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Personalized in vitro models reveal functional impact of a <i>KCNH2</i> mutation and enable drug screening in LQTS2. [PDF]
Zheng B +11 more
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Electrophysiologic effects of potassium channel openers
Cardiovascular Drugs and Therapy, 1995Potassium-channel openers or activators have been introduced as a new class of antihypertensive and antianginal agents that act by increasing membrane conductance to potassium, mainly through augmentation of the ATP-sensitive potassium current. Recent in vitro studies have shown that K(+)-channel openers exert concentration-dependent effects on cardiac
Wilhelm Haverkamp +2 more
exaly +3 more sources
Pharmacology of the potassium channel openers
Cardiovascular Drugs and Therapy, 1995The potassium-channel openers comprise a large number of molecules that can be classified into three basic groups: (1) agents like levcromakalim that open a small-conductance (10-30 pS) glibenclamide-sensitive K+ channel currently known as the ATP-sensitive K+ channel, KATP; (2) hybrid molecules, such as nicorandil, that open KATP channels and that ...
Gillian Edwards, Arthur H Weston
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The open pore conformation of potassium channels
Nature, 2002Living cells regulate the activity of their ion channels through a process known as gating. To open the pore, protein conformational changes must occur within a channel's membrane-spanning ion pathway. KcsA and MthK, closed and opened K(+) channels, respectively, reveal how such gating transitions occur.
Jiang, Youxing +5 more
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Mitochondria and Big-Conductance Potassium Channel Openers
Toxicology Mechanisms and Methods, 2004Mitochondria play a central role in energy generation within the cell. Since the discovery of potassium channels in the inner mitochondrial membrane, mitochondria have been considered an important target for potassium channel openers. The purpose of this short review is to present the recent state of our knowledge about big-conductance potassium ...
Anna Kicińska +2 more
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Cardioprotective Actions of Potassium Channel Openers
European Heart Journal, 1994The potential cardioprotective effect of two pure potassium channel openers, bimakalim (EMD 52692) and aprikalim (RP 52891), on myocardial ischaemia/reperfusion injury was investigated in barbital-anaesthetized dogs. In a model of reversible ischaemia/reperfusion injury, administration of bimakalim as an intravenous bolus prior to ischaemia or ...
J A, Auchampach, M, Maruyama, G J, Gross
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Stoichiometry of Potassium Channel Opener Action
Molecular Pharmacology, 1999Potassium channel openers (KCOs; e.g., P1075, pinacidil) exert their effects on excitable cells by opening ATP-sensitive potassium channels. These channels are heteromultimers composed with a 4:4 stoichiometry of an inwardly rectifying K(+) channel subunit plus a regulatory subunit comprising the receptor sites for hypoglycemic sulfonylureas and KCOs ...
I, Gross +4 more
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Potassium Channel Openers: The Case of BK Channel Activators
Letters in Drug Design & Discovery, 2006Large-conductance calcium-activated potassium channels, also known as BK or Maxi-K channels, occur in many types of cells, where they play an essential role in the regulation of cell excitability and function. BK channel openers constitute a heterogeneous group of organic compounds being able to activate BK channels and having a wide therapeutic ...
Nardi A, CALDERONE, VINCENZO, Olesen SP
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Clinical Pharmacology of Potassium Channel Openers
Pharmacology & Toxicology, 1992Abstract:Opening of K+channels in cell membranes with resulting increase in K+conductance, shifts the membrane potential in a hyperpolarizing direction towards the K+equilibrium potential. Hyperpolarization reduces the opening probability of ion channels involved in membrane depolarization and excitation is reduced.
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