COR 170

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].

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

COR170 (11u) (0-1 μM) inhibits CB2 receptor in HEK cell membranes[2]. Cell Viability Assay[2] Cell Line: HEK cells Concentration: 0-1 μM Incubation Time: Result: Possessed a Ki value of 3.8 nM for CB2 receptor in HEK cell membranes.

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<>sub receptor partial agonist.

[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.

[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):5075-84.

[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.