JZL 184

Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA) are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid and glycerol, thus terminating its biological function. JZL 184 is a potent and selective inhibitor of monoacylglycerol lipase (MAGL) that displays IC₅₀ values of 8 nM and 4 µM for inhibition of MAGL and fatty acid amide hydrolase in mouse brain membranes, respectively.¹ When administered to mice at 16 mg/kg, intraperitoneally, JZL 184 reduces MAGL activity by 85%, elevates brain 2-AG levels by 8-fold, and elicits analgesic activity in a variety of pain assays that qualitatively mimics direct central cannabinoid (CB₁) agonists.¹

WARNING This product is not for human or veterinary use.

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Winters, N.D., Bedse, G., Astafyev, A.A., et al. Targeting diacylglycerol lipase reduces alcohol consumption in preclinical models. J. Clin. Invest. 146861 (2021).

Inazumi, T., Yamada, K., Shirata, N., et al. Prostaglandin E₂-EP₄ axis promotes lipolysis and fibrosis in adipose tissue leading to ectopic fat deposition and insulin resistance. Cell Rep. 33(2), 108265 (2020).

Soethoudt, M., Grether, U., Fingerle, J., et al. Cannabinoid CB₂ receptor ligand profiling reveals biased signalling and off-target activity. Nat. Commun. 8, 13958 (2017).