DOUBLE-ENKEPHALINS - SYNTHESIS, ACTIVITY ON GUINEA-PIG ILEUM, AND ANALGESIC EFFECT
DOUBLE-ENKEPHALINS - SYNTHESIS, ACTIVITY ON GUINEA-PIG ILEUM, AND ANALGESIC EFFECT
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DOI：
10.1016/0196-9781(82)90173-5
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发表时间：
1982-01-01
期刊：
影响因子：
3
通讯作者：
SROCZYNSKA, I
中科院分区：
文献类型：
--
作者：
LIPKOWSKI, AW;KONECKA, AM;SROCZYNSKA, I
脑啡肽类似物的c端Met Leu残基被脑啡肽类似物的第二个活性片段所取代。本文描述了两种化合物的合成：在一种化合物中，d - ala2 -脑啡肽类似物的两个片段通过- nh - nh -桥连接，在另一种化合物中，三个亚甲基在氨基之间结合。第一种化合物是一种非常有效的豚鼠回肠电致收缩抑制剂，在小鼠腹腔注射时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。双脑啡肽可与。mu -受体相互作用。
Enkephalin analogs were synthesized in which C-terminal Met Leu residues are replaced by a 2nd active fragment of the enkephalin analog. Synthesis of 2 compounds is described: in one, 2 fragments of a D-Ala2-enkephalin analog are connected by a -NH-NH- bridge, and in the other, 3 methylene groups are incorporated between the amino groups. The 1st compound is a very potent inhibitor of electrically induced contractions of guinea-pig ileum and produces a strong analgesia when administered i.p. in mice. The 2nd compound is less active on the ileum and fails to produce analgesia after systemic injection. The double-enkephalins may interact with .mu.-receptors.