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Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug
OBJECTIVE To attempt to determine the relative value of preclinical cardiac electrophysiology data (in vitro and in vivo) for predicting risk of torsade de pointes (TdP) in clinical use. METHODSExpand
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Isoproterenol antagonizes prolongation of refractory period by the class III antiarrhythmic agent E-4031 in guinea pig myocytes. Mechanism of action.
The mechanism by which isoproterenol (ISO) prevents the prolongation of action potential duration (APD) and refractory period (RP) by the class III antiarrhythmic agent E-4031 was studied. E-4031 (1Expand
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Torcetrapib-induced blood pressure elevation is independent of CETP inhibition and is accompanied by increased circulating levels of aldosterone
Inhibition of cholesteryl ester transfer protein (CETP) with torcetrapib in humans increases plasma high density lipoprotein (HDL) cholesterol levels but is associated with increased blood pressure.Expand
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Influence of ATP-sensitive potassium channel modulators on ischemia-induced fibrillation in isolated rat hearts.
We have confirmed the findings of Kantor and colleagues that ischemia-induced fibrillation in isolated Langendorff-perfused rat hearts can be prevented by glyburide, a blocker of ATP-dependent KExpand
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Comparison of electrocardiographic analysis for risk of QT interval prolongation using safety pharmacology and toxicological studies.
Testing for possible cardiovascular side effects of new drugs has been an essential part of drug development for years. A more detailed analysis of the electrocardiogram (ECG) to detect effects onExpand
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Inhibition of Na+/Ca2+ exchange in membrane vesicle and papillary muscle preparations from guinea pig heart by analogs of amiloride.
Na+/Ca2+ exchange is inhibited in both guinea pig cardiac membrane vesicles and papillary muscles in a concentration-dependent fashion by several analogs of the pyrazine diuretic amiloride.Expand
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Regional vasorelaxant selectivity of atrial natriuretic factor in isolated rabbit vessels.
Synthetic atrial natriuretic factor (ANF) exhibited a marked selectivity in its ability to relax isolated rabbit arteries and veins. The aorta, renal and mesenteric arteries and the facial vein wereExpand
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BRL 34915 (cromakalim) activates ATP-sensitive K+ current in cardiac muscle.
The mechanism by which the antihypertensive agent BRL 34915 (cromakalim) affects action potential duration (APD) and effective refractory period (ERP) in isolated cardiac muscle was investigated. BRLExpand
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In vitro pharmacology of L-158,809, a new highly potent and selective angiotensin II receptor antagonist.
L-158,809 interacted in a competitive manner with rabbit aortic angiotensin II (AII) receptors as determined by Scatchard analysis of the specific binding of [125I]Sar1Ile8-AII. The affinity ofExpand
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