Referenced in: none

Automatically associated channels: Kir2.3

Title: Novel neuroprotectant chiral 3-n-butylphthalide inhibits tandem-pore-domain potassium channel TREK-1.

Authors: Xin-cai Ji, Wan-hong Zhao, Dong-Xu Cao, Qiao-qiao Shi, Xiao-Liang Wang

Journal, date & volume: Acta Pharmacol. Sin., 2011 Feb , 32, 182-7

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/21293470

Abstract
To study the effects of 3-n-butylphthalide (NBP) on the TREK-1 channel expressed in Chinese hamster ovary (CHO) cells.Whole-cell patch-clamp recording was used to record TREK-1 channel currents. The effects of varying doses of l-NBP on TREK-1 currents were also observed. Current-clamp recordings were performed to measure the resting membrane potential in TREK-1-transfected CHO (TREK-1/CHO) and wild-type CHO (Wt/CHO) cells.l-NBP (0.01-10 μmol/L) showed concentration-dependent inhibition on TREK-1 currents (IC(50)=0.06±0.03 μmol/L), with a maximum current reduction of 70% at a concentration of 10 μmol/L. l-NBP showed a more potent inhibition on TREK-1 current than d-NBP or dl-NBP. This effect was partially reversed upon washout and was not voltage-dependent. l-NBP 10 μmol/L elevated the membrane potential in TREK-1/CHO cells from -55.3 mV to -42.9 mV. However, it had no effect on the membrane potential of Wt/CHO cells.1-NBP potently inhibited TREK-1 current and elevated the membrane potential, which may contribute to its neuroprotective activity.