脯氨酰-亮氨酰-甘氨酰胺、环（亮氨酰甘氨酸）及其衍生物可阻止小鼠对吗啡产生身体依赖性。
Prolyl-leucyl-glycinamide, cyclo(leucylglycine), and derivatives block development of physical dependence on morphine in mice.
作者信息
Walter R, Ritzmann R F, Bhargava H N, Flexner L B
出版信息
Proc Natl Acad Sci U S A. 1979 Jan;76(1):518-20. doi: 10.1073/pnas.76.1.518.
Abstract
Pro-Leu-Gly-NH2 (MIF) and several structural analogues, all injected in 50-microgram doses daily in mice receiving morphine chronically, were found to prevent development of physical dependence as measured by changes in body temperature associated with naloxone-induced withdrawal. Dose-response studies, using again a protocol of daily injections of peptide at 50, 5, 0.5, 0.05, 0.005 microgram per mouse revealed MIF and cyclo(Leu-Gly) to be the most potent peptides and to be effective in blocking physical dependence to morphine at a dose as low as 0.5 and 0.05 microgram per mouse, respectively. The benzyloxycarbonyl derivative of MIF, Pro-Leu, and Pro- -Leu exhibited significant activities down to a dose of 5 microgram of peptide per mouse.
摘要
每天给长期接受吗啡的小鼠注射50微克剂量的脯氨酸-亮氨酸-甘氨酸-酰胺（MIF）及几种结构类似物，结果发现，通过与纳洛酮诱导戒断相关的体温变化来衡量，这些物质可预防身体依赖性的形成。再次采用每天每只小鼠注射50、5、0.5、0.05、0.005微克肽的方案进行剂量反应研究，结果显示MIF和环（亮氨酸-甘氨酸）是最有效的肽，分别在低至每只小鼠0.5微克和0.05微克的剂量下就能有效阻断对吗啡的身体依赖性。MIF的苄氧羰基衍生物、脯氨酸-亮氨酸和脯氨酸-苯丙氨酸-亮氨酸在低至每只小鼠5微克肽的剂量时仍表现出显著活性。
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