WOBE437

WOBE437 is a potent endocannabinoid uptake inhibitor with IC₅₀ values of 10 and 283 nM for arachidonoyl ethanolamide (AEA; Item No. 90050) and 2-arachidonoyl glycerol (2-AG; Item No. 62160) uptake, respectively, in U937 cells.¹ It is greater than 1,000-fold selective for endocannabinoid transporters over fatty acid amide hydrolase (FAAH; Item No. 10010183) and the 2-AG hydrolyzing enzymes MAGL, ABHD6, and ABHD12. WOBE437 inhibits AEA uptake in FAAH-deficient HMC-1 human mast cells and Neuro2a mouse neuroblastoma cells (IC₅₀s = 137 and 55 nM, respectively) and reduces AEA uptake by 50% in rat cortical neurons when used at a concentration of 1 μM. It also reduces 2-AG uptake by 40% in Neuro2a cells at a concentration of 5 μM. In vivo, WOBE437 increases AEA and 2-AG levels by 1.5-fold in mouse brain but not peripheral tissues after intraperitoneal administration of a 10 mg/kg dose for seven days. WOBE437 (10 mg/kg) also induces a typical tetrad of hypothermia, catalepsy, analgesia, and hypomotility in mice, indicating it also acts as an indirect cannabinoid (CB) receptor 1 agonist.

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1. Chicca, A., Nicolussi, S., Bartholomäus, R., et al. Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake. Proc. Natl. Acad. Sci. USA 114(25), E5006-E5015 (2017).