Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.
Acta Pharmacol Sin. 2011 Feb;32(2):182-7. doi: 10.1038/aps.2010.210.
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.
研究 3-正丁基苯酞（NBP）对中国仓鼠卵巢（CHO）细胞表达的 TREK-1 通道的影响。
采用全细胞膜片钳记录技术记录 TREK-1 通道电流。观察不同剂量的 1-NBP 对 TREK-1 电流的影响。采用电流钳记录测量 TREK-1 转染 CHO（TREK-1/CHO）和野生型 CHO（Wt/CHO）细胞的静息膜电位。
l-NBP（0.01-10 μmol/L）对 TREK-1 电流呈浓度依赖性抑制（IC50=0.06±0.03 μmol/L），在 10 μmol/L 浓度下最大电流抑制率为 70%。l-NBP 对 TREK-1 电流的抑制作用强于 d-NBP 或 dl-NBP。这种作用在洗脱后部分逆转，且不依赖于电压。10 μmol/L 的 l-NBP 将 TREK-1/CHO 细胞的膜电位从-55.3 mV 升高至-42.9 mV。然而，它对 Wt/CHO 细胞的膜电位没有影响。
1-NBP 强烈抑制 TREK-1 电流并升高膜电位，这可能有助于其神经保护活性。
