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A G Protein-Biased Ligand at the μ-Opioid Receptor Is Potently Analgesic with Reduced Gastrointestinal and Respiratory Dysfunction Compared with Morphine

Journal of Pharmacology and Experimental Therapeutics · 2013 · Vol. 344(3) · pp. 708–717
Receptor Mechanisms and SignalingNeuropeptides and Animal PhysiologyPharmacological Receptor Mechanisms and EffectsMorphineAnalgesicOpioidμ-opioid receptorRespiratory systemPharmacologyReceptorMedicineG protein-coupled receptorOpioid receptor

MeSH terms

beta-Arrestinsbeta-Arrestin 2AnalgesicsAnimalsCell LineGastrointestinal DiseasesHumansLigandsMaleMice, Inbred C57BLMorphineRespiratory SystemRespiratory Tract DiseasesSignal TransductionRats, Sprague-Dawley

Funding

  • National Institutes of Health
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639
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17.04
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61
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Cited by
Biased agonism: An emerging paradigm in GPCR drug discovery
Bioorganic & Medicinal Chemistry Letters · 2015 · 269 citations
References
β-Arrestin-biased ligands at seven-transmembrane receptors
Trends in Pharmacological Sciences · 2007 · 587 citations
Morphine Side Effects in β-Arrestin 2 Knockout Mice
Journal of Pharmacology and Experimental Therapeutics · 2005 · 601 citations
A METHOD FOR DETERMINING LOSS OF PAIN SENSATION
Journal of Pharmacology and Experimental Therapeutics · 1941 · 3,222 citations
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