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研究布格呋喃(AF-5)抗焦虑及抑郁作用的电生理学机制。采用全细胞膜片钳技术,观察AF-5对原代培养大鼠皮层神经元上电压依赖性钠离子通道、电压依赖性钾离子通道、电压依赖性L-型钙离子通道、γ-氨基丁酸(GABA)依赖的氯离子通道以及稳定转染于HEK293细胞系上Kv2.1通道电流的影响。结果表明,AF-5能明显抑制原代培养大鼠皮层神经元上电压依赖性延迟整流钾电流(IK(DR))、L-型钙通道电流(IL-Ca)以及稳定转染于HEK293细胞系上Kv2.1通道电流,其IC50分别为6.17、4.4和5.29μmol.L 1,但对电压依赖性钠通道电流(INa)、瞬时外向钾电流(IK(A))以及GABA介导的氯离子通道电流的抑制作用较弱。研究表明,AF-5的抗焦虑及抑郁作用可能与其抑制以Kv2.1为主的神经元IK(DR)及IL-Ca有关。
To study the electrophysiological mechanism of the anti-anxiety and depression effects of buforfuran (AF-5). Whole-cell patch-clamp technique was used to observe the effects of AF-5 on voltage-dependent sodium channel, voltage-dependent potassium channel, voltage-dependent L-type calcium channel, γ-aminobutyric acid (GABA) -dependent chloride channel and Kv2.1 channel currents stably transfected into HEK293 cell line. The results showed that AF-5 significantly inhibited voltage-dependent delayed rectifier potassium current (IK (DR)), L-type calcium channel current (IL-Ca) and stably transfected HEK293 cells in primary cultured rat cortical neurons With Kv2.1 channel currents with IC50 of 6.17, 4.4 and 5.29 μmol.L 1, respectively, but not with voltage dependent sodium channel current (INa), transient outward potassium current (IK (A)), and GABA- Ion channel current inhibition is weak. Studies have shown that the anti-anxiety and depression of AF-5 may be related to the inhibition of IK (DR) and IL-Ca of Kv2.1-based neurons.