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Drug Alcohol Depend. 2012 Mar 1;121(3):167-72. doi: 10.1016/j.drugalcdep.2011.10.025. Epub 2011 Nov 23.

Functional relevance of μ-δ opioid receptor heteromerization: a role in novel signaling and implications for the treatment of addiction disorders: from a symposium on new concepts in mu-opioid pharmacology.

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Department of Pharmacology and Systems Therapeutics, The Mount Sinai School of Medicine, New York, NY 10029, United States.


Morphine and other opiates are among the most widely prescribed and clinically useful medications for the treatment of chronic pain. However, the applicability of these compounds has been severely hampered by the rapid development of tolerance and physical dependence that typically accompanies their repeated use. A growing body of evidence has implicated the regulated functioning of μ-δ opioid receptor heteromers in both the modulation of morphine-mediated antinociception, and in the limitation of undesirable side effects resulting from chronic opiate exposure. Moreover, μ-δ heteromers exhibit unique ligand binding characteristics and signaling properties, indicating that pharmacological targeting of the μ-δ heteromer may represent a novel therapeutic approach for the management of chronic pain and addiction disorders. Therefore, the present review will attempt to summarize the latest relevant findings regarding the regulation and functional characteristics of the μ-δ heteromer both in vitro and in vivo.

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