Gouardères Christine, Zajac Jean-Marie
Institut de Pharmacologie et de Biologie Structurale, CNRS UMR 5089, 205 Route de Narbonne, 31077 Toulouse Cedex, France.
Neurosci Res. 2007 May;58(1):91-4. doi: 10.1016/j.neures.2007.01.013. Epub 2007 Feb 1.
Neuropeptide FF (NPFF) agonists counteract the cellular opioid actions. We demonstrate for the first time a biochemical anti-opioid effect of NPFF receptors in the rat spinal cord by using the [(35)S]GTPgammaS binding assay in autoradiography. The mu agonist DAMGO as well as the potent and selective NPFF(2) agonist dNPA, stimulated [(35)S]GTPgammaS binding at different optimal GDP concentrations. dNPA decreased the effects induced by DAMGO alone; the maximal of G-protein coupling was decreased but not the potency of opioid agonist. We conclude that NPFF(2) receptors are coupled to G-protein in the rat spinal cord and could exert a molecular anti-opioid effect.
神经肽FF（NPFF）激动剂可对抗细胞的阿片样作用。我们首次通过在放射自显影中使用[（35）S] GTPγS结合试验，证明了大鼠脊髓中NPFF受体的生化抗阿片样作用。μ激动剂DAMGO以及强效选择性NPFF（2）激动剂dNPA，在不同的最佳GDP浓度下刺激了[（35）S] GTPγS结合。dNPA降低了单独由DAMGO诱导的效应；G蛋白偶联的最大值降低，但阿片样激动剂的效力未降低。我们得出结论，NPFF（2）受体在大鼠脊髓中与G蛋白偶联，并可发挥分子抗阿片样作用。
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