Opioid-receptor-heteromer-specific trafficking and pharmacology
نویسندگان
چکیده
منابع مشابه
Opioid receptor trafficking and interaction in nociceptors.
UNLABELLED Opiate analgesics such as morphine are often used for pain therapy. However, antinociceptive tolerance and dependence may develop with long-term use of these drugs. It was found that μ-opioid receptors can interact with δ-opioid receptors, and morphine antinociceptive tolerance can be reduced by blocking δ-opioid receptors. Recent studies have shown that μ- and δ-opioid receptors are...
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Anne Morinville,1,2 Catherine M. Cahill,2 M. James Esdaile,2 Haneen Aibak,2 Brian Collier,1 Brigitte L. Kieffer,3 and Alain Beaudet2 1Department of Pharmacology and Therapeutics, McGill University, Montréal, Québec, Canada H3G 1Y6, 2Montréal Neurological Institute, McGill University, Montréal, Québec, Canada H3A 2B4, and 3Institute of Genetics and of Molecular and Cellular Biology, National Cen...
متن کاملOpioid pharmacology.
BACKGROUND Mu agonists have been an important component of pain treatment for thousands of years. The usual pharmacokinetic parameters (half-life, clearance, volume of distribution) of opioids have been known for some time. However, the metabolism has, until recently, been poorly understood, and there has been recent interest in the role of metabolites in modifying the pharmacodynamic response ...
متن کاملHeteromerization of the μ- and δ-opioid receptors produces ligand-biased antagonism and alters μ-receptor trafficking.
Heteromerization of opioid receptors has been shown to alter opioid receptor pharmacology. However, how receptor heteromerization affects the processes of endocytosis and postendocytic sorting has not been closely examined. This question is of particular relevance for heteromers of the μ-opioid receptor (MOR) and δ-opioid receptor (DOR), because the MOR is recycled primarily after endocytosis a...
متن کاملAnti-Analgesic Effect of the Mu/Delta Opioid Receptor Heteromer Revealed by Ligand-Biased Antagonism
Delta (DOR) and mu opioid receptors (MOR) can complex as heteromers, conferring functional properties in agonist binding, signaling and trafficking that can differ markedly from their homomeric counterparts. Because of these differences, DOR/MOR heteromers may be a novel therapeutic target in the treatment of pain. However, there are currently no ligands selective for DOR/MOR heteromers, and, c...
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ژورنال
عنوان ژورنال: Current Opinion in Pharmacology
سال: 2010
ISSN: 1471-4892
DOI: 10.1016/j.coph.2009.09.007