4-Quinolone-3-Carboxamide CB2 Ligand

Uses

CB2 receptor antagonist 5 (compound 4A) is a ligand of CB2 receptor with antagonist effect[1].

Definition

ChEBI: 4-Quinolone-3-Carboxamide CB2 Ligand is a member of quinolines.

Biological Activity

ki: 0.6 nm4-quinolone-3-carboxamide cb2 ligand is a ligand of the cb2 receptor.cannabinoids (cbs) and their synthetic analogs exhibit biochemical and pharmacological effects via interacting with the central cb1 and peripheral cb2 receptors. the cb2 receptor has emerged as a pharmacological target for treating osteoporosis, and for eliciting antinociceptive effects in various pain models .

in vitro

previous study found that 4-quinolone-3-carboxamide cb2 ligand was a selective, high-affinity ligand of the cb2 receptor, displaying an in vitro ki values of 0.6 nm for cb2 and over 10,000 nm for cb1 [1].

in vivo

in animal study, it was found that 4-quinolone-3-carboxamide cb2 ligand at a dose of 6 mg/kg showed antinociceptive activity in a formalin test of nocifensive response in mice. moreover, such analgesic affect could not be significantly reversed by the cb2 antagonist am630 treatment, which suggested that 4-quinolone-3-carboxamide cb2 ligand might behave as an inverse agonist [1].

References

[1] s. pasquini, m. de rosa, v. pedani, 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. journal of medicinal chemistry 54, 5444-5453 (2011).

Raw materials

Preparation Products