CR-4056

CR-4056
Identifiers
	IUPAC name 6-(1H-imidazol-1-yl)-2-phenylquinazoline;
CAS Number	1004997-71-0 ;
PubChem CID	24898732;
ChemSpider	28669340;
UNII	W9SQ1X2NPZ;
Chemical and physical data
Formula	C17H12N4
Molar mass	272.311 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1(C2=CC=CC=C2)=NC=C3C=C(N4C=CN=C4)C=CC3=N1;
	InChI 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 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]

References

^ 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.
^ 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.
^ 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.
^ 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.
^ 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)

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[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)

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v t e Imidazoline receptor modulators
IRTooltip Imidazoline receptor	Agonists: 2-BFI 7-Me-Marsanidine Agmatine Apraclonidine BU224 Clonidine Clorgyline Harmalas LNP-509 LNP-911 mCPP Moxonidine Rilmenidine S-23515 S-23757 Antagonists: BU99006 Efaroxan Idazoxan Unsorted/unknown: CR-4056 Pargyline
See also: Receptor/signaling modulators

See also

References