M3-R/IK(M3)--a new target of antiarrhythmic agents.
- Author:
Yan LIU
1
;
Chao-qian XU
;
Jun-dong JIAO
;
Hui-zhen WANG
;
De-li DONG
;
Bao-feng YANG
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Anti-Arrhythmia Agents; Arrhythmias, Cardiac; etiology; physiopathology; Cell Separation; Choline; pharmacology; Guinea Pigs; Heart Ventricles; Male; Myocytes, Cardiac; drug effects; physiology; Piperidines; Rats; Rats, Wistar; Receptor, Muscarinic M3; agonists; antagonists & inhibitors
- From: Acta Pharmaceutica Sinica 2005;40(1):8-12
- CountryChina
- Language:English
-
Abstract:
AIMTo investigate the relationship between M3-R/IK(M3) and arrhythmia in order to find a new target for antiarrhythmic agents.
METHODSUsing the acute ischemic model of rats and patch-clamp techniques, the effects of the M3 receptor on the occurrence of arrhythmias and its possible mechanisms were studied.
RESULTSIn acute ischemic model of rats, the M3 receptor antagonist 4-diphenylacetoxy-N-methylpiperidine-methiodide (4DAMP) increased the occurrence of arrhythmias, and the M3 receptor agonist choline suppressed the onset and the development of arrhythmias (P < 0. 01). No change was observed after treatment with other receptor antagonists (M1, M2, and M4). With patch-clamp techniques, it was found that choline induced K+ current could be inhibited by 4DAMP. Antagonists toward M1, M2, and M4 receptors all failed to alter the current.
CONCLUSIONCholine modulates the cellular electrical properties of the heart, probably by activating a K+ current via stimulation of the M3 receptor. M3-R/IK(M3) may act as a new target for antiarrhythmic agents.
