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Items: 16


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.


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.


Diet-induced mouse model of fatty liver disease and nonalcoholic steatohepatitis reflecting clinical disease progression and methods of assessment.

Clapper JR, Hendricks MD, Gu G, Wittmer C, Dolman CS, Herich J, Athanacio J, Villescaz C, Ghosh SS, Heilig JS, Lowe C, Roth JD.

Am J Physiol Gastrointest Liver Physiol. 2013 Oct 1;305(7):G483-95. doi: 10.1152/ajpgi.00079.2013. Epub 2013 Jul 25.


Effects of amylin and bupropion/naltrexone on food intake and body weight are interactive in rodent models.

Clapper JR, Athanacio J, Wittmer C, Griffin PS, D'Souza L, Parkes DG, Roth JD.

Eur J Pharmacol. 2013 Jan 5;698(1-3):292-8. doi: 10.1016/j.ejphar.2012.11.010. Epub 2012 Nov 21.


2-arachidonoylglycerol signaling in forebrain regulates systemic energy metabolism.

Jung KM, Clapper JR, Fu J, D'Agostino G, Guijarro A, Thongkham D, Avanesian A, Astarita G, DiPatrizio NV, Frontini A, Cinti S, Diano S, Piomelli D.

Cell Metab. 2012 Mar 7;15(3):299-310. doi: 10.1016/j.cmet.2012.01.021.


Biphenyl-3-yl alkylcarbamates as fatty acid amide hydrolase (FAAH) inhibitors: steric effects of N-alkyl chain on rat plasma and liver stability.

Vacondio F, Silva C, Lodola A, Carmi C, Rivara S, Duranti A, Tontini A, Sanchini S, Clapper JR, Piomelli D, Tarzia G, Mor M.

Eur J Med Chem. 2011 Sep;46(9):4466-73. doi: 10.1016/j.ejmech.2011.07.021. Epub 2011 Jul 21.


Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism.

Clapper JR, Moreno-Sanz G, Russo R, Guijarro A, Vacondio F, Duranti A, Tontini A, Sanchini S, Sciolino NR, Spradley JM, Hohmann AG, Calignano A, Mor M, Tarzia G, Piomelli D.

Nat Neurosci. 2010 Oct;13(10):1265-70. doi: 10.1038/nn.2632. Epub 2010 Sep 19.


A role for 2-arachidonoylglycerol and endocannabinoid signaling in the locomotor response to novelty induced by olfactory bulbectomy.

Eisenstein SA, Clapper JR, Holmes PV, Piomelli D, Hohmann AG.

Pharmacol Res. 2010 May;61(5):419-29. doi: 10.1016/j.phrs.2009.12.013. Epub 2010 Jan 5.


A second generation of carbamate-based fatty acid amide hydrolase inhibitors with improved activity in vivo.

Clapper JR, Vacondio F, King AR, Duranti A, Tontini A, Silva C, Sanchini S, Tarzia G, Mor M, Piomelli D.

ChemMedChem. 2009 Sep;4(9):1505-13. doi: 10.1002/cmdc.200900210.


Structure-property relationships of a class of carbamate-based fatty acid amide hydrolase (FAAH) inhibitors: chemical and biological stability.

Vacondio F, Silva C, Lodola A, Fioni A, Rivara S, Duranti A, Tontini A, Sanchini S, Clapper JR, Piomelli D, Mor M, Tarzia G.

ChemMedChem. 2009 Sep;4(9):1495-504. doi: 10.1002/cmdc.200900120.


Fatty acid amide hydrolase inhibition heightens anandamide signaling without producing reinforcing effects in primates.

Justinova Z, Mangieri RA, Bortolato M, Chefer SI, Mukhin AG, Clapper JR, King AR, Redhi GH, Yasar S, Piomelli D, Goldberg SR.

Biol Psychiatry. 2008 Dec 1;64(11):930-7. doi: 10.1016/j.biopsych.2008.08.008. Epub 2008 Sep 23.


The endocannabinoid system as a target for the treatment of cannabis dependence.

Clapper JR, Mangieri RA, Piomelli D.

Neuropharmacology. 2009;56 Suppl 1:235-43. doi: 10.1016/j.neuropharm.2008.07.018. Epub 2008 Jul 19. Review.


Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.

Mor M, Lodola A, Rivara S, Vacondio F, Duranti A, Tontini A, Sanchini S, Piersanti G, Clapper JR, King AR, Tarzia G, Piomelli D.

J Med Chem. 2008 Jun 26;51(12):3487-98. doi: 10.1021/jm701631z. Epub 2008 May 29. Erratum in: J Med Chem. 2009 Jan 8;52(1):224.


URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices.

King AR, Duranti A, Tontini A, Rivara S, Rosengarth A, Clapper JR, Astarita G, Geaga JA, Luecke H, Mor M, Tarzia G, Piomelli D.

Chem Biol. 2007 Dec;14(12):1357-65.


Identification of a bioactive impurity in a commercial sample of 6-methyl-2-p-tolylaminobenzo[d][1,3]oxazin-4-one (URB754).

Tarzia G, Antonietti F, Duranti A, Tontini A, Mor M, Rivara S, Traldi P, Astarita G, King A, Clapper JR, Piomelli D.

Ann Chim. 2007 Sep;97(9):887-94.


The fatty-acid amide hydrolase inhibitor URB597 does not affect triacylglycerol hydrolysis in rat tissues.

Clapper JR, Duranti A, Tontini A, Mor M, Tarzia G, Piomelli D.

Pharmacol Res. 2006 Nov;54(5):341-4. Epub 2006 Jun 29.

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