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Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders.

Cisar JS, Weber OD, Clapper JR, Blankman JL, Henry CL, Simon GM, Alexander JP, Jones TK, Ezekowitz RAB, O'Neill GP, Grice CA.

J Med Chem. 2018 Oct 25;61(20):9062-9084. doi: 10.1021/acs.jmedchem.8b00951. Epub 2018 Aug 23.


Monoacylglycerol Lipase Inhibition in Human and Rodent Systems Supports Clinical Evaluation of Endocannabinoid Modulators.

Clapper JR, Henry CL, Niphakis MJ, Knize AM, Coppola AR, Simon GM, Ngo N, Herbst RA, Herbst DM, Reed AW, Cisar JS, Weber OD, Viader A, Alexander JP, Cunningham ML, Jones TK, Fraser IP, Grice CA, Ezekowitz RAB, O'Neill GP, Blankman JL.

J Pharmacol Exp Ther. 2018 Dec;367(3):494-508. doi: 10.1124/jpet.118.252296. Epub 2018 Oct 10.


Activity-Based Protein Profiling Delivers Selective Drug Candidate ABX-1431, a Monoacylglycerol Lipase Inhibitor, To Control Lipid Metabolism in Neurological Disorders.

Jiang M, van der Stelt M.

J Med Chem. 2018 Oct 25;61(20):9059-9061. doi: 10.1021/acs.jmedchem.8b01405. Epub 2018 Oct 11.


Peripheral antinociceptive effects of inhibitors of monoacylglycerol lipase in a rat model of inflammatory pain.

Guindon J, Guijarro A, Piomelli D, Hohmann AG.

Br J Pharmacol. 2011 Aug;163(7):1464-78. doi: 10.1111/j.1476-5381.2010.01192.x.


Increased tonic cannabinoid CB1R activity and brain region-specific desensitization of CB1R Gi/o signaling axis in mice with global genetic knockout of monoacylglycerol lipase.

Navia-Paldanius D, Aaltonen N, Lehtonen M, Savinainen JR, Taschler U, Radner FP, Zimmermann R, Laitinen JT.

Eur J Pharm Sci. 2015 Sep 18;77:180-8. doi: 10.1016/j.ejps.2015.06.005. Epub 2015 Jun 9.


O-hydroxyacetamide carbamates as a highly potent and selective class of endocannabinoid hydrolase inhibitors.

Niphakis MJ, Johnson DS, Ballard TE, Stiff C, Cravatt BF.

ACS Chem Neurosci. 2012 May 16;3(5):418-26. doi: 10.1021/cn200089j. Epub 2011 Oct 10.


Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.

Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, Beidler D, Liimatta MB, Smith SE, Dudley DT, Sadagopan N, Bhattachar SN, Kesten SJ, Nomanbhoy TK, Cravatt BF, Ahn K.

ACS Med Chem Lett. 2011 Feb 10;2(2):91-96.


N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases.

Otrubova K, Chatterjee S, Ghimire S, Cravatt BF, Boger DL.

Bioorg Med Chem. 2019 Apr 15;27(8):1693-1703. doi: 10.1016/j.bmc.2019.03.020. Epub 2019 Mar 11.


Selective monoacylglycerol lipase inhibitors: antinociceptive versus cannabimimetic effects in mice.

Ignatowska-Jankowska B, Wilkerson JL, Mustafa M, Abdullah R, Niphakis M, Wiley JL, Cravatt BF, Lichtman AH.

J Pharmacol Exp Ther. 2015 May;353(2):424-32. doi: 10.1124/jpet.114.222315. Epub 2015 Mar 11.


Comparative biochemical characterization of the monoacylglycerol lipase inhibitor KML29 in brain, spinal cord, liver, spleen, fat and muscle tissue.

Pasquarelli N, Porazik C, Hanselmann J, Weydt P, Ferger B, Witting A.

Neuropharmacology. 2015 Apr;91:148-56. doi: 10.1016/j.neuropharm.2014.12.001. Epub 2014 Dec 12.


Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2-arachidonoylglycerol.

Ghafouri N, Tiger G, Razdan RK, Mahadevan A, Pertwee RG, Martin BR, Fowler CJ.

Br J Pharmacol. 2004 Nov;143(6):774-84. Epub 2004 Oct 18.


Monoacylglycerol lipase (MGLL) polymorphism rs604300 interacts with childhood adversity to predict cannabis dependence symptoms and amygdala habituation: Evidence from an endocannabinoid system-level analysis.

Carey CE, Agrawal A, Zhang B, Conley ED, Degenhardt L, Heath AC, Li D, Lynskey MT, Martin NG, Montgomery GW, Wang T, Bierut LJ, Hariri AR, Nelson EC, Bogdan R.

J Abnorm Psychol. 2015 Nov;124(4):860-77. doi: 10.1037/abn0000079.


Endocannabinoids decrease neuropathic pain-related behavior in mice through the activation of one or both peripheral CB₁ and CB₂ receptors.

Desroches J, Charron S, Bouchard JF, Beaulieu P.

Neuropharmacology. 2014 Feb;77:441-52. doi: 10.1016/j.neuropharm.2013.10.006. Epub 2013 Oct 19.


Monoacylglycerol lipase inhibition by organophosphorus compounds leads to elevation of brain 2-arachidonoylglycerol and the associated hypomotility in mice.

Quistad GB, Klintenberg R, Caboni P, Liang SN, Casida JE.

Toxicol Appl Pharmacol. 2006 Feb 15;211(1):78-83. Epub 2005 Nov 28.


In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML29: antinociceptive activity without cannabimimetic side effects.

Ignatowska-Jankowska BM, Ghosh S, Crowe MS, Kinsey SG, Niphakis MJ, Abdullah RA, Tao Q, O' Neal ST, Walentiny DM, Wiley JL, Cravatt BF, Lichtman AH.

Br J Pharmacol. 2014 Mar;171(6):1392-407. doi: 10.1111/bph.12298.


The endocannabinoid hydrolysis inhibitor SA-57: Intrinsic antinociceptive effects, augmented morphine-induced antinociception, and attenuated heroin seeking behavior in mice.

Wilkerson JL, Ghosh S, Mustafa M, Abdullah RA, Niphakis MJ, Cabrera R, Maldonado RL, Cravatt BF, Lichtman AH.

Neuropharmacology. 2017 Mar 1;114:156-167. doi: 10.1016/j.neuropharm.2016.11.015. Epub 2016 Nov 25.


Development of a potent inhibitor of 2-arachidonoylglycerol hydrolysis with antinociceptive activity in vivo.

Bisogno T, Ortar G, Petrosino S, Morera E, Palazzo E, Nalli M, Maione S, Di Marzo V; Endocannabinoid Research Group.

Biochim Biophys Acta. 2009 Jan;1791(1):53-60. doi: 10.1016/j.bbalip.2008.10.007. Epub 2008 Nov 5.


Assay of Monoacylglycerol Lipase Activity.

Jung KM, Piomelli D.

Methods Mol Biol. 2016;1412:157-68. doi: 10.1007/978-1-4939-3539-0_17.


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