双脑啡肽——合成、对豚鼠回肠的活性及镇痛作用。

Double-enkephalins--synthesis, activity on guinea-pig ileum, and analgesic effect.

作者信息

Lipkowski A W, Konecka A M, Sroczyńska I

出版信息

Peptides. 1982 Jul-Aug;3(4):697-700. doi: 10.1016/0196-9781(82)90173-5.

Abstract

We have synthesized enkephalin analogues in which C-terminal methionine or leucine residues are replaced by a second active fragment of the enkephalin analogue. Synthesis of two compounds is described: in one, two fragments of a D-Ala2-enkephalin analogue are connected by a -NH-NH-bridge, and in the other, three methylene groups are incorporated between the amino groups. The first compound is a very potent inhibitor of electrically induced contractions of guinea-pig ileum and produces a strong analgesia when administered intraperitoneally in mice. The second compound is less active on the ileum and fails to produce analgesia after systemic injection. The double-enkephalins may interact with mu-receptors.

摘要

我们已经合成了脑啡肽类似物，其中C末端的甲硫氨酸或亮氨酸残基被脑啡肽类似物的第二个活性片段所取代。描述了两种化合物的合成：一种是通过-NH-NH-桥连接D-Ala2-脑啡肽类似物的两个片段，另一种是在氨基之间引入三个亚甲基。第一种化合物是豚鼠回肠电诱导收缩的非常有效的抑制剂，腹腔注射给小鼠时会产生强烈的镇痛作用。第二种化合物对回肠的活性较低，全身注射后不能产生镇痛作用。双脑啡肽可能与μ受体相互作用。