Regulation of opioid receptor function by chronic agonist exposure: Constitutive activity and desensitization

Molecular Pharmacology

Volumn 60, Issue 1, 2001, Pages 20-25

  Chavkin, Charles ^a,b   Mclaughlin, Jay P ^a   Celver, Jeremy P ^a  

^a UNIVERSITY OF WASHINGTON SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF WASHINGTON   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DELTA OPIATE RECEPTOR; G PROTEIN COUPLED RECEPTOR; MORPHINE; MU OPIATE RECEPTOR; OPIATE AGONIST; OPIATE RECEPTOR;

BINDING AFFINITY; DRUG MECHANISM; GENE EXPRESSION; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; PROTEIN STABILITY; RECEPTOR BINDING; RECEPTOR DOWN REGULATION; RECEPTOR INTRINSIC ACTIVITY; REVIEW;

EID: 0034954517     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.60.1.20     Document Type: Review

References (55)

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14. Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists
15. Selected cysteine residues in transmembrane domains of μ-opioid receptor are critical for effects of sulfhydryl reagents
16. Phosphorylation of Ser363, Thr370 and Ser375 residues within the carboxyl tail differentially regulates mu-opioid receptor internalization
17. The absence of a direct correlation between the loss of [D-Ala2, MePhe4, Gly5-ol]Enkephalin inhibition of adenylyl cyclase activity and agonist-induced mu-opioid receptor phosphorylation
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22. Allelic variation S268P of the human μ-opioid receptor affects both desensitization and G protein coupling
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34. 2 cannabinoid receptor
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41. The relationship between agonist intrinsic activity and the rate of endocytosis of muscarinic receptors in a human neuroblastoma cell line
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52. The conserved cysteine 7.38 residue is differentially accessible in the binding-site crevices of the mu, delta, and kappa opioid receptors
53. Functional role of the spatial proximity of Asp114(2.50) in TMH 2 and Asn332(7.49) in TMH 7 of the mu opioid receptor
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55. Mutation of human mu opioid receptor extracellular "disulfide cysteine" residues alters ligand binding but does not prevent receptor targeting to the cell plasma membrane