Delta opioid agonists: a concise update on potential therapeutic applications

Journal of Clinical Pharmacy and Therapeutics
J F Peppin, R B Raffa

Abstract

The endogenous opioid system co-evolved with chemical defences, or at times symbiotic relationships, between plants and other autotrophs and heterotrophic predators - thus, it is not surprising that endogenous opioid ligands and exogenous mimetic ligands produce diverse physiological effects. Among the endogenous opioid peptides (endomorphins, enkephalins, dynorphins and nociception/orphanin FQ) derived from the precursors encoded by four genes (PNOC, PENK, PDYN and POMC) are the pentapeptides Met-enkephalin (Tyr-Gly-Gly-Phe-Met) and Leu-enkephalin (Tyr-Gly-Gly-Phe-Leu). The physiological effects of the enkephalins are mediated via 7-transmembrane G protein-coupled receptors, including delta opioid receptor (DOR). We present a concise update on the status of progress and opportunities of this approach. A literature search of the PUBMED database and a combination of keywords including delta opioid receptor, analgesia, mood and individual compounds identified therein, from industry and other source, and from www.clinicaltrials.com. DOR agonist and antagonist ligands have been developed with ever increasing affinity and selectivity for DOR over other opioid receptor subtypes and studied for therapeutic utility, primarily for pain ...Continue Reading

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Citations

Jan 18, 2016·Bioorganic & Medicinal Chemistry Letters·Andrea WolkerstorferHelmut Buschmann
Sep 1, 2016·Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology·Bálint BotzZsuzsanna Helyes
Mar 7, 2018·Journal of Molecular Medicine : Official Organ of the Gesellschaft Deutscher Naturforscher Und Ärzte·Tsung-Chih TsengShiang-Jong Tzeng
Aug 22, 2017·Frontiers in Molecular Neuroscience·Johannes Burtscher, Christoph Schwarzer

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