Biomedical Engineering Reference
In-Depth Information
Potassium Channel Blockers as Antiarrhythmic
Agents
Qidong You, Qian Yang, and Xiaojian Wang
Contents
1 Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 118
2 Biological Characterization of Potassium Channel Subtypes
That Involved in Arrhythmic Diseases . . . .................................................. 119
3 The Chemical Structures and Structure-Activity Relationships (SARs)
of Potassium Channel Blockers . . .......................................................... 120
3.1 Typical I Kr ( K v 11.1 ) Blockers . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 120
3.2 Multiple Ion Channel Blockers ....................................................... 121
3.3 K v 1.5 Potassium Channel Blockers .................................................. 122
3.4 Other K v 1.5 Blockers in Clinical Trials . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 138
4 Binding Mode Studies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 140
5 Perspective . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 142
References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 142
Abstract This article highlights the development of potassium channel blockers
as antiarrhythmic agents. The chemical structures, the structure-activity rela-
tionships (SARs) of related potassium channel blockers, and their possible
binding modes reported so far in literatures and patents are summarized and
evaluated.
Keywords Cardiac arrhythmic ￿ Potassium channel blockers ￿ SARs
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