Banks W A, Kastin A J
Life Sci. 1987 Sep 14;41(11):1319-38. doi: 10.1016/0024-3205(87)90606-0.
Peptides can be transported across the blood-brain barrier by saturable transport systems. One system, characterized with radioactively labeled Tyr-MIF-1 (Tyr-Pro-Leu-Gly-amide), is specific for some of the small peptides with an N-terminal tyrosine, including Tyr-MIF-1, the enkephalins, beta-casomorphin, and dynorphin (1-8). Another separate system transports vasopressin-like peptides. The choroid plexus has at least one system distinguishable from those above that is capable of uptake and possibly transport of opiate-like peptides. The possibility of saturable transport of other peptides has been investigated to a varying degree. Specificity, stereo-specificity, saturability, allosteric regulation, modulation by physiologic and pharmacologic manipulations, and noncompetitive inhibition have been demonstrated to occur in peptide transport systems and suggest a role for them in physiology and disease.
肽可通过可饱和转运系统穿过血脑屏障。其中一个系统，以放射性标记的酪氨酰-促黑素细胞激素释放抑制因子-1（酪氨酰-脯氨酰-亮氨酰-甘氨酰胺）为特征，对一些N端为酪氨酸的小肽具有特异性，包括酪氨酰-促黑素细胞激素释放抑制因子-1、脑啡肽、β-酪蛋白吗啡和强啡肽（1-8）。另一个独立的系统转运加压素样肽。脉络丛至少有一个与上述系统不同的系统，能够摄取并可能转运阿片样肽。其他肽的可饱和转运可能性已在不同程度上进行了研究。肽转运系统已证明具有特异性、立体特异性、饱和性、变构调节、生理和药理操作调节以及非竞争性抑制，这表明它们在生理和疾病中发挥作用。
