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MK 499

Known as: MK-499 
 
National Institutes of Health

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L 706000

Papers overview

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Highly Cited
2006
Highly Cited
2006
New insights about HERG blockade obtained from protein modeling, potential energy mapping, and docking studies.
We created a homology model of the homo-tetrameric pore domain of HERG using the crystal structure of the bacterial potassium… Expand
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Highly Cited
2006
Highly Cited
2006
Molecular Determinants of hERG Channel Block
Drug-induced block of cardiac hERG K+ channels causes acquired long QT syndrome. Here, we characterized the molecular mechanism… Expand
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Highly Cited
2004
Highly Cited
2004
Physicochemical Features of the hERG Channel Drug Binding Site*
Blockade of hERG K+ channels in the heart is an unintentional side effect of many drugs and can induce cardiac arrhythmia and… Expand
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Highly Cited
2001
Highly Cited
2001
Open channel block of HERG K(+) channels by vesnarinone.
Vesnarinone, a cardiotonic agent, blocks I(Kr) and, unlike other I(Kr) blockers, produces a frequency-dependent prolongation of… Expand
Highly Cited
2000
Highly Cited
2000
A structural basis for drug-induced long QT syndrome.
Mutations in the HERG K(+) channel gene cause inherited long QT syndrome (LQT), a disorder of cardiac repolarization that… Expand
Highly Cited
2000
Highly Cited
2000
Trapping of a Methanesulfonanilide by Closure of the Herg Potassium Channel Activation Gate
Deactivation of voltage-gated potassium (K+) channels can slow or prevent the recovery from block by charged organic compounds, a… Expand
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Highly Cited
1998
Highly Cited
1998
A novel benzodiazepine that activates cardiac slow delayed rectifier K+ currents.
The slowly activating delayed rectifier K+ current, IKs, is an important modulator of cardiac action potential repolarization… Expand
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Highly Cited
1998
Highly Cited
1998
Molecular determinants of dofetilide block of HERG K+ channels.
The human ether-a-go-go-related gene (HERG) encodes a K+ channel with biophysical properties nearly identical to the rapid… Expand
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Highly Cited
1996
Highly Cited
1996
Class III antiarrhythmic drugs block HERG, a human cardiac delayed rectifier K+ channel. Open-channel block by methanesulfonanilides.
We recently reported that mutations in HERG, a potassium channel gene, cause long QT syndrome. Heterologous expression of HERG in… Expand
Highly Cited
1994
Highly Cited
1994
Cardiac electrophysiologic and antiarrhythmic actions of two long-acting spirobenzopyran piperidine class III agents, L-702,958 and L-706,000 [MK-499].
The cardiac electrophysiologic and antiarrhythmic actions of two Class III ketone- and alcohol-containing spirobenzopyran… Expand
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