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Personalized in vitro models reveal functional impact of a <i>KCNH2</i> mutation and enable drug screening in LQTS2. [PDF]

open access: yesHeart Rhythm O2
Zheng B   +11 more
europepmc   +1 more source
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Electrophysiologic effects of potassium channel openers

Cardiovascular Drugs and Therapy, 1995
Potassium-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, 1995
The 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
exaly   +3 more sources

The open pore conformation of potassium channels

Nature, 2002
Living 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
openaire   +2 more sources

Mitochondria and Big-Conductance Potassium Channel Openers

Toxicology Mechanisms and Methods, 2004
Mitochondria 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
exaly   +3 more sources

Cardioprotective Actions of Potassium Channel Openers

European Heart Journal, 1994
The 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
openaire   +2 more sources

Stoichiometry of Potassium Channel Opener Action

Molecular Pharmacology, 1999
Potassium 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
openaire   +2 more sources

Potassium Channel Openers: The Case of BK Channel Activators

Letters in Drug Design & Discovery, 2006
Large-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
openaire   +1 more source

Clinical Pharmacology of Potassium Channel Openers

Pharmacology & Toxicology, 1992
Abstract: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.
openaire   +2 more sources

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