The effect of lidocaine on hERG K+ channels / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1698-2016.
Article
in Chinese
| WPRIM
| ID: wpr-779360
ABSTRACT
We studied the effects of the lidocaine on the hERG K+ channels with a focus on the electrophysiology of the heart. The hERG current was recorded using the conventional whole-cell patch clamp technique and the channel protein expression level was measured with Western blot in HEK 293 cells stablely expressed hERG K+ channels. The langendorff perfusion system was used to record the ECG from isolated rabbit heart. Lidocaine inhibited hERG current in a concentration-dependent manner at 0.3-1 000 μmol·L-1, the IC50 value was 88.63±7.99 μmol·L-1. The inhibitory action was enhanced by positive votalge without changing the votalge-dependent activation of the channel. However, lidocaine inhibited hERG current in a frequency-dependent manner. In addition, chronic incubation of lidocaine did not change the hERG K+ channel protein expression. ECG recordings in the isolated perfused rabbit heart demonstrated that lidocaine (> 100 μmol·L-1) did not affected QTc interval, but decreased the heart rate and prolonged the PR interval and QRS duration. Our results demonstrate that lidocaine potentially inhibits the hERG K+ current at a high concentration, but does not prolonged the QTc of ECG.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2016
Type:
Article
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