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Curr Opin Pharmacol. 2010 Feb;10(1):73-9. doi: 10.1016/j.coph.2009.09.007. Epub 2009 Oct 19.

Opioid-receptor-heteromer-specific trafficking and pharmacology.

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Ernest Gallo Clinic and Research Center, University of California San Francisco, Department of Neurology, Emeryville, CA 94608, USA.


Homomerization and heteromerization of 7 transmembrane spanning (7TM)/G-protein-coupled receptors (GPCRs) have been an important field of study. Whereas initial studies were performed in artificial cell systems, recent publications are shifting the focus to the in vivo relevance of heteromerization. This is especially apparent for the field of opioid receptors. Drugs have been identified that selectively target opioid heteromers of the delta-opioid receptor with the kappa and the mu-opioid receptors that influence nociception and ethanol consumption, respectively. In addition, in several cases, the specific physiological response produced by the heteromer may be directly attributed to a difference in receptor trafficking properties of the heteromers compared with their homomeric counterparts. This review attempts to highlight some of the latest developments with regard to opioid receptor heteromer trafficking and pharmacology.

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