Ermisch A, Rühle H J, Neubert K, Hartrodt B, Landgraf R
J Neurochem. 1983 Nov;41(5):1229-33. doi: 10.1111/j.1471-4159.1983.tb00816.x.
After intracarotid injection of [3H]beta-casomorphin-5 (beta CM5) in rats, the accumulation of radioactivity was determined in 18 brain regions and the anterior pituitary. The relative accumulation in all regions significantly exceeded that of [3H]inulin by a factor of 2.5, indicating a low but measurable brain uptake of the peptide. In blood-brain barrier-free areas, the accumulation of radioactivity was 15-fold higher than in blood-brain barrier-protected areas. The relative accumulation was not dependent on the total beta CM5 concentration in the range of 0.3-1.1 microM, and was not depressed by 400 microM L-tyrosine. We conclude that beta CM5, like other peptides, is accumulated in the blood-brain barrier-free areas to a relatively high but differing degree, whereas in the areas with a tight endothelium the accumulation is relatively low and nearly uniform. A binding to endothelial cells may contribute to the low accumulation of beta CM5, especially in blood-brain barrier-protected areas.
给大鼠颈内注射[3H]β-酪蛋白吗啡-5（βCM5）后，测定了18个脑区和垂体前叶的放射性积累情况。所有区域的相对积累量比[3H]菊粉显著高出2.5倍，表明该肽在脑中的摄取量较低但可测量。在无血脑屏障区域，放射性积累比有血脑屏障保护的区域高15倍。相对积累量在0.3 - 1.1微摩尔范围内不依赖于βCM5的总浓度，且不受400微摩尔L-酪氨酸的抑制。我们得出结论，βCM5与其他肽一样，在无血脑屏障区域相对高度但不同程度地积累，而在内皮紧密的区域积累相对较低且几乎均匀。与内皮细胞的结合可能导致βCM5积累较低，尤其是在有血脑屏障保护的区域。
