ArticleMolecular pharmacology2018
Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors.
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Article in Molecular pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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42citing papers in PubMed
2.2field-weighted citation impact, top 11% of its field
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Who cites it
42 citing papers in PubMed, 111 citations in OpenAlex.
- Structure-guided allosteric modulation of the delta opioid receptor.Nature communications · 2026Article
- Positive allosteric modulation of the delta opioid receptor attenuates depression-like and pain-like behaviors but does not promote convulsions.The Journal of pharmacology and experimental therapeutics · 2026Article
- Molecular mechanism of allosteric modulation of opioid receptors.Signal transduction and targeted therapy · 2026Article
- Effects of the Mu Opioid Receptor Positive Allosteric Modulator BMS-986122 On Opioid Efficacy in Rat Neuropathic Pain States.bioRxiv : the preprint server for biology · 2026Article
- Structural and dynamic studies uncover a distinct allosteric modulatory site at the µ-opioid receptor.Nature communications · 2026Article
- A mu-opioid receptor positive allosteric modulator provides opioid-sparing antinociception without enhancing opioid side effects.The Journal of pharmacology and experimental therapeutics · 2026Article
- Structure-based design of an opioid receptor modulator for enhanced morphine analgesia.Science advances · 2026Article
- Multifaceted modulation of human opioid receptors by kratom alkaloids: binding affinity, functional selectivity, and allosteric activity.Frontiers in pharmacology · 2026Article
- Antidepressants and the endogenous opioid system.Biochemical pharmacology · 2025Review
- Effects of two structurally diverse positive allosteric modulators on signaling bias at the μ-opioid receptor.Molecular pharmacology · 2025Article
- Structural and dynamic studies uncover a distinct allosteric modulatory site at the μ-opioid receptor.bioRxiv : the preprint server for biology · 2025Article
- κ-Opioid Receptor Agonists as Robust Pain-Modulating Agents: Mechanisms and Therapeutic Potential in Pain Modulation.Journal of clinical medicine · 2025Review
- Mu Opioid Receptor Positive Allosteric Modulator BMS-986122 Confers Agonist-Dependent G Protein Subtype Signaling Bias.Biochemistry · 2025Article
- Insurmountable antagonism of human mu opioid receptors by buprenorphine is due to hemi-equilibrium.European journal of pharmacology · 2025Article
- Recommended Opioid Receptor Tool Compounds: ComparativeACS pharmacology & translational science · 2025Article
- Ketamine and Major Ketamine Metabolites Function as Allosteric Modulators of Opioid Receptors.Molecular pharmacology · 2024Article
- Structural and dynamic insights into the activation of the μ-opioid receptor by an allosteric modulator.Nature communications · 2024Article
- Structure-Activity Relationship Study of Cannabidiol-Based Analogs as Negative Allosteric Modulators of the μ-Opioid Receptor.Journal of medicinal chemistry · 2023Article
- Application of Mixed-Solvent Molecular Dynamics Simulations for Prediction of Allosteric Sites on G Protein-Coupled Receptors.Molecular pharmacology · 2023Article
- Allosteric Modulators of Dopamine DMolecules (Basel, Switzerland) · 2022Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Kathryn E LivingstonDepartment of Pharmacology and Edward F. Domino Research Center, University of Michigan, Ann Arbor, Michigan (K.E.L., M.A.S., J.R.T.); Research and Development/Discovery, Bristol-Myers Squibb Company, Wallingford, Connecticut (N.T.B., A.A.); and Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (M.C.).
M Alexander StanczykDepartment of Pharmacology and Edward F. Domino Research Center, University of Michigan, Ann Arbor, Michigan (K.E.L., M.A.S., J.R.T.); Research and Development/Discovery, Bristol-Myers Squibb Company, Wallingford, Connecticut (N.T.B., A.A.); and Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (M.C.).
Neil T BurfordDepartment of Pharmacology and Edward F. Domino Research Center, University of Michigan, Ann Arbor, Michigan (K.E.L., M.A.S., J.R.T.); Research and Development/Discovery, Bristol-Myers Squibb Company, Wallingford, Connecticut (N.T.B., A.A.); and Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (M.C.).
Andrew AltDepartment of Pharmacology and Edward F. Domino Research Center, University of Michigan, Ann Arbor, Michigan (K.E.L., M.A.S., J.R.T.); Research and Development/Discovery, Bristol-Myers Squibb Company, Wallingford, Connecticut (N.T.B., A.A.); and Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (M.C.).
Meritxell CanalsDepartment of Pharmacology and Edward F. Domino Research Center, University of Michigan, Ann Arbor, Michigan (K.E.L., M.A.S., J.R.T.); Research and Development/Discovery, Bristol-Myers Squibb Company, Wallingford, Connecticut (N.T.B., A.A.); and Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (M.C.).
John R TraynorDepartment of Pharmacology and Edward F. Domino Research Center, University of Michigan, Ann Arbor, Michigan (K.E.L., M.A.S., J.R.T.); Research and Development/Discovery, Bristol-Myers Squibb Company, Wallingford, Connecticut (N.T.B., A.A.); and Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (M.C.) jtraynor@umich.edu.
Bristol-Myers Squibb (United States) · USMonash University · AUUniversity of Michigan–Ann Arbor · US
Funding
Allosteric Modulation of the Mu-Opioid ReceptorR37DA039997 · NIDA · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI TRAYNOR, JOHN R. · 2015 to 2024
$6.4MSUBSTANCE ABUSE INTERDISCIPLINARY TRAINING PROGRAMT32DA007267 · NIDA · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI GNEGY, MARGARET E · 1994 to 2015
$4.5MNIDA NIH HHS R37 DA039997NIDA NIH HHS T32 DA007267
Abstract
Allosteric modulators of G protein-coupled receptors, including opioid receptors, have been proposed as possible therapeutic agents with enhanced selectivity. BMS-986122 is a positive allosteric modulator (PAM) of the
Indexed as
Allosteric RegulationAllosteric SiteAnimalsCell Line, TumorCHO CellsCricetulusHEK293 CellsHumansNarcotic AntagonistsRadioligand AssayRatsReceptors, Opioid, deltaReceptors, Opioid, kappaReceptors, Opioid, muSodiumSulfonesBMS-986122BMS-986187Narcotic AntagonistsReceptors, Opioid, deltaReceptors, Opioid, kappaReceptors, Opioid, muSodiumSulfonesXanthones
Identifiers
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.