Description
JTE-907 is a selective peripheral cannabinoid (CB
2) receptor agonist with K
d values of 25 and 2,370, 1.55 and 1,060, and 0.38 and 1,050 nM for human, mouse, and rat CB
2 and CB
1 receptors, respectively. It increases forskolin-stimulated cAMP production in CHO cells expressing human and mouse CB
2 in a dose-dependent manner.
In vivo, JTE-907 inhibits carrageenin-induced edema in mouse paws with an ED
50 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
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.
