Banks W A, Kastin A J
Veterans Administration Medical Center, New Orleans, LA 70146.
J Pharm Pharmacol. 1988 Apr;40(4):289-91. doi: 10.1111/j.2042-7158.1988.tb05248.x.
Tyr-MIF-1 (Tyr-Pro-Leu-Gly-amide) and methionine enkephalin are transported intact across the blood-brain barrier by a saturable, stereospecific system. This system has been found to be modulated by a few non-peptide substances and by certain conditions such as ageing and some stresses. We investigated the possibility that hormones structurally unrelated to Tyr-MIF-1 and the enkephalins might also be capable of modulating this transport. Twenty-one hormones were tested including steroids, proteins, glycoproteins, peptides, and thyroid hormones, in doses ranging from 0.01 pmol to 1 nmol/mouse by injecting each hormone directly into the lateral ventricle simultaneously with [125I]Tyr-MIF-1. No clear effect on transport could be established for any of the substances at the doses tested. None of these substances seemed able to act as competitive inhibitors, to share their respective transport systems with Tyr-MIF-1, or to modulate immediately the saturable transport system.
酪氨酰-促黑素细胞激素-1(酪氨酰-脯氨酰-亮氨酰-甘氨酰胺)和甲硫氨酸脑啡肽通过一个可饱和的、立体特异性系统完整地穿过血脑屏障。已发现该系统受到一些非肽类物质以及某些条件(如衰老和一些应激)的调节。我们研究了与酪氨酰-促黑素细胞激素-1和脑啡肽结构不相关的激素也可能调节这种转运的可能性。通过将21种激素(包括类固醇、蛋白质、糖蛋白、肽和甲状腺激素)以0.01皮摩尔至1纳摩尔/小鼠的剂量直接注射到侧脑室中,同时注射[125I]酪氨酰-促黑素细胞激素-1进行测试。在所测试的剂量下,没有一种物质对转运有明确的影响。这些物质似乎都不能作为竞争性抑制剂,不能与酪氨酰-促黑素细胞激素-1共享各自的转运系统,也不能立即调节可饱和转运系统。