Costa T, Aktories K, Schultz G, Wüster M
Life Sci. 1983;33 Suppl 1:219-22. doi: 10.1016/0024-3205(83)90482-4.
Neuroblastoma X glioma hybrid cells NG108-15 were treated with a toxin derived from Bordetella pertussis. As compared to control cells grown in the absence of toxin, the inhibitory effects of opioid agonists upon cAMP formation were dose-dependently impaired by a non-competitive mechanism. Radioligand binding studies revealed that opioid agonist binding was dramatically reduced in toxin-treated membranes when tested in the presence of Na+/Mg++/GMP-PNP. Further, the potencies of guanine nucleotides to decrease opioid agonist binding were differentially modulated. These studies may facilitate our understanding of the mechanisms responsible for acute and chronic opiate effects.
神经母细胞瘤X胶质瘤杂交细胞NG108-15用百日咳博德特氏菌衍生的毒素进行处理。与在无毒素条件下生长的对照细胞相比,阿片样物质激动剂对环磷酸腺苷(cAMP)形成的抑制作用通过非竞争性机制呈剂量依赖性受损。放射性配体结合研究表明,在存在Na+/Mg++/鸟苷5'-三磷酸(GMP-PNP)的情况下进行测试时,毒素处理的细胞膜中阿片样物质激动剂结合显著减少。此外,鸟嘌呤核苷酸降低阿片样物质激动剂结合的效力受到不同调节。这些研究可能有助于我们理解导致急性和慢性阿片类药物作用的机制。