ArticleJournal of pain research2017
Efficacy of CR4056, a first-in-class imidazoline-2 analgesic drug, in comparison with naproxen in two rat models of osteoarthritis.
Article in Journal of pain research, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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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.
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Who cites it
14 citing papers in PubMed, 21 citations in OpenAlex.
- Pharmacology, Medicinal Chemistry, and Therapeutic Potential of Imidazoline Receptor Ligands.ChemMedChem · 2026Review
- Hydrogen sulphide modifies the therapeutic potential of bone marrow mesenchymal stem cells in an adjuvant-induced polyarthritis rat model through the mitigation of angiogenesis, ectopic lymphoid tissue formation, and osteoclastogenesis.Inflammopharmacology · 2026Article
- Preconditioning of bone marrow mesenchymal stem cells with sodium hydrosulfide enhances their therapeutic potential in type II collagen-induced arthritis rat model.Naunyn-Schmiedeberg's archives of pharmacology · 2025Article
- A thermo-sensitive hydrogel targeting macrophage reprogramming for sustained osteoarthritis pain relief.Acta pharmaceutica Sinica. B · 2025Article
- Translational validity of quantitative sensory testing in chronic pain neuro-sensitization: guide of use and interpretation in osteoarthritis animal models.Frontiers in pain research (Lausanne, Switzerland) · 2025Review
- Early-stage knee OA induced by MIA and MMT compared in the murine model via histological and topographical approaches.Scientific reports · 2020Article
- Improved efficacy, tolerance, safety, and abuse liability profile of the combination of CR4056 and morphine over morphine alone in rodent models.British journal of pharmacology · 2020Article
- Understanding the Molecular Mechanisms Underlying the Pathogenesis of Arthritis Pain Using Animal Models.International journal of molecular sciences · 2020Review
- Recent advances in the treatment of osteoarthritis.F1000Research · 2020Review
- CR4056, a powerful analgesic imidazoline-2 receptor ligand, inhibits the inflammation-induced PKCε phosphorylation and membrane translocation in sensory neurons.British journal of pharmacology · 2020Article
- [Expression of KCNA2 in the dorsal root ganglia of rats with osteoarthritis pain induced by monoiodoacetate].Nan fang yi ke da xue xue bao = Journal of Southern Medical University · 2019Article
- Behavioral and Cognitive Improvement Induced by Novel Imidazoline INeurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2019Article
- What is new in pain modification in osteoarthritis?Rheumatology (Oxford, England) · 2018Review
- Monosodium iodoacetate-induced monoarthritis develops differently in knee versus ankle joint in rats.Neurobiology of pain (Cambridge, Mass.)Article
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Authors and funding
6 authors at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeCR4056, (2-phenyl-6-(1H-imidazol-1yl) quinazoline), an imidazoline-2 (I2) receptor ligand, is a promising analgesic drug that has been reported to be effective in several animal models of pain. The aim of this study was to evaluate the effects of CR4056 in two well-established rat models of osteoarthritis (OA), mimicking the painful and structural components of human OA.
methodsKnee OA was induced either by single intra-articular injection of monoiodoacetate (MIA) or by medial meniscal tear (MMT) in the right knee of male rats. In the MIA model, allodynia and hyperalgesia were measured as paw withdrawal threshold to mechanical stimulation. In the MMT model, pain behavior was analyzed as weight-bearing asymmetry (i.e. difference in hind paw weight distribution, HPWD) between the injured and the contralateral limbs.
resultsAcute oral administration of CR4056, 14 days after MIA injection, significantly and dose-dependently reduced allodynia and hyperalgesia 90 minutes after treatment, whereas acute naproxen administration significantly reduced allodynia but not hyperalgesia. After 7 days of repeated treatment, both CR4056 and naproxen showed significant anti-allodynic and anti-hyperalgesic effects in the MIA model. Rats undergoing MMT surgery developed a significant and progressive asymmetry in HPWD compared with sham-operated animals. Repeated treatment with CR4056 significantly reduced the progression of the pain behavior, whereas naproxen had no effects.
conclusionThe data presented here show that the I2 ligand CR4056 could be a new effective treatment for OA pain. The compound is currently under Phase II clinical evaluation for this indication.
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