Description
JTE-907 is a selective peripheral cannabinoid (CB2) receptor agonist with Kd values of 25 and 2,370, 1.55 and 1,060, and 0.38 and 1,050 nM for human, mouse, and rat CB2 and CB1 receptors, respectively. It increases forskolin-stimulated cAMP production in CHO cells expressing human and mouse CB2 in a dose-dependent manner. In vivo, JTE-907 inhibits carrageenin-induced edema in mouse paws with an ED50 value of 0.05 mg/kg. JTE-907 also inhibits spontaneous scratching in a mouse model of chronic dermatitis at doses of 1 and 10 mg/kg.
Uses
Potent and selective ligands for cannabinoid type 2 receptors (CB2Rs) may have therapeutic potential for treating CB2Rs related inflammatory diseases (1). JTE 907 is a selective cannabinoid CB2 receptor inverse agonist with anti-inflammatory properties (2,3). Synthetic cannabinoids
Definition
ChEBI: N-(1,3-benzodioxol-5-ylmethyl)-7-methoxy-2-oxo-8-pentoxy-1H-quinoline-3-carboxamide is a member of quinolines and an aromatic amide.
Biological Activity
Highly selective cannabinoid CB 2 receptor inverse agonist. Binds with high affinity to rat, mouse and human CB 2 receptors (K i values are 0.38, 1.55 and 35.9 nM respectively). Produces anti-inflammatory effects in vivo .
Biochem/physiol Actions
JTE-907 is a cannabinoid CB2 ligand (inverse agonist). CB2 cannabanoid receptors are expressed in periferal nerves and other non CNS tissues, but are not expressed in the brain. CB2 is believed to have a role in nociceptive pain, but additional functions pertaining to the immune system have yet to be determined. CB2 selective agonists and antagonists provide a necessary tool for functional analyses.
