Department of Biomolecular Chemistry, Medical University of Lodz, Lodz, Poland.
Institute of Organic Chemistry, Lodz University of Technology, Lodz, Poland.
Peptides. 2020 Aug;130:170331. doi: 10.1016/j.peptides.2020.170331. Epub 2020 Jun 1.
Reducing the well-known side effects of opioids prescribed to treat chronic pain remains unresolved, despite extensive research in this field. Among several options to tackle this problem the synthesis of multifunctional compounds containing hybridized structures gained a lot of interest. Recently, extensively investigated are combinations of opioid agonist and antagonist pharmacophores embodied in a single molecule. To this end, agonism at the μ opioid receptor (MOR) with simultaneous antagonism at the δ opioid receptor (DOR) emerged as a promising avenue to obtaining novel analogs devoid of serious adverse effects associated with morphine-based analgesics. In this review we covered up-to-date research on the synthesis of peptide-based ligands with MOR agonist/DOR antagonist profile.
尽管在该领域进行了广泛的研究，但仍未解决用于治疗慢性疼痛的阿片类药物的已知副作用问题。为了解决这个问题，有几种选择，其中包含杂化结构的多功能化合物的合成引起了广泛的关注。最近，人们对包含在单个分子中的阿片类激动剂和拮抗剂药效团的组合进行了广泛的研究。为此，μ阿片受体（MOR）的激动作用与δ阿片受体（DOR）的同时拮抗作用成为获得新型类似物的有前途的途径，这些类似物没有与基于吗啡的镇痛药相关的严重不良反应。在这篇综述中，我们涵盖了具有 MOR 激动剂/DOR 拮抗剂特性的基于肽的配体的最新研究进展。
