Synthesis, biological, and structural explorations of a series of μ-opioid receptor (MOR) agonists with high G protein signaling bias
- 1 January 2022
- journal article
- research article
- Published by Elsevier in European Journal of Medicinal Chemistry
- Vol. 228, 113986
Abstract
No abstract availableKeywords
This publication has 37 references indexed in Scilit:
- Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteersPain, 2014
- β-Arrestins: Regulatory Role and Therapeutic Potential in Opioid and Cannabinoid Receptor-Mediated Analgesia2013
- Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe PainJournal of Medicinal Chemistry, 2013
- A G Protein-Biased Ligand at the μ-Opioid Receptor Is Potently Analgesic with Reduced Gastrointestinal and Respiratory Dysfunction Compared with MorphineThe Journal of Pharmacology and Experimental Therapeutics, 2013
- Efficient, highly diastereoselective MS 4 Å-promoted one-pot, three-component synthesis of 2,6-disubstituted-4-tosyloxytetrahydropyrans via Prins cyclizationBeilstein Journal of Organic Chemistry, 2012
- Opioids and the control of respirationBritish Journal of Anaesthesia, 2008
- Morphine Side Effects in β-Arrestin 2 Knockout MiceThe Journal of Pharmacology and Experimental Therapeutics, 2005
- Mu opioid receptor regulation and opiate responsivenessThe AAPS Journal, 2005
- Anesthetic Potency and Influence of Morphine and Sevoflurane on Respiration in μ-Opioid Receptor Knockout MiceAnesthesiology, 2001
- Enhanced Morphine Analgesia in Mice Lacking β-Arrestin 2Science, 1999