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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Atrial-selective K + channel blockers: potential antiarrhythmic drugs in atrial fibrillation?
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Atrial-selective K + channel blockers: potential antiarrhythmic drugs in atrial fibrillation?

机译:心房选择性K +通道阻滞剂:心房颤动的潜在抗心律失常药物?

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摘要

+ ) channels that are either predominantly expressed in atria or possess electrophysiological properties distinct in atria from ventricles. These channels include the ultra-rapidly activating, delayed outward-rectifying Kv1.5 channel conducting I Kur , the acetylcholine-activated inward-rectifying Kir3.1/Kir3.4 channel conducting I K,ACh , the Ca 2+ -activated K + channels of small conductance (SK) conducting I SK , and the two-pore domain K + (K2P) channels (tandem of P domains, weak inward-rectifying K + channels (TWIK-1), TWIK-related acid-sensitive K + channels (TASK-1 and TASK-3)) that are responsible for voltage-independent background currents I TWIK-1 , I TASK-1 , and I TASK-3 . Direct drug effects on these channels are described and their putative value in treatment of atrial fibrillation is discussed. Although many potential drug targets have emerged in the process of unravelling details of the pathophysiological mechanisms responsible for atrial fibrillation, we do not know whether novel antiarrhythmic drugs will be more successful when modulating many targets or a single specific one. The answer to this riddle can only be solved in a clinical context.
机译:+)主要在心房表达的通道,或在心房和心室具有不同的电生理特性。这些通道包括超快速激活、延迟外向整流Kv1。5通道传导I-Kur,乙酰胆碱激活内向整流Kir3。1/3。4通道传导Ik,ACh,Ca2+激活的小电导K+通道(SK)传导Isk,以及两个孔结构域K+(K2P)通道(串联的P结构域,弱内向整流K+通道(TWIK-1),TWIK相关的酸敏感K+通道(TASK-1和TASK-3)),它们负责电压无关背景电流I TWIK-1,I TASK-1和I TASK-3。本文描述了药物对这些通道的直接作用,并讨论了它们在心房颤动治疗中的潜在价值。尽管在揭示心房颤动的病理生理机制细节的过程中,出现了许多潜在的药物靶点,但我们不知道新型抗心律失常药物在调节多个靶点或单一特定靶点时是否会更成功。这个谜题的答案只能在临床背景下解决。

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