ArticleThe journal of physical chemistry. B2013
Molecular details of the activation of the μ opioid receptor.
Article in The journal of physical chemistry. B, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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The trial behind it
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Who cites it
18 citing papers in PubMed, 29 citations in OpenAlex.
- Development and Validation of a Gas Chromatography-Mass Spectrometry Method for the Determination of Fentanyl and Butyryl Fentanyl in Oral Fluid.Analytical science advances · 2025Article
- Design, synthesis, in-vivo, and in-silico studies of 1,2,3-triazole tethered derivatives of morphine as novel anti-nociceptive agents.PloS one · 2025Article
- Three-Dimensional Structural Insights Have Revealed the Distinct Binding Interactions of Agonists, Partial Agonists, and Antagonists with the µ Opioid Receptor.International journal of molecular sciences · 2023Review
- Computational Methods for Understanding the Selectivity and Signal Transduction Mechanism of Aminomethyl Tetrahydronaphthalene to Opioid Receptors.Molecules (Basel, Switzerland) · 2022Article
- Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs.International journal of molecular sciences · 2021Review
- Unnarmicin D, an Anti-inflammatory Cyanobacterial Metabolite with δ and μ Opioid Binding Activity Discovered via a Pipeline Approach Designed to Target Neurotherapeutics.ACS chemical neuroscience · 2020Article
- Identification and characterization of fragment binding sites for allosteric ligand design using the site identification by ligand competitive saturation hotspots approach (SILCS-Hotspots).Biochimica et biophysica acta. General subjects · 2020Article
- Insights into the function of opioid receptors from molecular dynamics simulations of available crystal structures.British journal of pharmacology · 2018Review
- Computational insights into the G-protein-biased activation and inactivation mechanisms of the μ opioid receptor.Acta pharmacologica Sinica · 2018Article
- Predicting opioid receptor binding affinity of pharmacologically unclassified designer substances using molecular docking.PloS one · 2018Article
- Drug Binding Poses Relate Structure with Efficacy in the μ Opioid Receptor.Journal of molecular biology · 2017Article
- Competitive association binding kinetic assays: a new tool to detect two different binding orientations of a ligand to its target protein under distinct conditions?Naunyn-Schmiedeberg's archives of pharmacology · 2017Article
- Conformational Heterogeneity of Intracellular Loop 3 of the μ-opioid G-protein Coupled Receptor.The journal of physical chemistry. B · 2016Article
- Racemic Salsolinol and its Enantiomers Act as Agonists of the μ-Opioid Receptor by Activating the Gi Protein-Adenylate Cyclase Pathway.Frontiers in behavioral neuroscience · 2016Article
- Synthesis of Carfentanil Amide Opioids Using the Ugi Multicomponent Reaction.ACS chemical neuroscience · 2015Article
- Opioid receptors: Structural and mechanistic insights into pharmacology and signaling.European journal of pharmacology · 2015Review
- Differential Regulation of 6- and 7-Transmembrane Helix Variants of μ-Opioid Receptor in Response to Morphine Stimulation.PloS one · 2015Article
- On the modularity of the intrinsic flexibility of the µ opioid receptor: a computational study.PloS one · 2014Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Molecular details of μ opioid receptor activations were obtained using molecular dynamics simulations of the receptor in the presence of three agonists, three antagonists, and a partial agonist and on the constitutively active T279K mutant. Agonists have a higher probability of direct interactions of their basic nitrogen (N) with Asp147 as compared with antagonists, indicating that direct ligand-Asp147 interactions modulate activation. Medium-size substituents on the basic N of antagonists lead to steric interactions that perturb N-Asp147 interactions, while additional favorable interactions occur with larger basic N substituents, such as in N-phenethylnormorphine, restoring N-Asp147 interactions, leading to agonism. With the orvinols, the increased size of the C19 substituent in buprenorphine over diprenorphine leads to increased interactions with residues adjacent to Asp147, partially overcoming the presence of the cyclopropyl N substituent, such that buprenorphine is a partial agonist. Results also indicate different conformational properties of the intracellular regions of the transmembrane helices in agonists versus antagonists.
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Registered trials
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.