CB2 receptor agonist 2

CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2[1].

Research Areas >> Neurological Disease

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

CB2:8.5 nM (Ki)

CB2 receptor agonist 2 (compound 4g) (1  μM; 72 hours) has very low or no cytotoxicity to Hep-G2 cells[1]. Cell Proliferation Assay[1] Cell Line: Hep-G2 (Human hepatoblastoma) cells Concentration: 1  μM Incubation Time: 72 hours Result: Exhibited very low or no cytotoxicity to Hep-G2 cells.

CB2 receptor agonist 2 (compound 4g) (1 and 3 mg/kg; 1 hour) is very potent (with maximal effect being reached already at the 1 mg/kg dose) and has antihyperalgesic effects, efficacious also on the first phase of the nocifensive response and strongly reduced by AM630 (CB2-selective antagonist/inverse agonist) [1]. Animal Model: Formalin injection induces a biphasic stereotypical nocifensive behavior in mice[1] Dosage: Formalin (1.25% in saline, 30 μL), 1 and 3 mg/kg CB2 receptor agonist 2, 1 mg/kg AM630, monitor every 5 minutes for 1 hour Administration: Injection in the dorsal surface of one side of the hindpaw (Formalin), i.p. (CB2 receptor agonist, AM630) Result: Elicited antihyperalgesic effects and potent (with maximal effect being reached already at the 1 mg/kg dose) and efficacious, strongly reduced by AM630.

[1]. Pasquini S, et al. Investigations on the 4-quinolone-3-carboxylic acid motif. 4. Identification of new potent and selective ligands for the cannabinoid type 2 receptor with diverse substitution patterns and antihyperalgesic effects in mice. J Med Chem. 2011;54(15):5444-5453.