Herein we present the expedient synthesis of endomorphin-1 analogues containing stereoisomeric β²-homo-Freidinger lactam-like scaffolds ([Amo²]EM), and we discuss opioid receptor (OR) affinity, enzymatic stability, functional activity, in vivo antinociceptive effects, and conformational and molecular docking analysis. Hence, H-Tyr-Amo-Trp-PheNH₂ resulted to be a new chemotype of highly stable, selective, partial KOR agonist inducing analgesia, therefore displaying great potential interest as a painkiller possibly with reduced harmful side effects.

中文翻译：

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通过β，α混合二肽/杂环支架约束Endomorphin-1：新型κ阿片受体选择性局部激动剂的鉴定。

本文我们提出的内吗啡肽-1含有立体异构体β类似物权宜合成² -homo-Freidinger内酰胺状支架（[阿莫² ] EM），我们讨论阿片受体（OR）的亲和力，酶的稳定性，功能性活性，体内镇痛效应，以及构象和分子对接分析。因此，H-Tyr-Amo-Trp-PheNH ₂成为诱导镇痛的高度稳定，选择性，部分KOR激动剂的新化学型，因此显示出作为止痛药的巨大潜力，可能具有减少的有害副作用。