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PMID:20525224

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Citation

Gris, P, Gauthier, J, Cheng, P, Gibson, DG, Gris, D, Laur, O, Pierson, J, Wentworth, S, Nackley, AG, Maixner, W and Diatchenko, L (2010) A novel alternatively spliced isoform of the mu-opioid receptor: functional antagonism. Mol Pain 6:33

Abstract

Opioids are the most widely used analgesics for the treatment of clinical pain. They produce their therapeutic effects by binding to mu-opioid receptors (MORs), which are 7 transmembrane domain (7TM) G-protein-coupled receptors (GPCRs), and inhibiting cellular activity. However, the analgesic efficacy of opioids is compromised by side-effects such as analgesic tolerance, dependence and opioid-induced hyperalgesia (OIH). In contrast to opioid analgesia these side effects are associated with cellular excitation. Several hypotheses have been advanced to explain these phenomena, yet the molecular mechanisms underlying tolerance and OIH remain poorly understood.

Links

PubMed PMC2894766 Online version:10.1186/1744-8069-6-33

Keywords

Alternative Splicing; Analgesics, Opioid/metabolism; Analgesics, Opioid/pharmacology; Animals; COS Cells; Calcium/metabolism; Cercopithecus aethiops; Cyclic AMP/metabolism; GTP-Binding Proteins/metabolism; Humans; Morphine/metabolism; Morphine/pharmacology; Nitric Oxide/metabolism; Protein Isoforms/antagonists & inhibitors; Protein Isoforms/genetics; Protein Isoforms/metabolism; Receptors, Opioid, mu/agonists; Receptors, Opioid, mu/antagonists & inhibitors; Receptors, Opioid, mu/genetics

Significance

Annotations

Gene product Qualifier GO Term Evidence Code with/from Aspect Extension Notes Status

HUMAN:OPRM

involved_in

GO:0043951: negative regulation of cAMP-mediated signaling

ECO:0000314: direct assay evidence used in manual assertion

P

Seeded From UniProt

complete

HUMAN:OPRM

involved_in

GO:0045019: negative regulation of nitric oxide biosynthetic process

ECO:0000314: direct assay evidence used in manual assertion

P

Seeded From UniProt

complete

HUMAN:OPRM

involved_in

GO:0051481: negative regulation of cytosolic calcium ion concentration

ECO:0000314: direct assay evidence used in manual assertion

P

Seeded From UniProt

complete

See also

References

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