JZL 184

Biological Activity

JZL 184 is a potent and selective MAGL inhibitor. Blocks hydrolysis of the endocannabinoid 2-arachidonyl glycerol (2-AG) in vivo in the mouse brain (IC₅₀ = 8 nM). Potentiates depolarization-induced suppression of excitability in cerebellar Purkinje neurons. Exhibits >300-fold selectivity for MAGL over FAAH in vitro. Attenuates nociception in neuropathic and inflammatory pain models. Also reduces free fatty acid levels in primary tumors.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. Repeated low-dose administration of the monoacylglycerol lipase inhibitor JZL184 retains cannabinoid receptor type 1-mediated antinociceptive and gastroprotective effects.
   Kinsey et al.
   J.Pharmacol.Exp.Ther., 2013;345:492
2. Dysregulated lipid metabolism in cancer.
   Zhang et al.
   World J.Biol.Chem., 2012;3:167
3. Selective blockade of 2-arachidonylglycerol hydrolysis produces cannabinoid behavioral effects.
   Long et al.
   Nat.Chem.Biol., 2009;5:37
4. Blockade of 2-arachidonylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184) enhances retrograde endocannabinoid signaling.
   Pan et al.
   J.Pharm.Exp.Ther., 2009;331:591

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