ArticleJournal of medicinal chemistry2023
Structure-Activity Relationship Study of Cannabidiol-Based Analogs as Negative Allosteric Modulators of the μ-Opioid Receptor.
Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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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
10 citing papers in PubMed, 19 citations in OpenAlex.
- Does Kappa Agonism Improve Reversal of 'Tranq-Dope' Overdose? Evidence from a Rodent Model.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Cannabidiol and other non-psychotropic cannabinoids from Cannabis sativa as therapeutics for microglial-mediated neuroinflammation and neurodegeneration.Journal of cannabis research · 2026Review
- The Pharmacological Profile of Plant-Derived Cannabinoids In Vitro.Current topics in behavioral neurosciences · 2026Review
- Is Fentanyl Rebound an Intrinsic Feature of Naloxone Reversal?Pharmaceuticals (Basel, Switzerland) · 2025Article
- Advances in the structural understanding of opioid allostery.Trends in pharmacological sciences · 2025Review
- Analgesic and toxicological evaluation of cannabidiol-rich MoroccanOpen life sciences · 2025Article
- Proof of concept for high-dose Cannabidiol pretreatment to antagonize opioid induced persistent apnea in mice.Frontiers in neuroscience · 2025Article
- Advances, opportunities, and challenges in methods for interrogating the structure activity relationships of natural products.Natural product reports · 2024Review
- CBD Versus CBDP: Comparing In Vitro Receptor-Binding Activities.International journal of molecular sciences · 2024Article
- Cannabidiol at Nanomolar Concentrations Negatively Affects Signaling through the Adenosine AInternational journal of molecular sciences · 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
7 authors at 1 institution in 1 country.
Funding
Abstract
The US faces an unprecedented surge in fatal drug overdoses. Naloxone, the only antidote for opiate overdose, competes at the mu opioid receptor (μOR) orthosteric site. Naloxone struggles against fentanyl-class synthetic opioids that now cause ∼80% of deaths. Negative allosteric modulators (NAMs) targeting secondary sites may noncompetitively downregulate μOR activation. (-)-Cannabidiol ((-)-CBD) is a candidate μOR NAM. To explore its therapeutic potential, we evaluated the structure-activity relationships among CBD analogs to identify NAMs with increased potency. Using a cyclic AMP assay, we characterize reversal of μOR activation by 15 CBD analogs, several of which proved more potent than (-)-CBD. Comparative docking investigations suggest that potent compounds interact with a putative allosteric pocket to stabilize the inactive μOR conformation. Finally, these compounds enhance naloxone displacement of fentanyl from the orthosteric site. Our results suggest that CBD analogs offer considerable potential for the development of next-generation antidotes for opioid overdose.
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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.