ArticleMolecules (Basel, Switzerland)2022
A Journey through Diastereomeric Space: The Design, Synthesis, In Vitro and In Vivo Pharmacological Activity, and Molecular Modeling of Novel Potent Diastereomeric MOR Agonists and Antagonists.
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In one paragraph
Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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0cells of the map it votes in
8citing papers in PubMed
0.8field-weighted citation impact, top 31% of its field
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Who cites it
8 citing papers in PubMed, 10 citations in OpenAlex.
- Effects of repeated treatment with opioids that vary in mu opioid receptor efficacy on pain-depressed locomotor behavior in mice.Psychopharmacology · 2026Article
- Transformation of a Potent C9-Substituted Phenylmorphan into MOR Partial Agonists with Improvement of Metabolic Stability: An In Vitro, In Vivo, and In Silico Study.ACS chemical neuroscience · 2025Article
- Low-Efficacy Mu Opioid Agonists as Candidate Analgesics: Effects of Novel C-9 Substituted Phenylmorphans on Pain-Depressed Behavior in Mice.The Journal of pharmacology and experimental therapeutics · 2024Article
- Functional Activity of Enantiomeric Oximes and Diastereomeric Amines and Cyano Substituents at C9 in 3-Hydroxy-Molecules (Basel, Switzerland) · 2024Article
- Potent MOR Agonists from 2'-Hydroxy-5,9-dimethyl-Molecules (Basel, Switzerland) · 2023Article
- Role of efficacy as a determinant of locomotor activation by mu-opioid receptor (MOR) ligands in female and male mice. II. Effects of novel MOR-selective phenylmorphans with high-to-low MOR efficacy.Pharmacology research & perspectives · 2023Article
- A MOR Antagonist with High Potency and Antagonist Efficacy among Diastereomeric C9-Alkyl-SubstitutedMolecules (Basel, Switzerland) · 2023Article
- Discovery of a Potent Highly Biased MOR Partial Agonist among Diastereomeric C9-Hydroxyalkyl-5-phenylmorphans.Molecules (Basel, Switzerland) · 2023Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
14 authors at 6 institutions in 1 country.
Dana R ChambersDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892, USA.
Agnieszka SulimaDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892, USA.
Dan LuoDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 S. Limestone Street, Lexington, KY 40536, USA.
Thomas E PrisinzanoDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 S. Limestone Street, Lexington, KY 40536, USA.ORCID 0000-0002-0649-8052
Alexander GoldbergComputational Chemistry and Molecular Biophysics Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, 333 Cassell Drive, Baltimore, MD 21224, USA.
Bing XieComputational Chemistry and Molecular Biophysics Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, 333 Cassell Drive, Baltimore, MD 21224, USA.ORCID 0000-0002-1692-7199
Lei ShiComputational Chemistry and Molecular Biophysics Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, 333 Cassell Drive, Baltimore, MD 21224, USA.
Carol A ParonisMcLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.
Jack BergmanMcLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.
Nima NassehiDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, 1112 East Clay Street, Richmond, VA 23298, USA.
Dana E SelleyDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, 1112 East Clay Street, Richmond, VA 23298, USA.
Gregory H ImlerNaval Research Laboratory, Center for Biomolecular Science and Engineering, Washington, DC 20375, USA.
Arthur E JacobsonDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892, USA.ORCID 0000-0002-0011-8354
Kenner C RiceDrug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 9800 Medical Center Drive, Bethesda, MD 20892, USA.
National Institute on Drug Abuse · USNational Institutes of Health · USHarvard University · USUniversity of Kentucky · USVirginia Commonwealth University · USUnited States Naval Research Laboratory · US
Funding
Structural basis for the functions of dopamine receptors, neurotransmitter transporters, and sigma 1 receptorZIADA000606 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI SHI, LEI · 2015 to 2025
$20.5MVCU Center for Drug Addiction ResearchP30DA033934 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI Matthew Sean Halquist · 2014 to 2026
$13.8MDevelopment of Agents for Synthetic Opioid OverdoseU01DA051377 · NIDA · UNIVERSITY OF KENTUCKY · PI PRISINZANO, THOMAS EDWARD · 2021 to 2023
$1.4MIn vivo characterization of opioid biased agonistsR01DA047574 · NIDA · MCLEAN HOSPITAL · PI BERGMAN, JACK, PARONIS, CAROL A · 2019 to 2021
$809kBRIDGING THE DISCONNECTN01DA001101 · NIDA · MANAGEMENT ASSISTANCE CORPORATION · PI FISCHER, GLENN · 2000 to 2000
$322kIntramural NIH HHS ZIA DA000606NIDA NIH HHS DA047574NIDA NIH HHS DA051377NIDA NIH HHS P30 DA033934NIDA NIH HHS P30-DA033934NIDA NIH HHS R01 DA047574NIDA NIH HHS T32-DA007024NIDA NIH HHS U01 DA051377NIDA NIH HHS Y1-DA1101
Abstract
Four sets of diastereomeric C9-alkenyl 5-phenylmorphans, varying in the length of the C9-alkenyl chain, were designed to examine the effect of these spatially distinct ligands on opioid receptors. Functional activity was obtained by forskolin-induced cAMP accumulation assays and several compounds were examined in the [
Indexed as
NaltrexoneRespiratory InsufficiencyAnimalsCHO CellsColforsinCricetinaeLigandsMiceMorphineReceptors, OpioidReceptors, Opioid, deltaReceptors, Opioid, muColforsinLigandsMorphineNaltrexoneReceptors, OpioidReceptors, Opioid, deltaReceptors, Opioid, muactive (6DDF) MOR crystal structuresdiastereomeric C9-alkenyl 5-phenylmorphansDORinactive (4DKL) MOR crystal structuresKOR agonists and antagonistsm-hydroxy-N-phenethyl-5-phenylmorphanmolecular modeling and simulationMORN-phenethyl-2-azabicyclo [3.3.1] nonan-5-yl) phenolsrespiratory depression
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LicenceCC BY
Read underepoch 390
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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.