Synthesis and biological activity of N-methylated analogs of endomorphin-2

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• 作者：Rafal Kruszynski ; Jakub Fichna ; Jean-Claude do-Rego ; Tomasz Janecki ; Piotr Kosson ; Wanda Pakulska ; Jean Costentin and Anna Janecka
• 关键词：Antinociceptive activity ; Binding studies ; μ ; -Opioid receptor agonists
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2005
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：2005
• 卷：13
• 期：24
• 页码：6713-6717
• 文件大小：170 K

摘要

In this paper, we describe the synthesis of a series of endomorphin-2 analogs containing N-methylated amino acids, consecutively in each position. The μ-opioid receptor binding affinities of the new analogs were determined in the displacement experiments. Their in vivo antinociceptive activity was assessed in the hot-plate test in mice after central (icv) and peripheral (ip) administration. [Sar²]endomorphin-2, which had the highest μ-receptor affinity, also showed the strongest analgesic effect when administered centrally and was the only analog that retained activity after peripheral injection.