【摘要】 目的 研究异丙酚对多巴胺转运蛋白（DAT）转运功能的影响。方法 ①应用高表达DAT的中华仓鼠卵巢（CHO）细胞,在给予异丙酚后,测定 DAT摄取氢³H标记的多巴胺（³H-DA）功能;②应用非线性动力学方法,观测异丙酚作用时,DAT最大摄取速度（Vmax）和米氏常数（Km）的变化。结果 异丙酚显著降低了高表达多巴胺转运蛋白的中华仓鼠卵巢（CHO/DAT）细胞对多巴胺（DA）的摄取能力;异丙酚药物转运动力学实验表明,异丙酚降低了CHO/DAT对^H-DA的Vmax,对照细胞和异丙酚用药细胞Vmax分别为16.67pmol·min^-1·10^-5cells和11.6pmol·min^-1·10^-5cells,但与DAT的亲和力未发生改变,Km分别为0.46pmol·L^-1和0.53pmol·L^-1。结论 异丙酚以非竞争性的方式抑制了DAT的转运功能,降低了多巴胺（DA）的再摄取,导致突触间隙DA浓度升高,从而增强了中枢多巴胺能神经信息的传递。更多还原

【Abstract】 Objective To determine if propofol can affect uptake of dopamine ( DA) by dopamine transporter (DAT) . Methods Chinese hamster ovary (CHO) cells in which DAT was highly expressed were incubated with H-dopamine in the presence or absence of propofol. Uptake of H-DA was measured. The kinetic parameters Vmax and Km were calculated. Results Propofol significantly inhibited uptake of DA by DAT in CHO cells as compared with the control ( P < 0.05) . Propofol-induced inhibition of dopamine uptake was associated with a decrease in Vmax from 16.67 pmol·min·10-1 cells to 11.16 pmol·min·10-1 cells although the afferent affinity between DAT and DA remained unchanged. Conclusion Propofol inhibits the transport ability of DAT in a noncompetitive fashion and reduces the reuptake of dopamine, leading to elevation in DA concentration in the synaptic cleft and potentiation of dopaminergic neurotransmission in central nervous system.更多还原