摘要
Kv1.5钾离子通道仅在人心房肌中表达,因而特异性Kv1.5通道阻滞剂对心房具有高度选择性,不引发室性心律失常,故极有可能成为未来房颤治疗的新型主导药物之一。研究发现,Kv1.5通道阻滞剂对阵发性、持续性和永久性3种不同类型的房颤均有治疗作用,作用机制主要涉及延长心肌细胞动作电位复极时程和有效不应期。本文就Kv1.5通道的结构特点及其阻滞剂的研究进展进行综述,希望能为新型房颤治疗药物的研发提供一定线索和启示。
The Kv1.5 potassium channel is only expressed in human atrial myocytes,so specific Kv1.5 channel blockers have high selectivity to atria and will not trigger ventricular arrhythmias. Therefore,Kv1.5 channel blockers are likely to become a new leading drug for atrial fibrillation(AF)treatment in the future. Literature has revealed that Kv1.5 channel blockers have therapeutic effect on all the three types of AF:paroxysmal,persistent,and permanent. The mechanisms underlying the AF treatment by Kv1.5 channel blockers are probably related to the prolongation of the action potential duration and effective refractory period in atrial myocytes. In the present paper,we briefly described the structural characteristics of Kv1.5 channel and reviewed the research progress in Kv1.5 channel blockers,hoping to provide some clues for the study and development of new AF therapeutics.
出处
《中国药理学与毒理学杂志》
CAS
CSCD
北大核心
2016年第10期1097-1101,共5页
Chinese Journal of Pharmacology and Toxicology
基金
国家自然科学基金(81273501)
国家自然科学基金(81470378)~~
