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

Abstract：

AIM:To study the effects of 3-n-butylphthalide (NBP) on the TREK-1 channel expressed in Chinese hamster ovary (CHO) cells. METHODS: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. RESULTS: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. CONCLUSION:1-NBP potently inhibited TREK-1 current and elevated the membrane potential, which may contribute to its neuroprotective activity.

journal_name

Acta Pharmacol Sin

journal_title

Acta pharmacologica Sinica

authors

Ji XC,Zhao WH,Cao DX,Shi QQ,Wang XL

doi

10.1038/aps.2010.210

subject

Has Abstract

pub_date

2011-02-01 00:00:00

pages

182-7

issue

2

eissn

1671-4083

issn

1745-7254

pii

aps2010210

journal_volume

32

pub_type

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