JTE-907

JTE-907 is a highly selective, orally active small molecule that acts as an inverse agonist at the cannabinoid CB2 receptor. It binds with high affinity to rat, mouse, and human CB2 receptors (Ki values of 0.38 nM for rat, 1.55 nM for mouse, and 35.9 nM for human) and displays strong selectivity over the central CB1 receptor[2][5]. In preclinical studies, JTE-907 exhibits anti-inflammatory effects in vivo by inhibiting carrageenin-induced paw edema in mice and suppressing itch-associated responses in models of atopic dermatitis[4][5]. Mechanistically, it increases forskolin-stimulated cAMP production in cells expressing CB2 receptors—consistent with inverse agonism—and can drive immune responses toward regulatory T cell phenotypes via p38 phosphorylation and STAT5A activation[6]. Additionally, JTE-907 has been shown to stimulate insulin secretion from pancreatic islets independently of GPR55 signaling and protect β-cells from cytokine-induced apoptosis while promoting β-cell proliferation[7][10]. The compound was developed by Japan Tobacco primarily as a research tool; there are no known brand names or clinical approvals.

Other names

N-(benzo[d][1,3]dioxol-5-ylmethyl)-7-methoxy-2-oxo-8-(pentyloxy)-1,2-dihydroquinoline-3-carboxamide