Issue Archive

The inhibitory effects of artemisininderivatives on Na~(+)and K~(+)channels incomparison with those of procaine

Huang Fensheng, Hu Qian, Shi Yuliang

Key Laboratory of Neurobiology，Shanghai Institute of Physiology，Chinese Academy of Sciences. Shanghai 200031,Chian

Abstract

Some derivatives of artemisinin have been shown to have local anesthesia action. By using patch-clamp whole cell recording configuration, the effects of five artemisininderivatives on the voltage-gated I_(Na) and I_(K) have been studied on differentiated NG108-15 cells with reference to procaine. The results showed that all the five artemisininderivaives clearly inhibited the voltage-gated sodium current [I_(Na)] of the cells in a dosedependent manner and the effect was partially reversibly. Among the five artemisininderivatives, SM541 has been shown to be most potent, approaching that of procaine.However, 300 #mu#mol/L procaine showed only a slight inhibition of I_(K),whereas all the five derivatives at the same concentration not only decreased I_(K) cleary, but also accelerated its inactivation. Except for SM541,the inhibitory effects on I_(K) decreased rapidly with perfusion of the rest 4 derivatives.

Key words: Artemisinin-derivatives;Procaine;Whole cell recording;I_(Na);I_(K)

Received: 　　Accepted:

Corresponding author: 　　E-mail:

Citing This Article：

Huang Fensheng, Hu Qian, Shi Yuliang . The inhibitory effects of artemisininderivatives on Na~(+)and K~(+)channels incomparison with those of procaine. Acta Physiol Sin 1998; 50 (2): (in Chinese with English abstract).