β-内啡肽：羧基末端修饰的类似物的合成及其活性增强
beta-Endorphin: synthesis of analogs modified at the carboxyl terminus with increased activites.
作者信息
Li C H, Yamashiro D, Tseng L F, Chang W C, Ferrara P
出版信息
Proc Natl Acad Sci U S A. 1979 Jul;76(7):3276-8. doi: 10.1073/pnas.76.7.3276.
Abstract
Three analogs of human beta-endorphin (beta h-EP) have been synthesized: [Gly31]beta h-EP, [Gly31]beta h-endorphinamide, and [Gly31]beta h-endorphinylglycine. All are more active than beta h-EP in both the guinea pig ileum bioassay and the opiate receptor binding assay. The last two analogs are about twice as active as beta h-EP in an assay for analgesia. Modification at position 31 and extension at the COOH terminus may afford a route toward analogs with even greater biological activity.
摘要
已合成了三种人β-内啡肽（βh-EP）类似物：[甘氨酸31]βh-EP、[甘氨酸31]βh-内啡肽酰胺和[甘氨酸31]βh-内啡肽基甘氨酸。在豚鼠回肠生物测定和阿片受体结合测定中，所有这些类似物的活性均高于βh-EP。在镇痛测定中，后两种类似物的活性约为βh-EP的两倍。31位的修饰和COOH末端的延伸可能为获得具有更高生物活性的类似物提供一条途径。
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