Vavrek R J, Cui R L, York E J, Stewart J M, Paterson S, Kosterlitz H W
Life Sci. 1983;33 Suppl 1:451-4. doi: 10.1016/0024-3205(83)90539-8.
A general trend toward increased mu-selectivity has been reported in two classes of minimal structure enkephalin analogs which contain the essential structural and functional information for potent enkephalin-like biological activity. A single Lys residue added to the amino terminal of several tripeptide amides, and to the potent dipeptide amide Tyr-DAla-phenylpropylamide, causes a further increase in mu-selectivity as determined in the stimulated guinea pig ileum (GPI) and mouse vas deferens (MVD) assays, and in receptor binding studies in homogenates of guinea pig brain. The effect of Lys substitution was a significant decrease in the delta-related MVD potencies.
据报道，在两类最小结构脑啡肽类似物中存在μ选择性增加的总体趋势，这些类似物包含了强效脑啡肽样生物活性的基本结构和功能信息。在几种三肽酰胺的氨基末端以及强效二肽酰胺Tyr-DAla-苯丙基酰胺上添加单个赖氨酸残基，会导致在刺激的豚鼠回肠（GPI）和小鼠输精管（MVD）试验以及豚鼠脑匀浆的受体结合研究中测定的μ选择性进一步增加。赖氨酸取代的作用是与δ相关的MVD效力显著降低。
