KML29, an O-hexafluoroisopropyl (HFIP) carbamate analogue of JZL184. is a potent and orally active monoacylglycerol lipase (monoglyceride lipase; MAGL; MGLL; MGL) inhibitor (IC50 = 5.9/15/43 nM against human/mouse/rat MAGL) that targets MAGL active site with greatly improved selectivity (rat/mouse ABHD6 IC50 = 1.60/4.87; no inhibitory activity against human/rat/mouse fatty acid amide hydrolase (FAAH) up to 50 μM). KML29 in vivo treatment results in a selective upregulation of 2-arachidonoyl glycerol (2-AG), but not N-arachidonoyl-ethanolamine (AEA) in mice (brain Emax ∼20 mg/kg p.o. or i.p.; peripheral Emax ∼1 mg/kg p.o.) and rats (brain Emax ∼40 mg/kg i.p.). KML29 reduces inflammatory and neuropathic nociceptive behaviour in animal studies without cannabimimetic side effects seen with dual FAAH & MAGL inhibition, chronic administration, however, leads to CB1 receptor desensitization as observed with other MAGL inhibitors.
Orally active, potent and highly selective monoacylglycerol lipase (MAGL) inhibitor with in vivo analgesic efficacy without cannabimimetic side effects.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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British journal of pharmacology, 171(6), 1392-1407 (2013-07-16)
Since monoacylglycerol lipase (MAGL) has been firmly established as the predominant catabolic enzyme of the endocannabinoid 2-arachidonoylglycerol (2-AG), a great need has emerged for the development of highly selective MAGL inhibitors. Here, we tested the in vivo effects of one
British journal of pharmacology, 174(23), 4523-4539 (2017-10-01)
Gabapentin is commonly prescribed for nerve pain but may also cause dizziness, sedation and gait disturbances. Similarly, inhibition of the endogenous cannabinoid enzyme monoacylglycerol lipase (MAGL) has antinociceptive and anti-inflammatory properties but also induces sedation in mice at high doses.
Metabolic specialization among major brain cell types is central to nervous system function and determined in large part by the cellular distribution of enzymes. Serine hydrolases are a diverse enzyme class that plays fundamental roles in CNS metabolism and signaling.
The modulation of the brain endocannabinoid system has been identified as an option to treat neurodegenerative diseases including Parkinson's disease (PD). Especially the elevation of endocannabinoid levels by inhibition of hydrolytic degradation represents a valuable approach. To evaluate whether monoacylglycerol
Cannabinoids, such as Δ9-THC, act through an endogenous signaling system in the vertebrate eye that reduces IOP via CB1 receptors. Endogenous cannabinoid (eCB) ligand, 2-arachidonoyl glycerol (2-AG), likewise activates CB1 and is metabolized by monoacylglycerol lipase (MAGL). We investigated ocular
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