ArticleACS chemical neuroscience2024
In Vitro Functional Profiling of Fentanyl and Nitazene Analogs at the μ-Opioid Receptor Reveals High Efficacy for Gi Protein Signaling.
Article in ACS chemical neuroscience, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 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
15 citing papers in PubMed, 21 citations in OpenAlex.
- Preclinical pharmacology of N-pyrrolidino "nitazene" opioids appearing in nonmedical drug markets.The Journal of pharmacology and experimental therapeutics · 2026Article
- Emerging Insights into the Distinct Pharmacological Mechanisms of Buprenorphine.Journal of chemical information and modeling · 2026Article
- 5-Methyl etodesnitazene human metabolism: LC-ESIAnalytical and bioanalytical chemistry · 2026Article
- Slow Dissociation of Nitazenes from thebioRxiv : the preprint server for biology · 2026Article
- Article
- Quantum Chemical Exploration of Fentanyl and Its Analogs: Conformational Landscapes and Energetics in Solution.ACS omega · 2025Article
- The nitazene epidemic in Estonia: a first report.European journal of public health · 2025Article
- Membrane Permeability Drives the Extreme Potency of Fentanyl but not Isotonitazene.bioRxiv : the preprint server for biology · 2025Article
- Identification of the Novel Synthetic Opioid N-Pyrrolidino Isotonitazene at an Australian Drug Checking Service.Drug testing and analysis · 2025Article
- Nitazenes: The Emergence of a Potent Synthetic Opioid Threat.Molecules (Basel, Switzerland) · 2025Review
- A putative binding model of nitazene derivatives at the μ-opioid receptor.Neuropharmacology · 2025Article
- Structural Determinants of Buprenorphine Partial Agonism at the μ-Opioid Receptor.Journal of chemical information and modeling · 2025Article
- Fentanyl-Antibody Interaction as a Novel Strategy against Opiates and Opioids Abuse.Journal of medicinal chemistry · 2025Review
- Characterization of novel nitazene recreational drugs: Insights into their risk potential from in vitro µ-opioid receptor assays and in vivo behavioral studies in mice.Pharmacological research · 2024Article
- In vitro structure-activity relationships and forensic case series of emerging 2-benzylbenzimidazole 'nitazene' opioids.Archives of toxicology · 2024Article
Corrections and comments
- Update ofThe2023
Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
Novel synthetic opioids (NSOs), including both fentanyl and non-fentanyl analogs that act as μ-opioid receptor (MOR) agonists, are associated with serious intoxication and fatal overdose. Previous studies proposed that G-protein-biased MOR agonists are safer pain medications, while other evidence indicates that low intrinsic efficacy at MOR better explains the reduced opioid side effects. Here, we characterized the in vitro functional profiles of various NSOs at the MOR using adenylate cyclase inhibition and β-arrestin2 recruitment assays, in conjunction with the application of the receptor depletion approach. By fitting the concentration-response data to the operational model of agonism, we deduced the intrinsic efficacy and affinity for each opioid in the Gi protein signaling and β-arrestin2 recruitment pathways. Compared to the reference agonist [d-Ala
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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.