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CR-4056

From Wikipedia, the free encyclopedia
Investigational analgesic drug
Pharmaceutical compound
CR-4056
Identifiers
  • 6-(1H-imidazol-1-yl)-2-phenylquinazoline
CAS Number
PubChemCID
ChemSpider
UNII
Chemical and physical data
FormulaC17H12N4
Molar mass272.311 g·mol−1
3D model (JSmol)
  • C1(C2=CC=CC=C2)=NC=C3C=C(N4C=CN=C4)C=CC3=N1
  • InChI=1S/C17H12N4/c1-2-4-13(5-3-1)17-19-11-14-10-15(6-7-16(14)20-17)21-9-8-18-12-21/h1-12H
  • Key:CSZGXYBGYFNSCO-UHFFFAOYSA-N

CR-4056 is ananalgesic drug candidate with a novel mechanism of action, acting as aligand for theimidazoline receptor I2. It showed promising results in animal studies against various types ofneuropathic pain, and has reached Phase II humanclinical trials as a potential treatment for pain associated withosteoarthritis.[1][2][3][4][5]

See also

[edit]

References

[edit]
  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. 69 (suppl 10). 2017 ACR/ARHP Annual Meeting, Abstract 1193.{{cite journal}}: CS1 maint: location (link)
IRTooltip Imidazoline receptor


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