From Wikipedia, the free encyclopedia
Investigational analgesic drug
CR-4056
![](https://upload.wikimedia.org/wikipedia/commons/thumb/0/0f/CR-4056.svg/220px-CR-4056.svg.png) |
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6-(1H-imidazol-1-yl)-2-phenylquinazoline
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PubChem
CID | |
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UNII | |
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Formula | C17H12N4 |
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Molar mass | 272.311 g·mol−1 |
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3D model (
JSmol) | |
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C1(C2=CC=CC=C2)=NC=C3C=C(N4C=CN=C4)C=CC3=N1
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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
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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]
See also
References
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^ 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.
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^ 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.
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^ 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.
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^ 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.
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^ 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.
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