Crebanine inhibits voltage-dependent Na+ current in guinea-pig ventricular myocytes.
10.1016/S1875-5364(14)60004-2
- Author:
He XIAO-SHAN
1
;
Lin QING
1
;
Ma YUN-SHU
1
;
Yu ZE-PU
1
Author Information
1. Yunnan University of Traditional Chinese Medicine, Kunming 650500, China.
- Publication Type:Journal Article
- Keywords:
Arrhythmia;
Crebanine;
Myocardium;
Patch-clamp techniques;
R285;
Sodium channels
- MeSH:
Animals;
Aporphines;
pharmacology;
Cells, Cultured;
Down-Regulation;
drug effects;
Drugs, Chinese Herbal;
pharmacology;
Female;
Guinea Pigs;
Heart Ventricles;
cytology;
drug effects;
metabolism;
Male;
Myocytes, Cardiac;
drug effects;
metabolism;
Stephania;
chemistry;
Voltage-Gated Sodium Channel Blockers;
pharmacology;
Voltage-Gated Sodium Channels;
metabolism
- From:
Chinese Journal of Natural Medicines (English Ed.)
2014;12(1):20-23
- CountryChina
- Language:English
-
Abstract:
AIM:To study the effects of crebanine on voltage-gated Na(+) channels in cardiac tissues.
METHODS:Single ventricular myocytes were enzymatically dissociated from adult guinea-pig heart. Voltage-dependent Na(+) current was recorded using the whole cell voltage-clamp technique.
RESULTS:Crebanine reversibly inhibited Na(+) current with an IC50 value of 0.283 mmol·L(-1) (95% confidence range: 0.248-0.318 mmol·L(-1)). Crebanine at 0.262 mmol·L(-1) caused a negative shift (about 12 mV) in the voltage-dependence of steady-state inactivation of Na(+) current, and retarded its recovery from inactivation, but did not affect its activation curve.
CONCLUSION:In addition to blocking other voltage-gated ion channels, crebanine blocked Na(+) channels in guinea-pig ventricular myocytes. Crebanine acted as an inactivation stabilizer of Na(+) channels in cardiac tissues.
