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| D PiomelliSummaryAffiliation: University of California Country: USA Publications
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Publications
Structural determinants for recognition and translocation by the anandamide transporterD Piomelli
The Neurosciences Institute, San Diego, CA 92121, USA
Proc Natl Acad Sci U S A 96:5802-7. 1999..These results outline the general structural requisites for anandamide transport and may assist in the development of selective inhibitors with potential clinical applications...
The element of surpriseDaniele Piomelli
Department of Pharmacology, MedSurge II, University of California, Irvine, California 92697-4625, USA
Nat Med 14:720-1. 2008- The endogenous cannabinoid system and the treatment of marijuana dependenceDaniele Piomelli
Department of Pharmacology, University of California, Irvine, Irvine, CA 92697 4625, USA
Neuropharmacology 47:359-67. 2004.... - The fat-induced satiety factor oleoylethanolamide suppresses feeding through central release of oxytocinSilvana Gaetani
Department of Physiology and Pharmacology V Erspamer, Sapienza University of Rome, 00185 Rome, Italy
J Neurosci 30:8096-101. 2010..The results suggest that OEA suppresses feeding by activating central oxytocin transmission... - The molecular logic of endocannabinoid signallingDaniele Piomelli
Department of Pharmacology, University of California, Irvine 92697-4625, USA
Nat Rev Neurosci 4:873-84. 2003 - A neuroscientist's guide to lipidomicsDaniele Piomelli
Department of Pharmacology, University of California, Irvine, California 92697, USA
Nat Rev Neurosci 8:743-54. 2007..The objective of neural lipidomics is to understand how these molecules work together; this difficult task will greatly benefit from technical advances that might enable the testing of emerging hypotheses... - The ligand that came from withinD Piomelli
Department of Pharmacology, 360 MSRII, University of California, Irvine, CA 92697 4625, USA
Trends Pharmacol Sci 22:17-9. 2001..Are these lipid-like second messengers the long-sought endogenous vanilloids?.. - Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597)Daniele Piomelli
Kadmus Pharmaceuticals, Inc Irvine, California 92697 4625, USA
CNS Drug Rev 12:21-38. 2006..The results suggest that KDS-4103 will offer a novel approach with a favorable therapeutic window for the treatment of anxiety, depression and pain... - The endocannabinoid system: a drug discovery perspectiveDaniele Piomelli
Department of Pharmacology, University of California, Irvine, CA 92697 4625, USA
Curr Opin Investig Drugs 6:672-9. 2005.... - Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptorsKwang Mook Jung
Department of Pharmacology, 3101 Gillespie NRF, University of California, Irvine, CA 92697 4625
Mol Pharmacol 68:1196-202. 2005..The results suggest that 2-AG is a primary endocannabinoid mediator of mGlu receptor-dependent neuronal plasticity... - The endocannabinoid system as a target for therapeutic drugsD Piomelli
University of California, Irvine, 92697 4625, USA
Trends Pharmacol Sci 21:218-24. 2000..Recent advances in the biochemistry and pharmacology of the endocannabinoid system in relation to the opportunities that this system offers for the development of novel therapeutic agents will be discussed... - The challenge of brain lipidomicsDaniele Piomelli
Department of Pharmacology, Center for the Neurobiology of Learning and Memory, University of California, Irvine, CA 92697 4625, USA
Prostaglandins Other Lipid Mediat 77:23-34. 2005..In this review, I outline several key features of brain lipid signaling and discuss the opportunities and challenges that such features impose on future lipidomic approaches... - Mechanisms of endocannabinoid inactivation: biochemistry and pharmacologyA Giuffrida
Department of Pharmacology, University of California, Irvine, California 92697 4625, USA
J Pharmacol Exp Ther 298:7-14. 2001..A more thorough characterization of the roles of endocannabinoids in health and disease will be necessary to define the significance of endocannabinoid inactivation mechanisms as targets for therapeutic drugs... - Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanismJason R Clapper
Department of Pharmacology, University of California Irvine, Irvine, California, USA
Nat Neurosci 13:1265-70. 2010..Brain-impenetrant FAAH inhibitors, which strengthen this gating mechanism, might offer a new approach to pain therapy... - Anandamide transport is independent of fatty-acid amide hydrolase activity and is blocked by the hydrolysis-resistant inhibitor AM1172D Fegley
Department of Pharmacology and Center for the Neurobiology of Learning and Memory, University of California, Irvine, CA 92697-4625, USA
Proc Natl Acad Sci U S A 101:8756-61. 2004..AM1172 may serve as a prototype for novel anandamide transport inhibitors with increased metabolic stability... - Receptor-dependent formation of endogenous cannabinoids in cortical neuronsN Stella
Department of Pharmacology, 360 Med Surge II, University of California, Irvine 92697-4625, USA
Eur J Pharmacol 425:189-96. 2001.... - Characterization of the fatty acid amide hydrolase inhibitor cyclohexyl carbamic acid 3'-carbamoyl-biphenyl-3-yl ester (URB597): effects on anandamide and oleoylethanolamide deactivationDarren Fegley
Department of Pharmacology, University of California, Irvine CA 92697-4625, USA
J Pharmacol Exp Ther 313:352-8. 2005..The results also suggest that an enzyme distinct from FAAH catalyzes OEA hydrolysis in the duodenum, where this lipid substance acts as a local satiety factor... - Modulation of anxiety through blockade of anandamide hydrolysisSatish Kathuria
Department of Pharmacology, University of California, Irvine, California, USA
Nat Med 9:76-81. 2003..Our results indicate that anandamide participates in the modulation of emotional states and point to fatty acid amide hydrolase inhibition as an innovative approach to anti-anxiety therapy... - Oleoylethanolamide stimulates lipolysis by activating the nuclear receptor peroxisome proliferator-activated receptor alpha (PPAR-alpha)Manuel Guzman
Department of Pharmacology, University of California, Irvine, CA 92697 4260, USA
J Biol Chem 279:27849-54. 2004..The results suggest that OEA stimulates fat utilization through activation of PPAR-alpha and that this effect may contribute to its anti-obesity actions... - Antidepressant-like activity of the fatty acid amide hydrolase inhibitor URB597 in a rat model of chronic mild stressMarco Bortolato
Department of Pharmacology, University of California, Irvine, California 92697 4260, USA
Biol Psychiatry 62:1103-10. 2007.... - The fatty-acid amide hydrolase inhibitor URB597 does not affect triacylglycerol hydrolysis in rat tissuesJason R Clapper
Center for Drug Discovery, University of California, Irvine, CA 92697, USA
Pharmacol Res 54:341-4. 2006..The results indicate that URB597, while potent at inhibiting FAAH, does not affect TGH and TGL activities in rat tissues... - Long-term plasticity of endocannabinoid signaling induced by developmental febrile seizuresKang Chen
Department of Anatomy and Neurobiology, University of California, Irvine, Irvine, CA 92697, USA
Neuron 39:599-611. 2003..These results demonstrate a selective, long-term increase in the gain of endocannabinoid-mediated retrograde signaling at GABAergic synapses in a model of a human neurological disease... - Elevated circulating levels of anandamide after administration of the transport inhibitor, AM404A Giuffrida
Department of Pharmacology, University of California, 360 Med Surge II, Irvine, CA 92697 4625, USA
Eur J Pharmacol 408:161-8. 2000..hydrochloride (SR141716A, 0.5 mg kg(-1), i.p). These results are consistent with the hypothesis that AM404 inhibits anandamide inactivation in vivo... - A critical cysteine residue in monoacylglycerol lipase is targeted by a new class of isothiazolinone-based enzyme inhibitorsA R King
Department of Pharmacology, University of California Irvine, Irvine, CA 92697 4625, USA
Br J Pharmacol 157:974-83. 2009..In the present study, we characterize the role of cysteines in MGL function and identify a series of cysteine-reactive agents that inhibit MGL activity with nanomolar potencies by interacting with cysteine residue 208... - Brain monoglyceride lipase participating in endocannabinoid inactivationT P Dinh
Department of Pharmacology, University of California, Irvine, CA 92697 4625, USA
Proc Natl Acad Sci U S A 99:10819-24. 2002..No such effect was observed on the accumulation of anandamide, another endocannabinoid lipid. The results suggest that hydrolysis by means of MGL is a primary mechanism for 2-AG inactivation in intact neurons... - Modulation of neuropathic and inflammatory pain by the endocannabinoid transport inhibitor AM404 [N-(4-hydroxyphenyl)-eicosa-5,8,11,14-tetraenamide]G La Rana
Department of Experimental Pharmacology, 3101 Gillespie NRF, University of California, Irvine, CA 92697-4625, USA
J Pharmacol Exp Ther 317:1365-71. 2006..The results provide new evidence for a role of the endocannabinoid system in pain modulation and point to anandamide transport as a potential target for analgesic drug development... - Anxiolytic-like properties of the anandamide transport inhibitor AM404Marco Bortolato
Department of Psychiatry and Human Behavior, Center for Drug Discovery, University of California, Irvine, CA 92697-4625, USA
Neuropsychopharmacology 31:2652-9. 2006..These results support a role of anandamide in the regulation of emotion and point to the anandamide transport system as a potential target for anxiolytic drugs... - Selective N-acylethanolamine-hydrolyzing acid amidase inhibition reveals a key role for endogenous palmitoylethanolamide in inflammationCarlos Solorzano
Department of Pharmacology, University of California, Irvine, CA 92697 4624, USA
Proc Natl Acad Sci U S A 106:20966-71. 2009..The PEA-hydrolyzing amidase NAAA may provide a previously undescribed target for antiinflammatory medicines... 
The endocannabinoid system as a target for novel anxiolytic and antidepressant drugsSilvana Gaetani
Department of Physiology and Pharmacology, Sapienza University of Rome, P le Aldo Moro 5, 00185 Rome, Italy
Int Rev Neurobiol 85:57-72. 2009....- Regulation of food intake by oleoylethanolamideJ Lo Verme
Department of Pharmacology, University of California, Irvine, California, 92697-4260, USA
Cell Mol Life Sci 62:708-16. 2005..Finally, we discuss the possible role of OEA as a peripheral satiety hormone... - Cannabinoid CB1 receptors and ligands in vertebrate retina: localization and function of an endogenous signaling systemA Straiker
Department of Neurosciences, University of California School of Medicine, San Diego, CA 92093, USA
Proc Natl Acad Sci U S A 96:14565-70. 1999.... - Endogenous cannabinoid signaling and psychomotor disordersA Giuffrida
Department of Pharmacology, University of California, 360 Med Surge II, Irvine, CA, USA
Prostaglandins Other Lipid Mediat 61:63-70. 2000..This mini-review discusses the participation of the endogenous cannabinoid system in the regulation of motor behaviors, pointing out its possible involvement in the pathophysiology of psychomotor disorders... - Oleoylethanolamide, an endogenous PPAR-alpha agonist, lowers body weight and hyperlipidemia in obese ratsJin Fu
Department of Psychiatry, University of California, Irvine, CA 92697 4625, USA
Neuropharmacology 48:1147-53. 2005..The results suggest that OEA regulates lipid metabolism and that this effect may contribute to its anti-obesity properties... - Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in miceJesse LoVerme
Department of Pharmacology, 360 MedScience II, University of California, Irvine, CA 92697 4625, USA
Bioorg Med Chem Lett 19:639-43. 2009..URB447 may provide a useful pharmacological tool for investigating the cannabinoid system, and might serve as a starting point for developing clinically viable CB(1) antagonists devoid of central side effects... - A role for endocannabinoids in viral-induced dyskinetic and convulsive phenomenaMarylou V Solbrig
Department of Neurology, 3226 Gillespie Neuroscience Research Bldg, University of California Irvine, Irvine, CA 92697 4292, USA
Exp Neurol 194:355-62. 2005.... - A key role for diacylglycerol lipase-alpha in metabotropic glutamate receptor-dependent endocannabinoid mobilizationKwang Mook Jung
Department of Pharmacology, University of California, Irvine, CA 92697 4625, USA
Mol Pharmacol 72:612-21. 2007..The findings indicate that DGL-alpha mediates group I mGlu receptor-induced 2-AG mobilization. They further suggest that the interaction of CC-Homer with DGL-alpha is necessary for appropriate function of this lipase... - Pharmacological characterization of hydrolysis-resistant analogs of oleoylethanolamide with potent anorexiant propertiesGiuseppe Astarita
Department of Pharmacology, 360 MSRII, University of California, Irvine, CA 92697-4625, USA
J Pharmacol Exp Ther 318:563-70. 2006..These results suggest that the endogenous high-affinity PPAR-alpha agonist OEA may provide a scaffold for the discovery of novel orally active PPAR-alpha ligands... - CD36 gene deletion decreases oleoylethanolamide levels in small intestine of free-feeding miceAna Guijarro
Department of Pharmacology, University of California, Irvine, CA 92697 4625, USA
Pharmacol Res 61:27-33. 2010..The results underscore the important role of CD36 in jejunal OEA production linked to feeding... - Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-alphaJin Fu
Department of Pharmacology, University of California, Irvine, California 92697 4625, USA
Nature 425:90-3. 2003..Our results, which show that OEA induces satiety by activating PPAR-alpha, identify an unexpected role for this nuclear receptor in regulating behaviour, and raise possibilities for the treatment of eating disorders... - Discovery of potent and reversible monoacylglycerol lipase inhibitorsAlvin R King
Department of Pharmacology, University of California Irvine, Irvine, CA 92697, USA
Chem Biol 16:1045-52. 2009..This previously unrecognized regulatory region might offer a molecular target for potent and reversible inhibitors of MGL... - Fat-induced satiety factor oleoylethanolamide enhances memory consolidationPatrizia Campolongo
Department of Pharmacology, University of California, Irvine, CA 92697 4625, USA
Proc Natl Acad Sci U S A 106:8027-31. 2009..The results indicate that OEA, acting as a PPAR-alpha agonist, facilitates memory consolidation through noradrenergic activation of the BLA, a mechanism that is also critically involved in memory enhancement induced by emotional arousal... - A role for monoglyceride lipase in 2-arachidonoylglycerol inactivationThien P Dinh
Department of Pharmacology, University of California, 360 Med Surge II, Irvine, CA 92697-4625, USA
Chem Phys Lipids 121:149-58. 2002..These results indicate that hydrolysis via MGL may be a primary route of 2-AG inactivation in intact neuronal cells... - The endocannabinoid system: a physiological perspective on its role in psychomotor controlA Giuffrida
Department of Pharmacology, University of California, 360 Med Surge II, Irvine, CA 92697 4625, USA
Chem Phys Lipids 108:151-8. 2000..The role of the endocannabinoids as modulators of psychomotor behaviors and the potential therapeutic perspectives deriving from the pharmacological manipulation of the endogenous cannabinoid system are also discussed... - Targeted lipidomics as a tool to investigate endocannabinoid functionGiuseppe Astarita
Department of Pharmacology, University of California, Irvine, California 92967, USA
Int Rev Neurobiol 85:35-55. 2009..Targeted lipidomics provides new opportunities for understanding endocannabinoid metabolism... - Rapid broad-spectrum analgesia through activation of peroxisome proliferator-activated receptor-alphaJesse LoVerme
Department of Pharmacology, Center for Drug Discovery, University of California, Irvine, CA 92697-4625, USA
J Pharmacol Exp Ther 319:1051-61. 2006..Our results suggest that PPAR-alpha agonists may represent a novel class of analgesics... - Food intake regulates oleoylethanolamide formation and degradation in the proximal small intestineJin Fu
Department of Pharmacology and Center for Drug Discovery, University of California, Irvine, California 92697, USA
J Biol Chem 282:1518-28. 2007..Collectively, these results indicate that nutrient availability controls OEA mobilization in the mucosa of the proximal intestine through a concerted regulation of OEA biosynthesis and degradation... - Oleoylethanolamide inhibits food intake in free-feeding rats after oral administrationFariba Oveisi
Department of Pharmacology, University of California, Irvine, CA 92697-4625, USA
Pharmacol Res 49:461-6. 2004..This effect is accompanied by a marked elevation in OEA levels in the small intestine, but not in brain or muscle... - A second generation of carbamate-based fatty acid amide hydrolase inhibitors with improved activity in vivoJason R Clapper
Departments of Pharmacology and Biological Chemistry, 360 MSRII, University of California, Irvine, Irvine, CA 92697, USA
ChemMedChem 4:1505-13. 2009..The results suggest that an approach balancing inhibitor reactivity with target recognition produces FAAH inhibitors that display significantly improved drug-likeness... - URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slicesAlvin R King
Department of Pharmacology, University of California, Irvine, Irvine, CA 92697, USA
Chem Biol 14:1357-65. 2007..Thus, URB602 may provide a useful tool by which to investigate the physiological roles of 2-AG and explore the potential interest of MGL as a therapeutic target... - Anandamide hydrolysis: a new target for anti-anxiety drugs?Silvana Gaetani
Department of Psychiatry, University of California, Irvine, CA 92697 4625, USA
Trends Mol Med 9:474-8. 2003..These findings suggest that anandamide contributes to the regulation of emotion and anxiety, and that FAAH might be the target for a novel class of anxiolytic drugs... - Identification of biosynthetic precursors for the endocannabinoid anandamide in the rat brainGiuseppe Astarita
Department of Pharmacology and Center for Drug Discovery, University of California, Irvine, CA 92967, USA
J Lipid Res 49:48-57. 2008..These results reveal a previously unrecognized preference of brain N-acyl transferase activity for polyunsaturated NArPE and provide new insights on the physiological regulation of anandamide biosynthesis... - The endocannabinoid system as a target for the treatment of cannabis dependenceJason R Clapper
Department of Pharmacology, University of California, Irvine 3101 Gillespie NRF, Irvine, CA 92697, USA
Neuropharmacology 56:235-43. 2009..In this article, we review evidence suggesting that (i) cannabis influences brain endocannabinoid signaling and (ii) FAAH inhibitors such as URB597 might offer a possible therapeutic avenue for the treatment of cannabis withdrawal... - Targeted enhancement of oleoylethanolamide production in proximal small intestine induces across-meal satiety in ratsJin Fu
Department of Pharmacology and Center for Drug Discovery, University of California, Irvine, California, USA
Am J Physiol Regul Integr Comp Physiol 295:R45-50. 2008.... - The search for the palmitoylethanolamide receptorJesse LoVerme
Center for Drug Discovery, University of California, Irvine, CA 92697-4260, USA
Life Sci 77:1685-98. 2005..Here we outline the history of PEA, starting with its initial discovery in the 1950s, and discuss the pharmacological properties of this compound, particularly in regards to its ability to activate PPAR-alpha... - RNA interference suggests a primary role for monoacylglycerol lipase in the degradation of the endocannabinoid 2-arachidonoylglycerolThien P Dinh
Department of Pharmacology, University of California, Irvine, 360 Med Surge II, Irvine, CA 92697, USA
Mol Pharmacol 66:1260-4. 2004.... - The nuclear receptor peroxisome proliferator-activated receptor-alpha mediates the anti-inflammatory actions of palmitoylethanolamideJesse Lo Verme
Department of Pharmacology, 360 MSRII, University of California, Irvine, CA 92697 4625, USA
Mol Pharmacol 67:15-9. 2005..These findings indicate that PPAR-alpha mediates the anti-inflammatory effects of PEA and suggest that this fatty-acid ethanolamide may serve, like its analog OEA, as an endogenous ligand of PPAR-alpha... - Modulation of meal pattern in the rat by the anorexic lipid mediator oleoylethanolamideSilvana Gaetani
Department of Pharmacology, University of California, Irvine, CA 92697-4625, USA
Neuropsychopharmacology 28:1311-6. 2003..These results suggest that OEA may participate in the regulation of satiety and may provide a chemical scaffold for the design of novel appetite-suppressing medications... - Effects of diet and behavioral enrichment on free fatty acids in the aged canine brainS Snigdha
Institute for Memory Impairments and Neurological Disorders, University of California Irvine, Irvine, CA, USA
Neuroscience 202:326-33. 2012..Together with data showing increased palmitoleic acid levels in AD patients, our data suggest that reducing palmitoleic acid levels and desaturation index in the brain may be associated with improved cognitive performance... - Lipidomic analysis of endocannabinoid metabolism in biological samplesGiuseppe Astarita
Department of Pharmacology, University of California, Irvine, CA 92967 4625, United States
J Chromatogr B Analyt Technol Biomed Life Sci 877:2755-67. 2009..Here, we review these new developments from the perspective of our laboratory's experience in the field... - An endocannabinoid signal associated with desire for alcohol is suppressed in recently abstinent alcoholicsRegina A Mangieri
Department of Pharmacology, University of California, Irvine, 3101 Gillespie NRF, Irvine, CA 92697, USA
Psychopharmacology (Berl) 205:63-72. 2009..Alcoholics report persistent alcohol craving that is heightened by cognitive cues, stressful situations, and abstinence. The role of endogenous cannabinoids in human alcohol craving--though long suspected--remains elusive... - Oleylethanolamide activates Ras-Erk pathway and improves myocardial function in doxorubicin-induced heart failureHou-Fen Su
Department of Medicine, University of California, Irvine, 92697, USA
Endocrinology 147:827-34. 2006..These findings suggest OEA is a novel cardioprotective compound that may be used to develop new strategies for the management of cardiomyopathy... - Enhancement of endocannabinoid signaling and the pharmacotherapy of depressionRegina A Mangieri
Department of Pharmacology and Center for Drug Discovery, The University of California, Irvine, CA 92697, USA
Pharmacol Res 56:360-6. 2007..This article will review these areas of research, highlighting the potential of endocannabinoid metabolism modulators as therapeutics for the treatment of depression... - Cerebrospinal anandamide levels are elevated in acute schizophrenia and are inversely correlated with psychotic symptomsAndrea Giuffrida
Department of Pharmacology, University of California, Irvine, CA, USA
Neuropsychopharmacology 29:2108-14. 2004..452, P = 0.001). The results suggest that anandamide elevation in acute paranoid schizophrenia may reflect a compensatory adaptation to the disease state... - Cold exposure stimulates synthesis of the bioactive lipid oleoylethanolamide in rat adipose tissueJesse LoVerme
Center for Drug Discovery, and Department of Pharmacology, University of California, Irvine, California 92697, USA
J Biol Chem 281:22815-8. 2006..Collectively, these results identify cold exposure as a natural stimulus for OEA formation in white fat and suggest a role for the sympathetic nervous system in regulating OEA biosynthesis... - Diacylglycerol lipase-alpha and -beta control neurite outgrowth in neuro-2a cells through distinct molecular mechanismsKwang Mook Jung
Department of Pharmacology, University of California, Irvine, California 92697 4625, USA
Mol Pharmacol 80:60-7. 2011..The findings further suggest that DGL-α and -β may regulate neurite outgrowth by engaging temporally and spatially distinct molecular pathways... - Proinflammatory stimuli control N-acylphosphatidylethanolamine-specific phospholipase D expression in macrophagesChenggang Zhu
Department of Biological Chemistry, University of California, Irvine, California, USA
Mol Pharmacol 79:786-92. 2011..Our findings suggest that proinflammatory stimuli suppress NAPE-PLD expression and PEA biosynthesis in macrophages and that this effect might contribute to the inflammatory response... - Synthesis and structure-activity relationships of N-(2-oxo-3-oxetanyl)amides as N-acylethanolamine-hydrolyzing acid amidase inhibitorsCarlos Solorzano
Department of Pharmacology, University of California, Irvine, 360 MSRII, Irvine, California 92697 4625, USA
J Med Chem 53:5770-81. 2010.... - Postprandial increase of oleoylethanolamide mobilization in small intestine of the Burmese python (Python molurus)Giuseppe Astarita
Dept. of Psychiatry and Human Behavior, Univ. of California, Irvine, CA, USA
Am J Physiol Regul Integr Comp Physiol 290:R1407-12. 2006.... - Increase of brain endocannabinoid anandamide levels by FAAH inhibition and alcohol abuse behaviours in the ratAndrea Cippitelli
Department of Experimental Medicine and Public Health, University of Camerino, Via Madonna delle Carceri, 62032 Camerino, Italy
Psychopharmacology (Berl) 198:449-60. 2008..As an alternative approach, CB1-receptor-mediated activity can be facilitated by increasing anandamide levels with the use of hydrolase fatty acid amide hydrolase (FAAH) inhibitors... - Selective inhibition of 2-AG hydrolysis enhances endocannabinoid signaling in hippocampusJudit K Makara
Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, 8. Szigony u. 43, Budapest, H-1083 Hungary
Nat Neurosci 8:1139-41. 2005..These results establish a role for 2-AG in synaptic plasticity and point to monoacylglycerol lipase as a possible drug target... - Endocannabinoid transport tightly controls 2-arachidonoyl glycerol actions in the hippocampus: effects of low temperature and the transport inhibitor AM404Norbert Hajos
Institute of Experimental Medicine, Hungarian Academy of Sciences, Szigony u 43, H 1083 Budapest, Hungary
Eur J Neurosci 19:2991-6. 2004.... - Inhibition of anandamide hydrolysis by cyclohexyl carbamic acid 3'-carbamoyl-3-yl ester (URB597) reverses abuse-related behavioral and neurochemical effects of nicotine in ratsMaria Scherma
Preclinical Pharmacology Section, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, Department of Health and Human Services, Baltimore, MD 21224, USA
J Pharmacol Exp Ther 327:482-90. 2008..These findings suggest that FAAH inhibition can counteract the addictive properties of nicotine and that FAAH may serve as a new target for development of medications for treatment of tobacco dependence... - The effect of cannabidiol and URB597 on conditioned gaping (a model of nausea) elicited by a lithium-paired context in the ratErin M Rock
Department of Psychology, University of Guelph, Guelph, ON, Canada
Psychopharmacology (Berl) 196:389-95. 2008..In this study, the effect of manipulation of the endocannabinoid (EC) system on a rat model of nausea (conditioned gaping) was determined... - Effects of levodopa on endocannabinoid levels in rat basal ganglia: implications for the treatment of levodopa-induced dyskinesiasBelen Ferrer
Fundacion Hospital Carlos Haya, 29010 Malaga, Spain
Eur J Neurosci 18:1607-14. 2003..These results indicate that a deficiency in endocannabinoid transmission may contribute to levodopa-induced dyskinesias and that these complications may be alleviated by activation of CB1 receptors... - Role of endogenous cannabinoids in synaptic signalingTamas F Freund
Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest 8, Szigony u 43, H 1083 Hungary
Physiol Rev 83:1017-66. 2003..Finally, the possible functions of endocannabinoids as retrograde synaptic signal molecules are discussed in relation to synaptic plasticity and network activity patterns... - Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitorsGiorgio Tarzia
Istituto di Chimica Farmaceutica e Tossicologica, , Piazza del Rinascimento 6, Italy
J Med Chem 46:2352-60. 2003..URB524 (N-cyclohexylcarbamic acid biphenyl-3-yl ester, 9g) is the most potent compound of the series (IC(50) = 63 nM) and was therefore selected for further optimization... - A peripheral mechanism for CB1 cannabinoid receptor-dependent modulation of feedingRaquel Gomez
University Institute of Drug Dependencies, Department of Psychobiology, University Complutense of Madrid, Madrid 28223, Spain
J Neurosci 22:9612-7. 2002..Pretreatment with SR141716A enhanced the inhibition of feeding induced by intraperitoneal administration of oleoylethanolamide. The results reveal an unexpected role for peripheral CB1 receptors in the regulation of feeding... - Attenuation of spontaneous opiate withdrawal in mice by the anandamide transport inhibitor AM404Ignacio del Arco
, Avda Carlos Haya 82. 7 Planta, , , Spain
Eur J Pharmacol 454:103-4. 2002..p.). These results suggest that spontaneous but not opioid antagonist-precipitated withdrawal is associated with dynamic changes in endogenous cannabinoid signaling... - Endogenous cannabinoids in patients with schizophrenia and substance use disorder during quetiapine therapyStephane Potvin
Fernand Seguin Research Center, Louis H Lafontaine Hospital and Biomedical Sciences Program, Faculty of Medicine, University of Montreal, Montreal, Quebec, Canada
J Psychopharmacol 22:262-9. 2008..Lastly, baseline anandamide predicted endpoint SUD scores (alcohol/ cannabis). Anandamide is a potential target for medications aimed at relieving SUD in schizophrenia... - Regulation of brain anandamide by acute administration of ethanolBelen Ferrer
Fundacion IMABIS, Hospital Carlos Haya, Malaga 29010, Spain
Biochem J 404:97-104. 2007..These results suggest that receptor-mediated release of acylethanolamide is inhibited by the acute administration of ethanol, and that this effect is not derived from increased fatty acid ethanolamide degradation... - Actions of the FAAH inhibitor URB597 in neuropathic and inflammatory chronic pain modelsAngelo Jayamanne
Pain Management Research Institute, Northern Clinical School, The University of Sydney, NSW, Australia
Br J Pharmacol 147:281-8. 2006..These findings suggest that the FAAH inhibitor URB597 produces cannabinoid CB1 and CB2 receptor-mediated analgesia in inflammatory pain states, without causing the undesirable side effects associated with cannabinoid receptor activation... - Synthesis and structure-activity relationships of FAAH inhibitors: cyclohexylcarbamic acid biphenyl esters with chemical modulation at the proximal phenyl ringGiorgio Tarzia
Istituto di Chimica Farmaceutica e Tossicologica, , Piazza del Rinascimento 6, 61029 Urbino, Italy
ChemMedChem 1:130-9. 2006..Derivatives with small polar groups at the para position of the proximal phenyl ring were slightly better FAAH inhibitors than the parent compound URB524... - Effects of the FAAH inhibitor, URB597, and anandamide on lithium-induced taste reactivity responses: a measure of nausea in the ratShelley K Cross Mellor
Department of Psychology, University of Guelph, Guelph, ON, Canada
Psychopharmacology (Berl) 190:135-43. 2007..Because of the rapid breakdown and hydrolysis of endocannabinoids, such as anandamide, the therapeutic effects may be enhanced by prolonging their duration of action... - The endogenous cannabinoid anandamide produces delta-9-tetrahydrocannabinol-like discriminative and neurochemical effects that are enhanced by inhibition of fatty acid amide hydrolase but not by inhibition of anandamide transportMarcello Solinas
Laboratoire de Biologie et Physiologie Cellulaires, CNRS 6187, Universite de Poitiers, Poitiers, France
J Pharmacol Exp Ther 321:370-80. 2007.... - The fatty acid amide hydrolase inhibitor URB597 (cyclohexylcarbamic acid 3'-carbamoylbiphenyl-3-yl ester) reduces neuropathic pain after oral administration in miceRoberto Russo
Department of Experimental Pharmacology, University of Naples, Italy
J Pharmacol Exp Ther 322:236-42. 2007..The results provide new evidence for a role of the endocannabinoid system in pain modulation and reinforce the proposed role of FAAH as a target for analgesic drug development... - Synergistic antinociception by the cannabinoid receptor agonist anandamide and the PPAR-alpha receptor agonist GW7647Roberto Russo
Department of Experimental Pharmacology, University of Naples, Naples, Italy
Eur J Pharmacol 566:117-9. 2007..These findings reveal a synergistic interaction between the endocannabinoid and PPAR-alpha systems that might be exploited clinically and identify a new pharmacological effect of the BK channel activator isopimaric acid... - Identification and functional characterization of brainstem cannabinoid CB2 receptorsMarja D Van Sickle
Institute of Infection, Immunity, and Inflammation and Hotchkiss Brain Institute, Department of Physiology and Biophysics, University of Calgary, Calgary, AB, Canada T2N 4N1
Science 310:329-32. 2005..CB2 receptors represent an alternative site of action of endocannabinoids that opens the possibility of nonpsychotropic therapeutic interventions using enhanced endocannabinoid levels in localized brain areas... - Molecular composition of the endocannabinoid system at glutamatergic synapsesIstvan Katona
Institute of Experimental Medicine, Hungarian Academy of Sciences, H 1083 Budapest, Hungary
J Neurosci 26:5628-37. 2006.... - The antinociceptive effects of local injections of propofol in rats are mediated in part by cannabinoid CB1 and CB2 receptorsJosee Guindon
Department of Pharmacology, Faculty of Medicine, Université de Montréal CHUM, Montreal, Quebec, Canada
Anesth Analg 104:1563-9, table of contents. 2007.... - Anandamide levels in cerebrospinal fluid of first-episode schizophrenic patients: impact of cannabis useF Markus Leweke
Department of Psychiatry and Psychotherapy, University of Cologne, Kerpener Str 62, 50924 Cologne, Germany
Schizophr Res 94:29-36. 2007..In the present study we examined whether cannabis use may alter such a mechanism... - An endocannabinoid mechanism for stress-induced analgesiaAndrea G Hohmann
Neuroscience and Behavior Program, Department of Psychology, The University of Georgia, Athens, Georgia 30602 3013, USA
Nature 435:1108-12. 2005..These studies also identify monoacylglycerol lipase as a previously unrecognized therapeutic target... - Role of the basolateral nucleus of the amygdala in endocannabinoid-mediated stress-induced analgesiaKatherine Connell
Neuroscience and Behavior Program, Department of Psychology, University of Georgia, Athens, GA 30602-3013, USA
Neurosci Lett 397:180-4. 2006..Our findings suggest that CB1 receptors in the BLA but not the CeA contribute to SIA, but pharmacological inhibition of endocannabinoid degradation at these sites does not affect the expression of stress antinociception... - The endogenous cannabinoid anandamide has effects on motivation and anxiety that are revealed by fatty acid amide hydrolase (FAAH) inhibitionMaria Scherma
Preclinical Pharmacology Section, Behavioral Neuroscience Research Branch, Intramural Research Program, National Institute on Drug Abuse, NIH, DHHS, Baltimore, MD, USA
Neuropharmacology 54:129-40. 2008..Thus, additive interactions between the effects of anandamide on brain reward processes and on anxiety may account for its aversive effects when intravenously administered during FAAH inhibition with URB597... - Tandem mass spectrometric data-FAAH inhibitory activity relationships of some carbamic acid O-aryl estersElisa Basso
CNR, Istituto di Scienze e Tecnologie Molecolari, Corso Stati Uniti 4, 35127 Padova, Italy
J Mass Spectrom 39:1450-5. 2004..797) with their FAAH-inhibitory activity. This indicates that the energetics of the C(O)--O bond cleavage may be relevant in explaining FAAH inhibition... - Correlation between energetics of collisionally activated decompositions, interaction energy and biological potency of carbamate FAAH inhibitorsGiovanni Valitutti
J Mass Spectrom 42:1624-7. 2007 - Endocannabinoids at the spinal level regulate, but do not mediate, nonopioid stress-induced analgesiaRichard L Suplita
Neuroscience and Behavior Program, Department of Psychology, University of Georgia, Baldwin Street, Athens, GA 30602-3013, USA
Neuropharmacology 50:372-9. 2006..Our results suggest that endocannabinoids in the spinal cord regulate, but do not mediate, nonopioid SIA... - Release of fatty acid amides in a patient with hemispheric stroke: a microdialysis studyWolf R Schabitz
Department of Neurology, University of Heidelberg, Heidelberg, Germany
Stroke 33:2112-4. 2002..We therefore studied release of FAEs such as anandamide, palmitylethanolamide (PEA), and oleylethanolamide (OEA) in the brain of a patient suffering from malignant hemispheric infarction treated with hypothermia... - N-Acylethanolamines in human reproductive fluidsHerbert Schuel
Department of Pathology and Anatomical Sciences, School of Medicine and Biomedical Sciences, University at Buffalo, State University of New York, Buffalo, NY 14214, USA
Chem Phys Lipids 121:211-27. 2002.... - Synergistic antinociceptive effects of anandamide, an endocannabinoid, and nonsteroidal anti-inflammatory drugs in peripheral tissue: a role for endogenous fatty-acid ethanolamides?Josee Guindon
Department of Pharmacology, Faculty of Medicine, Universite de Montreal C P 6128, Succ Centre Ville, Montreal, Quebec, Canada H2W 1T8
Eur J Pharmacol 550:68-77. 2006..Finally, locally injected anandamide with either NSAID (ibuprofen or rofecoxib) generates higher amount of fatty-acid ethanolamides. The exact comprehension of the mechanisms involved needs further investigation... - Conformational effects in enzyme catalysis: reaction via a high energy conformation in fatty acid amide hydrolaseAlessio Lodola
Biophys J 92:L20-2. 2007..They also show that approaches based simply on studying enzyme-substrate complexes can be misleading for understanding biochemical reactivity... - Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studiesMarco Mor
Dipartimento Farmaceutico, , Parco Area delle Scienze 27/A, I-43100 Parma, Italy
J Med Chem 47:4998-5008. 2004..The structure-activity characterization reported here should help optimize the pharmacodynamic and pharmacokinetic properties of this class of compounds...
Research Grants
- Role of oleoylethanolamide in the control of food intakeDaniele Piomelli; Fiscal Year: 2010....
- Role of oleoylethanolamide in the control of food intakeDaniele Piomelli; Fiscal Year: 2009....
- Characterization of anandamide transport in brainDaniele Piomelli; Fiscal Year: 2007..abstract_text> ..
- Role of Endocannabinoids in the Behavioral Consequences of Social IsolationDaniele Piomelli; Fiscal Year: 2007....
- Characterization of anandamide transport in brainDaniele Piomelli; Fiscal Year: 2007..abstract_text> ..
- Characterization of a novel cannabinoid ligandDaniele Piomelli; Fiscal Year: 2007..These studies will help reveal the roles played by the endocannabinoid system in the brain and may open innovative avenues for the treatment of neuropsychiatric and substance abuse disorders. ..
- Role of oleoylethanolamide in the control of food intakeDaniele Piomelli; Fiscal Year: 2009....
- Oleylethanolamide derivatives as anti-obesity agentsDaniele Piomelli; Fiscal Year: 2005....
- CONTROL OF ENDOCANNABINOID RELEASE IN VIVODaniele Piomelli; Fiscal Year: 2003..Moreover, by uncovering the neurochemical interactions between cocaine and the endogenous cannabinoids, our studies will contribute to the general understanding of substance abuse and neuropsychiatric disorders. ..
- NOVEL BRAIN CANNABINOID LIGANDDaniele Piomelli; Fiscal Year: 2002....
- ANANDAMIDE TRANSPORT IN BRAINDaniele Piomelli; Fiscal Year: 2002....
- Characterization of a novel brain cannabinoid ligandDaniele Piomelli; Fiscal Year: 2010..The objective of our research is to understand how these transmitters are produced and eliminated, and discover innovative medicines that target these processes. ..