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Cells 2013, 2(4), 689-714; doi:10.3390/cells2040689

Pharmacological Profiles of Oligomerized μ-Opioid Receptors

Center for Drug Abuse and Addiction, China Medical University Hospital, Taichung 40447, Taiwan
China Medical University, Taichung 40442, Taiwan
Graduate Institute of Clinical Medical Science, China Medical University, Taichung 40442, Taiwan
Center for Neuropsychiatric Research, National Health Research Institutes, Zhunan, Miaoli County 35053, Taiwan
Author to whom correspondence should be addressed.
Received: 21 August 2013 / Revised: 30 September 2013 / Accepted: 9 October 2013 / Published: 11 October 2013
(This article belongs to the Special Issue Oligomerization & Trafficking of Opioid Receptors)
View Full-Text   |   Download PDF [261 KB, uploaded 11 October 2013]


Opioids are widely prescribed pain relievers with multiple side effects and potential complications. They produce analgesia via G-protein-protein coupled receptors: μ-, δ-, κ-opioid and opioid receptor-like 1 receptors. Bivalent ligands targeted to the oligomerized opioid receptors might be the key to developing analgesics without undesired side effects and obtaining effective treatment for opioid addicts. In this review we will update the biological effects of μ-opioids on homo- or hetero-oligomerized μ-opioid receptor and discuss potential mechanisms through which bivalent ligands exert beneficial effects, including adenylate cyclase regulation and receptor-mediated signaling pathways.
Keywords: μ-opioid receptor; bivalent ligand; receptor oligomerization μ-opioid receptor; bivalent ligand; receptor oligomerization
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Lee, C.W.-S.; Ho, I.-K. Pharmacological Profiles of Oligomerized μ-Opioid Receptors. Cells 2013, 2, 689-714.

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