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Trends Pharmacol Sci. 2016 Apr;37(4):279-289. doi: 10.1016/j.tips.2016.01.001. Epub 2016 Jan 29.

New Technologies for Elucidating Opioid Receptor Function.

Author information

1
Departments of Anesthesiology and Neuroscience, Washington University, School of Medicine, St Louis, MO, USA. Electronic address: bruchasm@wustl.edu.
2
Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, NC, USA. Electronic address: bryan_roth@med.unc.edu.

Abstract

Recent advances in technology, including high resolution crystal structures of opioid receptors, novel chemical tools, and new genetic approaches have provided an unparalleled palette of tools for deconstructing opioid receptor actions in vitro and in vivo. Here we provide a brief description of our understanding of opioid receptor function from both molecular and atomic perspectives, as well as their role in neural circuits in vivo. We then show how insights into the molecular details of opioid actions can facilitate the creation of functionally selective (biased) and photoswitchable opioid ligands. Finally, we describe how newly engineered opioid receptor-based chemogenetic and optogenetic tools, and new mouse lines, are expanding and transforming our understanding of opioid function and, perhaps, paving the way for new therapeutics.

KEYWORDS:

DREADDs; biased signaling; chemogenetics; functional selectivity; mouse models; optogenetics

PMID:
26833118
PMCID:
PMC4811714
DOI:
10.1016/j.tips.2016.01.001
[Indexed for MEDLINE]
Free PMC Article

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