103 ± 9 pS in symmetrical 150 mM KCl. Single-channel activity of this reconstituted protein showed properties of the mitoKATP channel: it was blocked by 500 μM ATP/Mg, activated by the potassium-channel opener diazoxide at 30 μM, inhibited by 50 μM glibenclamide or 150 μM 5-hydroxydecanoic acid, and was not affected by the plasma membrane ATP-regulated potassium-channel blocker HMR1098 at 100 μM. We observed that the mitoKATP channel was blocked by quinine in the micromolar concentration range. The inhibition by quinine was additionally verified with the use of 86Rb+ flux experiments and submitochondrial particles. Quinine inhibited binding of the sulfonylurea derivative [3H]glibenclamide to the inner mitochondrial membrane. We conclude that quinine inhibits the cardiac mitoKATP channel by acting on the mitochondrial sulfonylurea receptor.
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dateModified:
pageStart:63
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Heart mitochondrial
Potassium channel
Quinine
Glibenclamide
Potassium channel openers
Bilayer lipid membrane
Biochemistry
general
Human Physiology
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