نتایج جستجو برای: propafenone
تعداد نتایج: 393 فیلتر نتایج به سال:
The drug efflux pump P-glycoprotein (P-gp) has been shown to promote multidrug resistance (MDR) in tumors as well as to influence ADME properties of drug candidates. Here we synthesized and tested a series of benzophenone derivatives structurally analogous to propafenone-type inhibitors of P-gp. Some of the compounds showed ligand efficiency and lipophilic efficiency (LipE) values in the range ...
Propafenone, a Class IC antiarrhythmic drug, is an orally active sodium channel-blocking agent. It is effective in supraventricular tachyarrhythmias and is particularly useful in converting atrial fibrillation to sinus rhythm. In therapeutic doses, it may cause non-cardiac and cardiac toxicity, including proarrhythmia.
Background. A main side effect of antiarrhythmic drug therapy is the tendency of these drugs to promote arrhythmia within the therapeutic concentration range, i.e., the proarrhythmic activity of these drugs. However, a model for in vitro assessment, quantification, and comparison of proarrhythmic drug activities was still lacking, and only sparse data were available. Methods and Results. To ana...
BACKGROUND The objective of this study was to develop an acute experimental model showing both focal and macroreentrant sustained atrial fibrillation (AF). METHODS AND RESULTS In 31 anesthetized dogs, bilateral thoracotomies allowed the attachment of electrode catheters at the right and left superior pulmonary veins, atrial free walls, and atrial appendages. Acetylcholine, 100 mmol/L, was app...
1Ege University School of Medicine, Department of Paediatrics, Emergency Medicine, Izmir, Turkey 2Ege University School of Medicine, Department of Paediatric Metabolism, Izmir, Turkey 3Ege University School of Medicine, Department of Cardiology, Izmir, Turkey 4Ege University School of Medicine, Department of Emergency Medicine, Izmir, Turkey 5Texas Heart Institute St. Luke’s Episcopal Hospital,...
Human-specific or disproportionately abundant human metabolites of drug candidates that are not adequately formed and qualified in preclinical safety assessment species pose an important drug development challenge. Furthermore, the overall metabolic profile of drug candidates in humans is an important determinant of their drug-drug interaction susceptibility. These risks can be effectively asse...
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