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Annu Rev Neurosci. 2018 Jul 8;41:453-473. doi: 10.1146/annurev-neuro-080317-061522. Epub 2018 May 31.

Endogenous and Exogenous Opioids in Pain.

Corder G1,2,3,4, Castro DC5, Bruchas MR5,6,7,8,9, Scherrer G1,2,3,4,10.

Author information

1
Department of Anesthesiology, Perioperative and Pain Medicine, Stanford University, Palo Alto, California 94304, USA; email: gs25@stanford.edu.
2
Department of Molecular and Cellular Physiology, Stanford University, Palo Alto, California 94304, USA.
3
Department of Neurosurgery, Stanford University, Palo Alto, California 94304, USA.
4
Stanford Neurosciences Institute, Palo Alto, California 94304, USA.
5
Department of Anesthesiology, Washington University in St. Louis, St. Louis, Missouri 63130, USA; email: bruchasm@wustl.edu.
6
Division of Basic Research, Department of Anesthesiology, Washington University School of Medicine, St. Louis, Missouri 63130, USA.
7
Washington University Pain Center, Washington University School of Medicine, St. Louis, Missouri 63130, USA.
8
Department of Neuroscience, Washington University School of Medicine, St. Louis, Missouri 63130, USA.
9
Department of Biomedical Engineering, Washington University in St. Louis, St. Louis, Missouri 63130, USA.
10
New York Stem Cell Foundation - Robertson Investigator, Stanford University, Palo Alto, California 94304, USA.

Abstract

Opioids are the most commonly used and effective analgesic treatments for severe pain, but they have recently come under scrutiny owing to epidemic levels of abuse and overdose. These compounds act on the endogenous opioid system, which comprises four G protein-coupled receptors (mu, delta, kappa, and nociceptin) and four major peptide families (β-endorphin, enkephalins, dynorphins, and nociceptin/orphanin FQ). In this review, we first describe the functional organization and pharmacology of the endogenous opioid system. We then summarize current knowledge on the signaling mechanisms by which opioids regulate neuronal function and neurotransmission. Finally, we discuss the loci of opioid analgesic action along peripheral and central pain pathways, emphasizing the pain-relieving properties of opioids against the affective dimension of the pain experience.

KEYWORDS:

analgesia; neuroanatomy; opioid; pain; perception; signaling

[Indexed for MEDLINE]
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