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HomeProduct name listJZL 184

JZL 184

Synonym(s):4-Nitrophenyl-4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate, Monoacylglycerol Lipase Inhibitor III, JZL184;MAGL Inhibitor III, JZL184 - CAS 1101854-58-3 - Calbiochem

JZL 184 Structural

What is JZL 184?

Description

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. 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.

The Uses of JZL 184

JZL 184 hydrate has been used as an inhibitor of monoacylglycerol lipase to study its effect on human osteoblast differentiation and proliferation and postsynaptic neurons.

The Uses of JZL 184

JZL184 is a strong and selective inhibitor of Monoglyceride Lipase.

What are the applications of Application

JZL 184 is an irreversible inhibitor of Monoglyceride Lipase (monoacylglycerol lipase, MAGL)

What are the applications of Application

JZL184 is a strong and selective inhibitor of Monoglyceride Lipase

Definition

ChEBI: 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]-1-piperidinecarboxylic acid (4-nitrophenyl) ester is a member of benzodioxoles.

Biochem/physiol Actions

JZL184 selectively inhibits MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). Anandamide and 2-AG are the two endogenous endocannabinoids that activate the cannabinoid receptors CB1 and CB2. Anandamide is predominantly metabolized by fatty acid amide hydrolase (FAAH), whereas monoacylglycerol lipase (MAGL) is thought to be the enzyme primarily responsible for the degradation of 2-AG. It is difficult to separate the activities of the two because most currently available inhibitors of MAGL are not selective, and also inhibit FAAH or other enzymes. JZL 184 is the first selective inhibitor of MAGL with nanomolar portency and over 200-fold selectivity for MAGL vs FAAH. When administered to mice, JZL184 increased levels of 2-arachidonoylglycerol in the brain by about 8-fold, with no effect on levels of anandamide.

storage

Store at -20°C

References

1) Long et al. (2009), Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects; Nat. Chem. Biol.,5 37 2) Pan et al. (2009), Blockade of 2-arachidonoylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxyl)methyl)piperidine-1-carboxylate (JZL 184) enhances retrograde endocannabinoid signaling; J. Pharmacol. Exp. Ther., 331 591 3) Kinsey et al. (2009), Blockade of endocannabinoid-degrading enzymes attenuates neuropathic pain; J. Pharmacol. Exp. Ther., 330 902

Properties of JZL 184

Melting point: 116-120°C
Boiling point: 706.4±60.0 °C(Predicted)
Density  1.467±0.06 g/cm3(Predicted)
storage temp.  2-8°C
solubility  Soluble in DMSO (up to 25 mg/ml).
form  White to off-white solid
pka 13.32±0.29(Predicted)
color  light yellow to yellow-green
Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months
CAS DataBase Reference 1101854-58-3

Safety information for JZL 184

Signal word Danger
Pictogram(s)
ghs
Skull and Crossbones
Acute Toxicity
GHS06
GHS Hazard Statements H301:Acute toxicity,oral
Precautionary Statement Codes P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

Computed Descriptors for JZL 184

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