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CR-4056 structure.png
CAS Number
  • 1004997-71-0
PubChem CID
  • 24898732
Chemical and physical data
Formula C17H12N4
Molar mass 272.304 g/mol g·mol−1
3D model (JSmol)
  • Interactive image

CR-4056 is an analgesic drug candidate with a novel mechanism of action, acting as a ligand for the imidazoline receptor I2. It showed promising results in animal studies against various types of neuropathic pain, and has reached Phase II human clinical trials as a potential treatment for pain associated with osteoarthritis.[1] [2] [3] [4] [5]


  1. ^ Ferrari F, Fiorentino S, Mennuni L, Garofalo P, Letari O, Mandelli S, Giordani A, Lanza M, Caselli G (2011). "Analgesic efficacy of CR4056, a novel imidazoline-2 receptor ligand, in rat models of inflammatory and neuropathic pain". Journal of Pain Research. 4: 111–25. doi:10.2147/JPR.S18353. PMC 3100226. PMID 21647215.
  2. ^ Li JX, Thorn DA, Qiu Y, Peng BW, Zhang Y (March 2014). "Antihyperalgesic effects of imidazoline I(2) receptor ligands in rat models of inflammatory and neuropathic pain". British Journal of Pharmacology. 171 (6): 1580–90. doi:10.1111/bph.12555. PMC 3954494. PMID 24329196.
  3. ^ Comi E, Lanza M, Ferrari F, Mauri V, Caselli G, Rovati LC (May 4, 2017). "Efficacy of CR4056, a first-in-class imidazoline-2 analgesic drug, in comparison with naproxen in two rat models of osteoarthritis". Journal of Pain Research. 10: 1033–1043. doi:10.2147/JPR.S132026. PMC 5422496. PMID 28496359.
  4. ^ Li JX (October 2017). "2 receptors: An update". Pharmacology & Therapeutics. 178: 48–56. doi:10.1016/j.pharmthera.2017.03.009. PMC 5600648. PMID 28322973.
  5. ^ Rovati LC, Brambilla N, Blicharski T, Probert NJ, Vitalini C, Giacovelli G, Girolami F, D'Amato M (2017). "A Randomized, Placebo-Controlled, Double-Blind, Phase II Clinical Trial of the First-in-Class Imidazoline-2 Receptor Ligand CR4056 in Pain from Knee Osteoarthritis and Disease Phenotypes". Arthritis Rheumatol. 2017 ACR/ARHP Annual Meeting, Abstract 1193. 69 (suppl 10).CS1 maint: location (link)
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