JTE 907

JTE-907 is a selective peripheral cannabinoid (CB₂) 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 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.

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

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.

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 .

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.

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[1] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
[2] MARCO GENTILI . Selective CB2 inverse agonist JTE907 drives T cell differentiation towards a Treg cell phenotype and ameliorates inflammation in a mouse model of inflammatory bowel disease[J]. Pharmacological research, 2019, 141: Pages 21-31. DOI: 10.1016/j.phrs.2018.12.005
[3] TATSUYA MAEKAWA . The cannabinoid CB2 receptor inverse agonist JTE-907 suppresses spontaneous itch-associated responses of NC mice, a model of atopic dermatitis[J]. European journal of pharmacology, 2006, 542 1: Pages 179-183. DOI: 10.1016/j.ejphar.2006.05.040
[4] LUCAS GOMES-DE SOUZA . CB1 and CB2 receptors in the bed nucleus of the stria terminalis differently modulate anxiety-like behaviors in rats[J]. Progress in Neuro-Psychopharmacology & Biological Psychiatry, 2021, 110: Article 110284. DOI: 10.1016/j.pnpbp.2021.110284