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首页> 外文期刊>Life sciences >Region-dependent g-protein activation by #mu#-, #delta#_1-and #delta#_2-opioid receptor agonists in the brain: comparison between the midbrain and forebrain
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Region-dependent g-protein activation by #mu#-, #delta#_1-and #delta#_2-opioid receptor agonists in the brain: comparison between the midbrain and forebrain

机译：脑中#mu＃-，＃delta＃_1-和＃delta＃_2-阿片样物质受体激动剂对区域依赖性g蛋白的活化作用：中脑和前脑之间的比较

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The ability of selective #mu#- ([D-Ala~2, NHPhe~4, Gly-ol]enkephalin: DAMGO), #delta#_1- ([D-Pen~2, Pen~5]enkephalin: DPDPE) and #delta#_2- ([D-Ala~2]deltorphin II: DELT II) opioid receptor agonists to activate G-proteins in the midbrain and forebrain of mice and rats was examined by monitoring the binding of guanosine-5'-O-(3-[~(35)S]thio)triphosphate ([~(35)S]GTP#gamma#S). The levels of [~(35)S]GTP#gamma#S binding stimulated by DAMGO in the mouse and rat midbrain were significantly greater than those by DPDPE or DELT II. However, relatively lower levels of stimulation of [~(35)S]GTP#gamma#S binding by all of the agonists than would have been predicted from the receptor densities were observed in either the limbic forebrain or striatum of mice and rats. The effects of DAMGO, DPDPE and DELT II in all three regions were completely reversed by selective #mu#-, #delta#_1- and #delta#_2-antagonists, respectively. The results indicate that the levels of #mu#-, #delta#_1- and #delta#_2-opioid receptor agonist-induced G-protein activation in the midbrain are in good agreement with the previously determined distribution densities of each receptor type. Furthermore, the discrepancies observed in the forebrain might reflect differential catalytic efficiencies of receptor-G-protein coupling.
机译：选择性＃mu＃-（[D-Ala〜2，NHPhe〜4，甘醇]脑啡肽：DAMGO），＃delta＃_1-（[D-Pen〜2，Pen〜5]脑啡肽：DPDPE）的能力和＃delta＃_2-（[D-Ala〜2] deltorphin II：DELT II）阿片受体激动剂激活小鼠和大鼠中脑和前脑中的G蛋白，方法是监测鸟苷5'-O的结合-（3- [〜（35）S]硫代）三磷酸酯（[〜（35）S] GTP＃gamma＃S）。 DAMGO在小鼠和大鼠中脑中刺激的[〜（35）S] GTP＃γ＃S结合水平明显高于DPDPE或DELT II。然而，在小鼠和大鼠的边缘前脑或纹状体中观察到，所有激动剂对[〜（35）S] GTP＃gamma＃S结合的刺激水平均低于从受体密度所预期的水平。 DAMGO，DPDPE和DELT II在所有三个区域的作用分别被选择性的#mu＃-，＃delta＃_1-和＃delta＃_2-拮抗剂完全逆转。结果表明，＃mu＃-，＃delta＃_1-和＃delta＃_2-阿片样物质受体激动剂诱导的中脑G蛋白活化水平与每种受体类型先前确定的分布密度高度吻合。此外，在前脑中观察到的差异可能反映了受体-G-蛋白偶联的不同催化效率。

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