JTE-907

JTE-907 is a cannabinoid 2 (CB₂) receptor inverse agonist.¹ It is selective for CB₂ over CB₁ receptors (K_is = 35.9 and 2,370 nM, respectively, for the human receptors). JTE-907 increases forskolin-induced cAMP production in CHO cells expressing human or mouse CB₂ receptors in a concentration-dependent manner. It promotes the differentiation of isolated mouse splenic CD4⁺ T cells into regulatory T cells (Tregs) when used at a concentration of 100 nM and decreases disease severity in a mouse model of inflammatory bowel disease (IBD) induced by dinitrobenzene sulfonic acid (DNBS).² JTE-907 (1 and 10 mg/kg) inhibits spontaneous scratching in a mouse model of chronic dermatitis, as well as reduces carrageenan-induced paw edema in mice (ED₅₀ = 0.05 mg/kg).^3,1 Bilateral injection of JTE-907 (25 pmol/animal) into the anterior bed nucleus of the stria terminalis decreases the percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiety-like behavior.⁴

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1. Iwamura, H., Suzuki, H., Ueda, Y., et al. In vitro and in vivo pharmacological characterization of JTE-907, a novel selection ligand for cannabinoid CB₂ receptor. J. Pharmacol. Exp. Ther. 296(2), 420-425 (2001).

2. Gentili, M., Ronchetti, S., Ricci, E., et al. 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. Pharmacol. Res. 141, 21-31 (2019).

3. Maekawa, T., Nojima, H., Kuraishi, Y., et al. The cannabinoid CB₂ receptor inverse agonist JTE-907 suppresses spontaneous itch-associated responses of NC mice, a model of atopic dermatitis. Euro. J. Pharmacol. 542(1-3), 179-183 (2006).

4. Gomes-de-Souza, L., Bianchi, P.C., Costa-Ferreira, W., et al. CB₁ and CB₂ receptors in the bed nucleus of the stria terminalis differently modulate anxiety-like behaviors in rats. Prog. Neuropsychopharmacol. Biol. Psychiatry 110, 110284 (2021).