首页    期刊浏览 2024年11月26日 星期二
登录注册

文章基本信息

  • 标题:On resin click-chemistry-mediated synthesis of novel enkephalin analogues with potent anti-nociceptive activity
  • 本地全文:下载
  • 作者:Azzurra Stefanucci ; Wei Lei ; Stefano Pieretti
  • 期刊名称:Scientific Reports
  • 电子版ISSN:2045-2322
  • 出版年度:2019
  • 卷号:9
  • 期号:1
  • 页码:1-13
  • DOI:10.1038/s41598-019-42289-5
  • 出版社:Springer Nature
  • 摘要:Here, we report the chemical synthesis of two DPDPE analogues 7a (NOVA1) and 7b (NOVA2). This entailed the solid-phase synthesis of two enkephalin precursor chains followed by a CuI-catalyzed azide-alkyne cycloaddition, with the aim of improving in vivo analgesic efficacy versus DPDPE. NOVA2 showed good affinity and selectivity for the μ-opioid receptor (KI of 59.2 nM, EC50 of 12.9 nM, EMax of 87.3%), and long lasting anti-nociceptive effects in mice when compared to DPDPE.
国家哲学社会科学文献中心版权所有