JZL 184
Chemical Name: 4-[Bis(1,3-benzodioxol-5-yl)hydroxymethyl]-1-piperidinecarboxylic acid 4-nitrophenyl ester
Purity: ≥98%
Biological Activity
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
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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 -
Dysregulated lipid metabolism in cancer.
Zhang et al.
World J.Biol.Chem., 2012;3:167 -
Selective blockade of 2-arachidonylglycerol hydrolysis produces cannabinoid behavioral effects.
Long et al.
Nat.Chem.Biol., 2009;5:37 -
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
Product Datasheets
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Citations for JZL 184
The citations listed below are publications that use Tocris products. Selected citations for JZL 184 include:
7 Citations: Showing 1 - 7
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Endocannabinoid Signaling Mediates Local Dendritic Coordination between Excitatory and Inhibitory Synapses.
Authors: Hu Et al.
Cell Rep 2019;27:666
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Cannabinoid CB1 Receptors Inhibit Gut-Brain Satiation Signaling in Diet-Induced Obesity.
Authors: Argueta Et al.
Front Physiol 2019;10:704
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Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex.
Authors: Martin Et al.
Stem Cells Dev 2015;9:457
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Inhibiting endocannabinoid biosynthesis: a novel approach to the treatment of constipation.
Authors: Bashashati Et al.
Br J Pharmacol 2015;172:3099
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Experimental cannabinoid 2 receptor-mediated immune modulation in sepsis.
Authors: Sardinha Et al.
Front Cell Neurosci 2014;2014:978678
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The inhibition of 2-arachidonoyl-glycerol (2-AG) biosynthesis, rather than enhancing striatal damage, protects striatal neurons from malonate-induced death: a potential role of cyclooxygenase-2-dependent metabolism of 2-AG.
Authors: Valdeolivas Et al.
Cell Death Dis 2013;4:e862
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CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release.
Authors: Malenczyk Et al.
J Biol Chem 2013;288:32685
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