Molecular Mechanisms of Opioid Receptor-Dependent Signaling and Behavior

By R. Al-Hasani, M. Bruchas. Anesthesiology, 2011

919 citations recorded by the source corpus.

Opioid receptors have been targeted for the treatment of pain and related disorders for thousands of years, and remain the most widely used analgesics in the clinic. Mu (μ), kappa (κ), and delta (δ) opioid receptors represent the originally classified receptor subtypes, with opioid receptor like-1 (ORL1) being the least characterized. All four receptors are G-protein coupled, and activate inhibitory G-proteins. These receptors form homo- and hetereodimeric complexes, signal to kinase cascades, and scaffold a variety of proteins. In this review, we discuss classical mechanisms and developments in understanding opioid tolerance, opioid receptor signaling, and highlight advances in opioid molecular pharmacology, behavioral pharmacology, and human genetics. We put into context how opioid receptor signaling leads to the modulation of behavior with the potential for therapeutic intervention. Finally, we conclude that there is a continued need for more translational work on opioid receptors in vivo.

Subfields: Cellular and Molecular Neuroscience, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/5096f422043a772227bac7064ec8d2b597622113

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In Cellular and Molecular Neuroscience

In Molecular Biology

Citations in the corpus

The Neuroscience of Drug Reward and Addiction. (2019, positive): “In addition, activation of MOR increases mitogen-activated protein kinase (MAPK) signaling while their phosphorylation activates the arrestin pathway (5), which has the ability to desensitize, activate, and control the trafﬁcking of G protein-coupled receptors (GPCR) (140).”