ChemicalBook CAS DataBase List 1048039-15-1

1048039-15-1

Name	COR 170
CAS	1048039-15-1
Molecular Formula	C31H36N2O2
MDL Number	MFCD27991277
Molecular Weight	468.63
MOL File	1048039-15-1.mol

Chemical Properties

storage temp.	Store at RT
solubility	Soluble to 100 mM in ethanol and to 20 mM in DMSO
form	Powder

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Description

Selective inverse agonist of CB2 receptors (Ki values are 3.8 and >10,000 nM for CB2 and CB1, respectively).

Uses

COR170 (11u) is a selective CB2 inverse-agonist which is a 4-quinolone-3-carboxylic acid derivative with a Ki value of 3.8 nM for CB2 receptor. COR170 can be used for the research of inflammation and neuroprotection[1][2][3].

in vivo

COR170 (11u) (1.5-6 mg/kg; i.p, once) reduces the late phase nociceptive behaviour induced by formalin^[3].

Animal Model:	Mice with formalin (1.25%, 30 μL) injections^[3]
Dosage:	1.5, 3 and 6 mg/kg
Administration:	Intraperitoneal injection; 1.5, 3 and 6 mg/kg for once
Result:	Reduced the late phase nociceptive behaviour induced by formalin with a 6 mg/kg dose and 10 min before formalin and abolished the analgesic effect from GW405833 which is a CB₂ receptor partial agonist.

storage

Store at RT

References

[1] Contartese A, et al. A novel CB2 agonist, COR167, potently protects rat brain cortical slices against OGD and reperfusion injury. Pharmacol Res. 2012 Dec;66(6):555-63. DOI:10.1016/j.phrs.2012.08.003
[2] Pasquini S, et al. Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo. J Med Chem. 2008 Aug 28;51(16): DOI:10.1021/jm800552f
[3] Cascio MG, et al. In vitro and in vivo pharmacological characterization of two novel selective cannabinoid CB(2) receptor inverse agonists. Pharmacol Res. 2010 Apr;61(4):349-54. DOI:10.1016/j.phrs.2009.11.011

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