ArticleJournal of medicinal chemistry2020
Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.
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Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13citing papers in PubMed
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Who cites it
13 citing papers in PubMed, 30 citations in OpenAlex.
- Divergence in μ and δ opioid receptor pharmacology in neurons and antinociceptive efficacy in neuropathic pain: Insights from MP135 and CYM51010.British journal of pharmacology · 2026Article
- Activation of µ-δ Opioid Receptor Heteromer Attenuates Chemotherapy-Induced Neuropathic Pain in Mice.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2025Article
- Identification and Pharmacological Characterization of a Low-Liability Antinociceptive Bifunctional MOR/DOR Cyclic Peptide.Molecules (Basel, Switzerland) · 2023Article
- Activation of the Mu-Delta Opioid Receptor Heteromers Blocks Morphine Rewarding Effects.The international journal of neuropsychopharmacology · 2023Article
- Opioid signaling and design of analgesics.Progress in molecular biology and translational science · 2023Review
- G protein-coupled receptor-effector macromolecular membrane assemblies (GEMMAs).Pharmacology & therapeutics · 2022Review
- MOP and NOP receptor interaction: Studies with a dual expression system and bivalent peptide ligands.PloS one · 2022Article
- GPCR heteromers: An overview of their classification, function and physiological relevance.Frontiers in endocrinology · 2022Review
- Oxidative Metabolism as a Modulator of Kratom's Biological Actions.Journal of medicinal chemistry · 2021Article
- A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.Journal of medicinal chemistry · 2021Article
- Kratom Alkaloids as Probes for Opioid Receptor Function: Pharmacological Characterization of Minor Indole and Oxindole Alkaloids from Kratom.ACS chemical neuroscience · 2021Article
- Site selective C-H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy.Nature communications · 2021Article
- Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site.eLife · 2021Article
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Authors and funding
17 authors at 6 institutions in 1 country.
Abdelfattah FaouziCenter for Clinical Pharmacology, St Louis College of Pharmacy and Washington University, School of Medicine, St. Louis, Missouri 63110, United States.
Rajendra UpretyDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
Ivone GomesDepartment of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Nicolas MassalyDepartment of Anesthesiology, Washington University School of Medicine, St. Louis, Missouri 63110, United States.
Attila I KeresztesDepartment of Pharmacology, College of Medicine, University of Arizona, Tucson, Arkansas 85724, United States.
Valerie Le RouzicDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
Achla GuptaDepartment of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Tiffany ZhangDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
Hye Jean YoonDepartment of Anesthesiology, Washington University School of Medicine, St. Louis, Missouri 63110, United States.
Michael AnsonoffDepartment of Neuroscience and Cell Biology, Rutgers Robert Wood Johnson Medical School, Piscataway, New Jersey 08854, United States.
Abdullah AllaoaDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
Ying Xian PanDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
John PintarDepartment of Neuroscience and Cell Biology, Rutgers Robert Wood Johnson Medical School, Piscataway, New Jersey 08854, United States.
Jose A MorónDepartment of Anesthesiology, Washington University School of Medicine, St. Louis, Missouri 63110, United States.
John M StreicherDepartment of Pharmacology, College of Medicine, University of Arizona, Tucson, Arkansas 85724, United States.ORCID 0000-0002-4173-7362
Lakshmi A DeviDepartment of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.ORCID 0000-0002-2179-2874
Susruta MajumdarCenter for Clinical Pharmacology, St Louis College of Pharmacy and Washington University, School of Medicine, St. Louis, Missouri 63110, United States.ORCID 0000-0002-2931-3823
Memorial Sloan Kettering Cancer Center · USIcahn School of Medicine at Mount Sinai · USWashington University in St. Louis · USRutgers, The State University of New Jersey · USUniversity of Arizona · USUniversity of Health Sciences and Pharmacy · US
Funding
X-RAY CRYSTALLOGRAPHYP30CA008748 · NCI · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI Nicholas D Socci · 1985 to 2026
$347.4MTRAINING IN BEHAV. PHARMACOLOGY OF HUMAN DRUG DEPENDENCET32DA007242 · NIDA · UNIVERSITY OF VERMONT &ST AGRIC COLLEGE · PI HEIL, SARAH H, HIGGINS, STEPHEN T · 1990 to 2025
$8.2MEnzymes Involved in Neuropeptide Biosynthesis, Processing and RegulationR01NS026880 · NINDS · NEW YORK UNIVERSITY SCHOOL OF MEDICINE · PI DEVI, LAKSHMI A · 1994 to 2019
$6.5MSynthesis &Pharmacology of Novel Opiates and SystemsR01DA006241 · NIDA · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI PAN, YING-XIAN · 1990 to 2018
$6.4MRegulation Of Opioid Receptor Signaling by Endogenous PeptidesR01DA008863 · NIDA · NEW YORK UNIVERSITY SCHOOL OF MEDICINE · PI Lakshmi A Devi, Elyssa Margolis · 1995 to 2026
$6.1MPHARMACOLOGY OF OPIOID RECEPTOR SUBTYPESR01DA007242 · NIDA · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI PAN, YING-XIAN · 1991 to 2022
$6.0MPost-translational Regulation of Opioid and Cannabinoid Receptors.R37DA008863 · NIDA · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI DEVI, LAKSHMI A · 2012 to 2021
$4.6MChemistry and Biology of Mitragynine AlkaloidsR01DA046487 · NIDA · COLUMBIA UNIV NEW YORK MORNINGSIDE · PI MAJUMDAR, SUSRUTA, SAMES, DALIBOR · 2018 to 2022
$3.0MDissecting circuits mediating pain-induced alterations in motivated behaviorR01DA041781 · NIDA · WASHINGTON UNIVERSITY · PI MORON-CONCEPCION, JOSE A · 2017 to 2021
$2.3MNon-addictive Angiotensin AT2 inhibitors for neuropathic pain reliefUH3NS116929 · NINDS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI CHEREZOV, VADIM, KATRITCH, VSEVOLOD · 2021 to 2023
$1.9MAlternative pre-mRNA splicing of mu opioid receptor gene and mu opioid actionsR01DA042888 · NIDA · SLOAN-KETTERING INST CAN RESEARCH · PI PAN, YING-XIAN · 2017 to 2021
$1.9MRole of SK2 channels in morphine dependenceR01DA042499 · NIDA · WASHINGTON UNIVERSITY · PI MORON-CONCEPCION, JOSE A · 2017 to 2021
$1.9MNCI NIH HHS P30 CA008748NIAAA NIH HHS R21 AA026949NIDA NIH HHS R01 DA006241NIDA NIH HHS R01 DA007242NIDA NIH HHS R01 DA008863NIDA NIH HHS R01 DA041781NIDA NIH HHS R01 DA042499NIDA NIH HHS R01 DA042888NIDA NIH HHS R01 DA045463NIDA NIH HHS R01 DA046487NIDA NIH HHS R21 DA026880NIDA NIH HHS R21 DA034106NIDA NIH HHS R21 DA044509NIDA NIH HHS R21 DA045884NIDA NIH HHS R21 DA046714NIDA NIH HHS R33 DA045884NIDA NIH HHS R37 DA007242NIDA NIH HHS R37 DA008863NIDA NIH HHS R56 DA008863NIDA NIH HHS T32 DA007242NIDA NIH HHS UG3 DA047717NINDS NIH HHS R01 NS026880NINDS NIH HHS UG3 NS116929NINDS NIH HHS UH3 NS116929
Abstract
In this work, we studied a series of carfentanyl amide-based opioid derivatives targeting the mu opioid receptor (μOR) and the delta opioid receptor (δOR) heteromer as a credible novel target in pain management therapy. We identified a lead compound named
Indexed as
AnalgesicsAnimalsCell LineFentanylHumansMaleMiceMice, 129 StrainMice, Inbred C57BLMice, KnockoutPain MeasurementRatsRats, Long-EvansReceptors, Opioid, deltaAnalgesicscarfentanilFentanylReceptors, Opioid, delta
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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.