Affiliation:
1. Department of Frontier Life Science, Nagasaki University Graduate School of Biomedical Sciences, Nagasaki, Japan
Abstract
Background and Objective:
The recent alarming reports related to “opioid crisis” necessitate
the development of safer and effective analgesics without unwanted side effects. Thus, there needs
to be an alternative target or strategy for the development of drugs for the treatment of opioid
use/abuse. As one of the novel targets, in these two decades, ligands targeting opioid receptor “heteromerization”
including mu-opioid receptor (MOPr)-delta opioid receptor (DOPr) heteromer have been
proposed and the pharmacological advancement of reduced side effects has been broadly accepted and
well recognized. In this review, some of the ligands targeting both MOPr and DOPr or MOPr-DOPr
heteromers are introduced especially focusing on their pharmacological effects in vivo.
Conclusion:
It has been found that most of those ligands possess potent antinociceptive activity (as
much as or higher than that of morphine) with reduced side effects such as tolerance. In addition, some
of them are also able to reduce or prevent physiological withdrawal symptoms observed under chronic
opioid use. Importantly, there are an increasing number of evidence that show changes in heteromer
expression in various pathological animal models and these strongly argue for targeting heteromers for
the development of the next generation of pain medication in the near future.
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,General Medicine
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