Bélanger P C, Scheigetz J, Young R N, Charleson S E, Hudgin R L, Engelhardt E L
J Med Chem. 1981 Nov;24(11):1297-9. doi: 10.1021/jm00143a007.
The N-arginyl derivative of methionine-enkephalin (fragment 60-65 of beta-lipotropin) has been shown to be equiactive with the parent pentapeptide, despite the fact that the tyrosine amino group in this compound has been neutralized by the formation of an amide linkage. A series of N-(amino acid) derivatives of (-)-5,9 alpha-diethyl-2'-hydroxybenzomorphan was prepared and evaluated for analgesic activity. In vitro activities were found to vary greatly, depending on the nature of the amino acid used. The N-arginyl derivative was found to be equipotent to (-)-5,9 alpha-diethyl-2'hydroxybenzomorphan and also to methionine-enkephaline in the naloxone binding assay.
已表明甲硫氨酸脑啡肽（β-促脂素的60 - 65片段）的N - 精氨酰衍生物与母体五肽具有同等活性，尽管该化合物中的酪氨酸氨基已通过酰胺键的形成而被中和。制备了一系列（-）-5,9α-二乙基-2'-羟基苯并吗啡烷的N-（氨基酸）衍生物，并对其镇痛活性进行了评估。发现体外活性差异很大，这取决于所使用氨基酸的性质。在纳洛酮结合试验中，发现N - 精氨酰衍生物与（-）-5,9α-二乙基-2'-羟基苯并吗啡烷以及甲硫氨酸脑啡肽具有同等效力。
