Chemical Name: 4-[Bis(1,3-benzodioxol-5-yl)hydroxymethyl]-1-piperidinecarboxylic acid 4-nitrophenyl ester
Biological ActivityJZL 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Repeated low-dose administration of the monoacylglycerol lipase inhibitor JZL184 retains cannabinoid receptor type 1-mediated antinociceptive and gastroprotective effects.
Kinsey et al.
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.
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.
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
Endocannabinoid Signaling Mediates Local Dendritic Coordination between Excitatory and Inhibitory Synapses.
Authors: Hu Et al.
Cell Rep 2019;27:666
Cannabinoid CB1 Receptors Inhibit Gut-Brain Satiation Signaling in Diet-Induced Obesity.
Authors: Argueta Et al.
Front Physiol 2019;10:704
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
Inhibiting endocannabinoid biosynthesis: a novel approach to the treatment of constipation.
Authors: Bashashati Et al.
Br J Pharmacol 2015;172:3099
Experimental cannabinoid 2 receptor-mediated immune modulation in sepsis.
Authors: Sardinha Et al.
Front Cell Neurosci 2014;2014:978678
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
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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