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BRL-32872 : ウィキペディア英語版
BRL-32872

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BRL-32872 is an experimental drug candidate that provides a novel approach to the treatment of cardiac arrhythmia. Being a derivative of verapamil, it possesses the ability to inhibit Ca+2 membrane channels. Specific modifications in hydrogen bonding activity, nitrogen lone pair availability, and molecular flexibility allow BRL-32872 to inhibit K+ channels as well. As such, BRL-32872 is classified as both a class III (K+ blocking) and class IV (Ca+2 blocking) antiarrhythmic agent.〔Nadler, G., Faivre, J. F., Forest, M. C., Cheval, B., Martin, M., Souchet, M., et al. (1998). Synthesis, electrophysiological properties and analysis of structural requirements of a novel class of antiarrhythmic agents with potassium and calcium channel blocking properties. Bioorganic & Medicinal Chemistry, 6(11), 1993-2011〕
==Arrhythmia==

Cardiac arrhythmia arises from abnormalities in action potential formation and propagation through the heart. Changes in electrolyte balance, or development of ectopic pacemaker activity, disrupt normal heart rhythmicity and conduction.〔Guyton, Arthur C., Hall, John E. (2006). Textbook of Medical Physiology (11th ed.). Philadelphia: Elsevier Saunders. ISBN 0-7216-0240-1〕 Antiarrhythmic agents are used to manipulate ion flux through membrane channels to restore normal pacemaker activity. Cellular conduction and refractory periods are also modified to eliminate re-entry depolarization causing arrhythmia. Factors contributing to the generation of arrhythmia include: ischemia, hypoxia, acidosis and drug toxicity. If untreated, arrhythmias may present as bradycardia, tachycardia, or progress to atrial/ventricular fibrillation.〔Katzung, Bertram G.; Masters, Susan B.; Trevor, Anthony J. (2009). ''Basic and Clinical Pharmacology''. 11th ed. New York: McGraw Hill. ISBN 978-0-07-160405-5〕

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