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