ArticleJournal of medicinal chemistry2013
Bivalent ligands that target μ opioid (MOP) and cannabinoid1 (CB1) receptors are potent analgesics devoid of tolerance.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
35 citing papers in PubMed, 79 citations in OpenAlex.
- Multivalent antibody-based conjugates as new tools for tailored modulation of G protein-coupled receptors.British journal of pharmacology · 2026Review
- The crosstalk between 5-HTNeuropharmacology · 2023Review
- Recent Advancement in Drug Design and Discovery of Pyrazole Biomolecules as Cancer and Inflammation Therapeutics.Molecules (Basel, Switzerland) · 2022Review
- Melanocortin-4 receptor complexity in energy homeostasis,obesity and drug development strategies.Diabetes, obesity & metabolism · 2022Review
- Fentanyl Structure as a Scaffold for Opioid/Non-Opioid Multitarget Analgesics.International journal of molecular sciences · 2022Review
- Novel bivalent ligands carrying potential antinociceptive effects by targeting putative mu opioid receptor and chemokine receptor CXCR4 heterodimers.Bioorganic chemistry · 2022Article
- Contributions of the International Narcotics Research Conference to Opioid Research Over the Past 50 years.Advances in drug and alcohol research · 2022Review
- An Effective and Safe Enkephalin Analog for Antinociception.Pharmaceutics · 2021Article
- Targeting Cannabinoid 1 and Delta Opioid Receptor Heteromers Alleviates Chemotherapy-Induced Neuropathic Pain.ACS pharmacology & translational science · 2019Article
- Article
- Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors.Journal of medicinal chemistry · 2019Article
- The size matters? A computational tool to design bivalent ligands.Bioinformatics (Oxford, England) · 2018Article
- A bivalent compound targeting CCR5 and the mu opioid receptor treats inflammatory arthritis pain in mice without inducing pharmacologic tolerance.Arthritis research & therapy · 2018Article
- Bivalent ligand MCC22 potently attenuates nociception in a murine model of sickle cell disease.Pain · 2018Article
- Heteromerization Modulates mu Opioid Receptor Functional PropertiesFrontiers in pharmacology · 2018Review
- Article
- Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors.Journal of enzyme inhibition and medicinal chemistry · 2017Article
- Intra-accumbal Cannabinoid Agonist Attenuated Reinstatement but not Extinction Period of Morphine-Induced Conditioned Place Preference; Evidence for Different Characteristics of Extinction Period and Reinstatement.Neurochemical research · 2017Article
- Basic/Translational Development of Forthcoming Opioid- and Nonopioid-Targeted Pain Therapeutics.Anesthesia and analgesia · 2017Review
- Orexin Receptor Multimerization versus Functional Interactions: Neuropharmacological Implications for Opioid and Cannabinoid Signalling and Pharmacogenetics.Pharmaceuticals (Basel, Switzerland) · 2017Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Given that μ opioid (MOP) and canabinoid (CB1) receptors are colocalized in various regions of the central nervous system and have been reported to associate as heteromer (MOP-CB1) in cultured cells, the possibility of functional, endogenous MOP-CB1 in nociception and other pharmacologic effects has been raised. As a first step in investigating this possibility, we have synthesized a series of bivalent ligands 1-5 that contain both μ agonist and CB1 antagonist pharmacophores for use as tools to study the functional interaction between MOP and CB1 receptors in vivo. Immunofluorescent studies on HEK293 cells coexpressing both receptors suggested 5 (20-atom spacer) to be the only member of the series that bridges the protomers of the heteromer. Antinociceptive testing in mice revealed 5 to be the most potent member of the series. As neither a mixture of monovalent ligands 9 + 10 nor bivalents 2-5 produced tolerance in mice, MOR-CB1 apparently is not an important target for reducing tolerance.
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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.