ArticleACS chemical neuroscience2025
Synthesis and Pharmacology of a Morphinan-Derived Dual Mu-Kappa Opioid Receptor Agonist Analgesic.
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Article in ACS chemical neuroscience, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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2citing papers in PubMed
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Who cites it
2 citing papers in PubMed.
- Characterization of Novel Sigma Receptor Ligands Derived from Multicomponent Reactions as Efficacious Treatments for Neuropathic Pain.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Conformational Heterogeneity Underlying Divergent Signaling in Class A G Protein-Coupled Receptors.ACS pharmacology & translational science · 2025Review
Corrections and comments
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Authors and funding
31 authors.
Balazs R VargaCenter for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences & Pharmacy at St Louis, St Louis, Missouri 63110-1010, United States.
Rajendra UpretyDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.
Barnali PaulCenter for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences & Pharmacy at St Louis, St Louis, Missouri 63110-1010, United States.
Alexis KnollCenter for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences & Pharmacy at St Louis, St Louis, Missouri 63110-1010, United States.
Nokomis Ramos-GonzalezCenter for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences & Pharmacy at St Louis, St Louis, Missouri 63110-1010, United States.ORCID 0000-0002-9398-8956
Kevin AppourchauxCenter for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences & Pharmacy at St Louis, St Louis, Missouri 63110-1010, United States.
Tori TaylorCenter for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences & Pharmacy at St Louis, St Louis, Missouri 63110-1010, United States.
Bengisu TurgutalpCenter for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences & Pharmacy at St Louis, St Louis, Missouri 63110-1010, United States.ORCID 0000-0001-8507-5420
Ryosuke ShinouchiDepartment of Pharmacodynamics, University of Florida; Gainesville, Florida 32610, United States.
Shainnel O EansDepartment of Pharmacodynamics, University of Florida; Gainesville, Florida 32610, United States.
Ashai K WilliamsDepartment of Pharmacodynamics, University of Florida; Gainesville, Florida 32610, United States.
Steven G Vasquez-GrinnellDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.
Saheem ZaidiDepartment of Quantitative and Computational Biology, Department of Chemistry, Bridge Institute, University of Southern California, Los Angeles, California 90089-0001, United States.
Antonina L NazarovaDepartment of Quantitative and Computational Biology, Department of Chemistry, Bridge Institute, University of Southern California, Los Angeles, California 90089-0001, United States.
Andras VaradiDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.ORCID 0000-0001-5591-377X
Valerie Le RouzicDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.
Taylor G BrownLong Island University, Post Campus, Brookville, New York 11201-5301, United States.
Shani MartinezLong Island University, Post Campus, Brookville, New York 11201-5301, United States.
Michael AnsonoffDepartment of Neuroscience and Cell Biology, UMDNJ-Robert Wood Johnson Medical School, Piscataway, New Jersey 08901-1962, United States.
Rebecca Notis DardashtiDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.
Amanda HunkeleDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.
Joan SubrathDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.
Matthew WelchCenter for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences & Pharmacy at St Louis, St Louis, Missouri 63110-1010, United States.
Jin XuDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.
Grace C RossiLong Island University, Post Campus, Brookville, New York 11201-5301, United States.
John PintarDepartment of Neuroscience and Cell Biology, UMDNJ-Robert Wood Johnson Medical School, Piscataway, New Jersey 08901-1962, United States.
Gavril W PasternakDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.
Vsevolod KatritchDepartment of Quantitative and Computational Biology, Department of Chemistry, Bridge Institute, University of Southern California, Los Angeles, California 90089-0001, United States.ORCID 0000-0003-3883-4505
Jay P McLaughlinDepartment of Pharmacodynamics, University of Florida; Gainesville, Florida 32610, United States.
Ying Xian PanDepartment of Neurology and Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, New York 10065-6007, United States.
Susruta MajumdarCenter for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences & Pharmacy at St Louis, St Louis, Missouri 63110-1010, United States.ORCID 0000-0002-2931-3823
Funding
X-RAY CRYSTALLOGRAPHYP30CA008748 · NCI · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI SELWYN M VICKERS · 1985 to 2026
$347.4MStructure-Function of Opioid ReceptorsP01DA035764 · NIDA · UNIVERSITY OF SOUTHERN CALIFORNIA · PI CHEREZOV, VADIM, ROTH, BRYAN L. · 2014 to 2018
$7.1MSynthesis &Pharmacology of Novel Opiates and SystemsR01DA006241 · NIDA · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI PAN, YING-XIAN · 1990 to 2018
$6.4MCharacterizing exon 11 promoter of the mu opioid receptor gene, OPRMR01DA013997 · NIDA · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI PAN, YING-XIAN · 2002 to 2012
$3.3MTargeting the allosteric sodium site with novel probes for delta opioid receptorR01DA057790 · NIDA · WASHINGTON UNIVERSITY · PI Tao Che, VSEVOLOD KATRITCH · 2023 to 2026
$2.6MAlternative 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
$1.9MEfficacy and signaling modulation by targeting the sodium site at mu opioid receptorR01DA059978 · NIDA · WASHINGTON UNIVERSITY · PI Susruta Majumdar · 2024 to 2026
$1.8MComputational approaches to discover ligands with new chemotypes and functional propertiesR35GM153437 · NIGMS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI VSEVOLOD KATRITCH · 2024 to 2026
$899kAnalgesics targeting truncated 6transmembrane exon 11 variants of MOR-1 (6TM-E11)R33DA034106 · NIDA · SLOAN-KETTERING INST CAN RESEARCH · PI MAJUMDAR, SUSRUTA · 2014 to 2015
$596kAnalgesics targeting truncated 6transmembrane exon 11 variants of MOR-1 (6TM-E11)R21DA034106 · NIDA · SLOAN-KETTERING INST CAN RESEARCH · PI MAJUMDAR, SUSRUTA · 2012 to 2013
$443kNCI NIH HHS P30 CA008748NIDA NIH HHS P01 DA035764NIDA NIH HHS R01 DA006241NIDA NIH HHS R01 DA013997NIDA NIH HHS R01 DA042888NIDA NIH HHS R01 DA057790NIDA NIH HHS R01 DA059978NIDA NIH HHS R21 DA034106NIDA NIH HHS R33 DA034106NIGMS NIH HHS R35 GM153437
Abstract
We present the synthesis and pharmacological characterization of 3'-iodobenzoylamido epoxymorphinans, with a saturated ring C and devoid of 14-OH, based on a dihydronormorphine backbone with various
Indexed as
Analgesics, OpioidMorphinansReceptors, Opioid, kappaReceptors, Opioid, muAnimalsGuanosine 5'-O-(3-Thiotriphosphate)HumansMaleMiceMice, Inbred C57BLAnalgesics, OpioidGuanosine 5'-O-(3-Thiotriphosphate)MorphinansReceptors, Opioid, kappaReceptors, Opioid, mubiased agonismmiceopioidspartial agonism
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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.