Institut de Pharmacologie et de Biologie Structurale, CNRS/Université de Toulouse, UMR 5089, 205 route de Narbonne, 31077 Toulouse Cedex, France.
Pharmacol Rep. 2011;63(4):1061-5. doi: 10.1016/s1734-1140(11)70623-5.
This study investigated the presence of neuropeptide FF (NPFF) receptors on F-11 cells, a hybridoma derived from rat dorsal root ganglia (DRG) and mouse neuroblastoma. Binding experiments revealed a low density (4 fmol/mg) of high affinity (0.5 nM) [(3)H]-EYF binding sites in these cells. The whole-cell planar patch-clamp technique showed that dNPA, a selective NPFF(2) agonist, increased the voltage-dependent potassium outward currents (about 30 pA/pF) by 21%; this reversible effect on sustained delayed potassium currents is blocked by tetraethylammonium. The similar effects of NPFF and opioid agonists on K(+) currents in this cell line may explain their similar antinociceptive actions at the spinal level.
本研究调查了神经肽 FF（NPFF）受体在 F-11 细胞上的存在情况，F-11 细胞是一种源自大鼠背根神经节（DRG）和小鼠神经母细胞瘤的杂交瘤。结合实验表明，这些细胞上存在低密度（4 fmol/mg）、高亲和力（0.5 nM）的[（3）H]-EYF 结合位点。全细胞膜片钳平面技术表明，选择性 NPFF(2)激动剂 dNPA 使电压依赖性钾外向电流（约 30 pA/pF）增加 21%；这种对持续延迟钾电流的可逆作用被四乙铵阻断。NPFF 和阿片类激动剂对该细胞系中 K(+)电流的类似作用可能解释了它们在脊髓水平的类似镇痛作用。
