Design, synthesis, and evaluation of opioid analogues with non-peptidic β-turn scaffold:: Enkephalin and endomorphin mimetics

被引:79
作者
Eguchi, M
Shen, RYW
Shea, JP
Lee, MS
Kahn, M
机构
[1] Pacific NW Res Inst, Seattle, WA 98122 USA
[2] Molecumet Ltd, Bellevue, WA 98005 USA
[3] Univ Washington, Dept Pathobiol, Seattle, WA 98195 USA
关键词
D O I
10.1021/jm0155897
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We have identified a mu-selective opioid receptor agonist without a cationic amino group in the molecule from libraries of bicyclic U-turn peptidomimetics. The biologically active conformation of the lead is proposed to mimic an endomorphin type III 4 --> 1 beta-turn conformation.
引用
收藏
页码:1395 / 1398
页数:4
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