Barg J, Belcheva M M, Bem W T, Lambourne B, McLachlan J A, Tolman K C, Johnson F E, Coscia C J
E. A. Doisy Department of Biochemistry and Molecular Biology, St. Louis University School of Medicine, MO 63104.
Peptides. 1991 Jul-Aug;12(4):845-9. doi: 10.1016/0196-9781(91)90144-e.
Exposure of C6 glial cell cultures to desipramine induced the appearance of opioid receptors and up-regulated sigma receptors. Opioid binding was demonstrated with 3H-etorphine and 3H-dihydromorphine (DHM), but was not observed with the mu, delta and kappa ligands 3H-DAMGE, 3H-DADLE or 3H-(-)ethylketocyclazocine in the presence of specific blockers, respectively. Competition experiments with 3H-DHM and either (-)naloxone or (+)naloxone indicated the presence of authentic opioid receptors. In similar studies with beta-endorphin, its truncated form (1-27) or their N-acetyl derivatives, beta-endorphin proved to have the highest affinity. Opioid receptors in glial cell aggregates were primarily kappa, with few mu and delta sites. Desipramine increased Bmax values for kappa but not mu and delta.
将C6神经胶质细胞培养物暴露于地昔帕明会诱导阿片受体的出现并上调σ受体。用³H-埃托啡和³H-二氢吗啡（DHM）证实了阿片结合，但在分别存在特异性阻滞剂的情况下，用μ、δ和κ配体³H-DAMGE、³H-DADLE或³H-（-）乙基酮环唑辛未观察到阿片结合。用³H-DHM与（-）纳洛酮或（+）纳洛酮进行的竞争实验表明存在真正的阿片受体。在对β-内啡肽、其截短形式（1-27）或其N-乙酰衍生物的类似研究中，β-内啡肽被证明具有最高的亲和力。神经胶质细胞聚集体中的阿片受体主要是κ型，μ和δ位点很少。地昔帕明增加了κ型的Bmax值，但未增加μ和δ型的Bmax值。
