Greenberg R, Whalley C E, Jourdikian F, Mendelson I S, Walter R, Nikolics K, Coy D H, Schally A V, Kastin A J
Pharmacol Biochem Behav. 1976;5(Suppl 1):151-8. doi: 10.1016/0091-3057(76)90345-2.
The intracarotid artery quick injection technique of Oldendorf was utilized to determine the Brain Uptake Index (BUI) of radio-labeled peptides in comparison with 3H2O or 14C-antipyrine as counterlabels. The normalized BUI values for 3H-MIF-I, 3H-alpha-MSH and 14C-AVP were 13.7, 9.6 and 13.0 respectively at 15 sec after injection consistent with their having readily penetrated the blood-brain barrier. The BUI values were similar, though somewhat increased, at 10 min postinjection consistent with their ready exit across the blood-brain barrier. At 15 sec after injection 0.5+/-0.1%/g brain of the originally injected peptide label was recovered; and 0.1+/-0.2%/g brain was recovered after 10 min. The label was distributed uniformly in the major brain regions at both times. However, the percentage of the originally injected label/g of pineal and pituitary gland tissue was 10-20 X increased as compared with the major brain regions as would be expected by their location outside the blood-brain barrier. The in vitro uptake of the radio-labeled peptides by synaptosomes prepared from the whole brain and the major brain regions was passive; it was not temperature dependent, nor was it Na+ dependent. However, the binding of the three peptides by the synaptosomes varied considerably: AVP greater than MSH greater MIF: 50 greater than 5 greater 1. The penetratin of the blood-brain barrier by the three peptides is consistent with their having CNS effects.
采用奥尔登多夫的颈内动脉快速注射技术，以3H2O或14C - 安替比林作为对照标记，测定放射性标记肽的脑摄取指数（BUI）。注射后15秒时，3H - MIF - I、3H - α - MSH和14C - AVP的标准化BUI值分别为13.7、9.6和13.0，这与它们易于穿透血脑屏障一致。注射后10分钟时，BUI值相似，尽管有所增加，这与它们易于穿过血脑屏障离开一致。注射后15秒时，回收了最初注射肽标记物的0.5±0.1%/g脑；10分钟后回收了0.1±0.2%/g脑。在这两个时间点，标记物在主要脑区均均匀分布。然而，与主要脑区相比，松果体和垂体组织中最初注射标记物的百分比增加了10 - 20倍，这与其位于血脑屏障之外的位置相符。从全脑和主要脑区制备的突触体对放射性标记肽的体外摄取是被动的；它不依赖温度，也不依赖Na +。然而，这三种肽与突触体的结合差异很大：AVP大于MSH大于MIF：50大于5大于1。这三种肽对血脑屏障的穿透与其具有中枢神经系统作用一致。
