β-内啡肽：在第1、2、4和5位带有D-氨基酸残基的类似物的合成及吗啡样活性
beta-endorphin: synthesis and morphine-like activity of analogs with D-amino acid residues in positions 1, 2, 4, and 5.
作者信息
Yamashiro D, Tseng L F, Doneen B A, Loh H H, Li C H
出版信息
Int J Pept Protein Res. 1977;10(2):159-66. doi: 10.1111/j.1399-3011.1977.tb02790.x.
Abstract
The solid-phase syntheses of [D-Tyr1]-, [D-Ala2]-, [D-Phe4]- and [D-Met5]-beta c-endorphins are described. A comparison of certain methods of purification and criteria of homogeneity is made with the use of these compounds. Bioassay of these synthetic analogs both in vitro and in vivo show that [D-Ala2]-beta c-endorphin possesses significant opiate activity whereas the other analogs have minimal activity.
摘要
本文描述了[D-酪氨酸1]-、[D-丙氨酸2]-、[D-苯丙氨酸4]-和[D-蛋氨酸5]-β内啡肽的固相合成。利用这些化合物对某些纯化方法和均一性标准进行了比较。这些合成类似物的体外和体内生物测定表明，[D-丙氨酸2]-β内啡肽具有显著的阿片活性，而其他类似物的活性则极小。
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