Daniele Piomelli

Dietary and behavioral interventions protect against age related activation of caspase cascades in the canine brain.

Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptors.

The challenge of brain lipidomics.

Targeted lipidomics: signaling lipids and drugs of abuse.

Selective inhibition of 2-AG hydrolysis enhances endocannabinoid signaling in hippocampus.

QM/MM modelling of oleamide hydrolysis in fatty acid amide hydrolase (FAAH) reveals a new mechanism of nucleophile activation.

Identification and functional characterization of brainstem cannabinoid CB2 receptors.

Oleylethanolamide activates Ras-Erk pathway and improves myocardial function in doxorubicin-induced heart failure.

Endocannabinoids at the spinal level regulate, but do not mediate, nonopioid stress-induced analgesia.

Actions of the FAAH inhibitor URB597 in neuropathic and inflammatory chronic pain models.

Postprandial increase of oleoylethanolamide mobilization in small intestine of the Burmese python (Python molurus).

Role of the basolateral nucleus of the amygdala in endocannabinoid-mediated stress-induced analgesia.

Anxiolytic-like properties of the anandamide transport inhibitor AM404.

Pharmacological characterization of hydrolysis-resistant analogs of oleoylethanolamide with potent anorexiant properties.

Molecular composition of the endocannabinoid system at glutamatergic synapses.

Cold exposure stimulates synthesis of the bioactive lipid oleoylethanolamide in rat adipose tissue.

Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597).

Synthesis and structure-activity relationships of FAAH inhibitors: cyclohexylcarbamic acid biphenyl esters with chemical modulation at the proximal phenyl ring.

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

Rapid broad-spectrum analgesia through activation of peroxisome proliferator-activated receptor-alpha.

Synergistic antinociceptive effects of anandamide, an endocannabinoid, and nonsteroidal anti-inflammatory drugs in peripheral tissue: a role for endogenous fatty-acid ethanolamides?

Conformational effects in enzyme catalysis: reaction via a high energy conformation in fatty acid amide hydrolase.

Effects of the FAAH inhibitor, URB597, and anandamide on lithium-induced taste reactivity responses: a measure of nausea in the rat.

Food intake regulates oleoylethanolamide formation and degradation in the proximal small intestine.

Determination of anandamide and other fatty acyl ethanolamides in human serum by electrospray tandem mass spectrometry.

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 transport.

Regulation of brain anandamide by acute administration of ethanol.

The fatty acid amide hydrolase inhibitor URB597 (cyclohexylcarbamic acid 3'-carbamoylbiphenyl-3-yl ester) reduces neuropathic pain after oral administration in mice.

Synergistic antinociception by the cannabinoid receptor agonist anandamide and the PPAR-alpha receptor agonist GW7647.

Antidepressant-like activity of the fatty acid amide hydrolase inhibitor URB597 in a rat model of chronic mild stress.

The antinociceptive effects of local injections of propofol in rats are mediated in part by cannabinoid CB1 and CB2 receptors.

Acute intracerebroventricular administration of palmitoylethanolamide, an endogenous peroxisome proliferator-activated receptor-alpha agonist, modulates carrageenan-induced paw edema in mice.

Anandamide levels in cerebrospinal fluid of first-episode schizophrenic patients: impact of cannabis use.

A key role for diacylglycerol lipase-alpha in metabotropic glutamate receptor-dependent endocannabinoid mobilization.

Hydrolysis of prostaglandin glycerol esters by the endocannabinoid-hydrolyzing enzymes, monoacylglycerol lipase and fatty acid amide hydrolase.

The anandamide transport inhibitor AM404 reduces ethanol self-administration.

A neuroscientist's guide to lipidomics.

The endogenous cannabinoid anandamide has effects on motivation and anxiety that are revealed by fatty acid amide hydrolase (FAAH) inhibition.

Enhancement of endocannabinoid signaling and the pharmacotherapy of depression.

Identification of biosynthetic precursors for the endocannabinoid anandamide in the rat brain.

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

The effect of cannabidiol and URB597 on conditioned gaping (a model of nausea) elicited by a lithium-paired context in the rat.

Correlation between energetics of collisionally activated decompositions, interaction energy and biological potency of carbamate FAAH inhibitors.

Identification of productive inhibitor binding orientation in fatty acid amide hydrolase (FAAH) by QM/MM mechanistic modelling.

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

Endogenous cannabinoids in patients with schizophrenia and substance use disorder during quetiapine therapy.

Effects of palmitoylethanolamide on signaling pathways implicated in the development of spinal cord injury.

Targeted enhancement of oleoylethanolamide production in proximal small intestine induces across-meal satiety in rats.

Increase of brain endocannabinoid anandamide levels by FAAH inhibition and alcohol abuse behaviours in the rat.

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

An endocannabinoid signaling system modulates anxiety-like behavior in male Syrian hamsters.

The element of surprise.

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

Inhibition of anandamide hydrolysis by cyclohexyl carbamic acid 3'-carbamoyl-3-yl ester (URB597) reverses abuse-related behavioral and neurochemical effects of nicotine in rats.

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

The lipid messenger OEA links dietary fat intake to satiety.

Distribution and function of monoacylglycerol lipase in the gastrointestinal tract.

The collisional behavior of ESI-generated protonated molecules of some carbamate FAAH inhibitors isosteres and its relationships with biological activity.

Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice.

Sleep deprivation increases oleoylethanolamide in human cerebrospinal fluid.

Rapid pain modulation with nuclear receptor ligands.

Responses to stress: from the periphery to the brain.

Lipidomic analysis of endocannabinoid metabolism in biological samples.

Anandamide elevation in cerebrospinal fluid in initial prodromal states of psychosis.

An endocannabinoid signal associated with desire for alcohol is suppressed in recently abstinent alcoholics.

Central administration of palmitoylethanolamide reduces hyperalgesia in mice via inhibition of NF-kappaB nuclear signalling in dorsal root ganglia.

Fat-induced satiety factor oleoylethanolamide enhances memory consolidation.

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

Targeted lipidomics as a tool to investigate endocannabinoid function.

The endocannabinoid system as a target for novel anxiolytic and antidepressant drugs.

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

Lipidomic analysis of biological samples by liquid chromatography coupled to mass spectrometry.

CD36 gene deletion decreases oleoylethanolamide levels in small intestine of free-feeding mice.

Discovery of potent and reversible monoacylglycerol lipase inhibitors.

A novel lipidomic strategy reveals plasma phospholipid signatures associated with respiratory disease severity in cystic fibrosis patients.

Selective N-acylethanolamine-hydrolyzing acid amidase inhibition reveals a key role for endogenous palmitoylethanolamide in inflammation.

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

Pitfalls and solutions in assaying anandamide transport in cells.

Evidence for a role of endocannabinoids, astrocytes and p38 phosphorylation in the resolution of postoperative pain.

The fat-induced satiety factor oleoylethanolamide suppresses feeding through central release of oxytocin.

Genetic deletion of fatty acid amide hydrolase alters emotional behavior and serotonergic transmission in the dorsal raphe, prefrontal cortex, and hippocampus.

Synthesis and structure-activity relationships of N-(2-oxo-3-oxetanyl)amides as N-acylethanolamine-hydrolyzing acid amidase inhibitors.

Blockade of nicotine reward and reinstatement by activation of alpha-type peroxisome proliferator-activated receptors.

Deficient liver biosynthesis of docosahexaenoic acid correlates with cognitive impairment in Alzheimer's disease.

Changes in cognition and amyloid-β processing with long term cholesterol reduction using atorvastatin in aged dogs.

Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism.

Ten years of Nature Reviews Neuroscience: insights from the highly cited.

PER2 controls lipid metabolism by direct regulation of PPARγ.

Evaluation of the emotional phenotype and serotonergic neurotransmission of fatty acid amide hydrolase-deficient mice.

Central and peripheral endocannabinoids and cognate acylethanolamides in humans: association with race, adiposity, and energy expenditure.

Deficiency of lipoprotein lipase in neurons modifies the regulation of energy balance and leads to obesity.

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

Proinflammatory stimuli control N-acylphosphatidylethanolamine-specific phospholipase D expression in macrophages.

Understanding the role of carbamate reactivity in fatty acid amide hydrolase inhibition by QM/MM mechanistic modelling.

Plasma lipidomics reveals potential prognostic signatures within a cohort of cystic fibrosis patients.

Sympathetic activity controls fat-induced oleoylethanolamide signaling in small intestine.

Diacylglycerol lipase-alpha and -beta control neurite outgrowth in neuro-2a cells through distinct molecular mechanisms.

Towards a whole-body systems [multi-organ] lipidomics in Alzheimer's disease.

An amyloid β(42)-dependent deficit in anandamide mobilization is associated with cognitive dysfunction in Alzheimer's disease.

New lipidomic approaches in cystic fibrosis.

Endocannabinoid signal in the gut controls dietary fat intake.

Decoding functional metabolomics with docosahexaenoyl ethanolamide (DHEA) identifies novel bioactive signals.

The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system.

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

Covalent inhibitors of fatty acid amide hydrolase: a rationale for the activity of piperidine and piperazine aryl ureas.

A thickening network of lipids.

Elevated stearoyl-CoA desaturase in brains of patients with Alzheimer's disease.

A catalytically silent FAAH-1 variant drives anandamide transport in neurons.

Endocannabinoid regulation of acute and protracted nicotine withdrawal: effect of FAAH inhibition.

Decreased body weight and hepatic steatosis with altered fatty acid ethanolamide metabolism in aged L-Fabp -/- mice.

Moving beyond "good fat, bad fat": the complex roles of dietary lipids in cellular function and health: session abstracts.

A catalytic mechanism for cysteine N-terminal nucleophile hydrolases, as revealed by free energy simulations.

2-arachidonoylglycerol signaling in forebrain regulates systemic energy metabolism.

Peripheral FAAH inhibition causes profound antinociception and protects against indomethacin-induced gastric lesions.

N-(2-oxo-3-oxetanyl)carbamic acid esters as N-acylethanolamine acid amidase inhibitors: synthesis and structure-activity and structure-property relationships.

The thrifty lipids: endocannabinoids and the neural control of energy conservation.

Selective cannabinoid-1 receptor blockade benefits fatty acid and triglyceride metabolism significantly in weight-stable nonhuman primates.

Activation of type 5 metabotropic glutamate receptors and diacylglycerol lipase-α initiates 2-arachidonoylglycerol formation and endocannabinoid-mediated analgesia.

Pretreatment with the monoacylglycerol lipase inhibitor URB602 protects from the long-term consequences of neonatal hypoxic-ischemic brain injury in rats.

Associations of fatty acids in cerebrospinal fluid with peripheral glucose concentrations and energy metabolism.

Peroxisome proliferator-activated receptor α mediates acute effects of palmitoylethanolamide on sensory neurons.

Uncoupling of the endocannabinoid signalling complex in a mouse model of fragile X syndrome.

Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease.

Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor.

Synergistic effects of galantamine and memantine in attenuating scopolamine-induced amnesia in mice.

Antinociceptive effects of the N-acylethanolamine acid amidase inhibitor ARN077 in rodent pain models.

A binding site for nonsteroidal anti-inflammatory drugs in fatty acid amide hydrolase.

Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity.

Quantum mechanics/molecular mechanics modeling of fatty acid amide hydrolase reactivation distinguishes substrate from irreversible covalent inhibitors.

Pharmacological characterization of memoquin, a multi-target compound for the treatment of Alzheimer's disease.

Endocannabinoid signaling in the gut mediates preference for dietary unsaturated fats.

Galantamine potentiates the neuroprotective effect of memantine against NMDA-induced excitotoxicity.

A fatty gut feeling.

Discovery of a new class of highly potent inhibitors of acid ceramidase: synthesis and structure-activity relationship (SAR).

Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors.

Development of fragment-based n-FABS NMR screening applied to the membrane enzyme FAAH.

More surprises lying ahead. The endocannabinoids keep us guessing.

Synthesis and structure-activity relationship (SAR) of 2-methyl-4-oxo-3-oxetanylcarbamic acid esters, a class of potent N-acylethanolamine acid amidase (NAAA) inhibitors.

Lipid-enriched diet rescues lethality and slows down progression in a murine model of VCP-associated disease.

A glycosylated, labionin-containing lanthipeptide with marked antinociceptive activity.

Brown adipose tissue quantification in human neonates using water-fat separated MRI.

Fluorine NMR-based screening on cell membrane extracts.

Effects of acute stress on cardiac endocannabinoids, lipogenesis, and inflammation in rats.

Synthesis, structure-activity, and structure-stability relationships of 2-substituted-N-(4-oxo-3-oxetanyl) N-acylethanolamine acid amidase (NAAA) inhibitors.

Circadian control of fatty acid elongation by SIRT1 protein-mediated deacetylation of acetyl-coenzyme A synthetase 1.

Peripheral gating of pain signals by endogenous lipid mediators.

A discount on cannabinoids.

Applying a multitarget rational drug design strategy: the first set of modulators with potent and balanced activity toward dopamine D3 receptor and fatty acid amide hydrolase.

Sample preparation and orthogonal chromatography for broad polarity range plasma metabolomics: application to human subjects with neurodegenerative dementia.

Advances in the discovery of N-acylethanolamine acid amidase inhibitors.

Cannabinoid type 1 receptor availability in the amygdala mediates threat processing in trauma survivors.

3-Aminoazetidin-2-one derivatives as N-acylethanolamine acid amidase (NAAA) inhibitors suitable for systemic administration.

Role of oleoylethanolamide as a feeding regulator in goldfish.

β-Lactones Inhibit N-acylethanolamine Acid Amidase by S-Acylation of the Catalytic N-Terminal Cysteine.

A mighty (ochondrial) fight?

Structural determinants of peripheral O-arylcarbamate FAAH inhibitors render them dual substrates for Abcb1 and Abcg2 and restrict their access to the brain.

O-(triazolyl)methyl carbamates as a novel and potent class of fatty acid amide hydrolase (FAAH) inhibitors.

Synthesis, biological evaluation, and 3D QSAR study of 2-methyl-4-oxo-3-oxetanylcarbamic acid esters as N-acylethanolamine acid amidase (NAAA) inhibitors.

A lipid gate for the peripheral control of pain.

Benzoxazolone carboxamides: potent and systemically active inhibitors of intracellular acid ceramidase.

Intestinal lipid-derived signals that sense dietary fat.

Methamphetamine accelerates cellular senescence through stimulation of de novo ceramide biosynthesis.

Structure of human N-acylphosphatidylethanolamine-hydrolyzing phospholipase D: regulation of fatty acid ethanolamide biosynthesis by bile acids.

Modulation of sweet taste sensitivities by endogenous leptin and endocannabinoids in mice.

Rapid evaluation of 25 key sphingolipids and phosphosphingolipids in human plasma by LC-MS/MS.

Effects of Fatty Acid Amide Hydrolase (FAAH) Inhibitors in Non-Human Primate Models of Nicotine Reward and Relapse.

Multitarget fatty acid amide hydrolase/cyclooxygenase blockade suppresses intestinal inflammation and protects against nonsteroidal anti-inflammatory drug-dependent gastrointestinal damage.

A Potent Systemically Active N-Acylethanolamine Acid Amidase Inhibitor that Suppresses Inflammation and Human Macrophage Activation.

Peripheral FAAH and soluble epoxide hydrolase inhibitors are synergistically antinociceptive.

Peroxide-Dependent MGL Sulfenylation Regulates 2-AG-Mediated Endocannabinoid Signaling in Brain Neurons.

Feeding-induced oleoylethanolamide mobilization is disrupted in the gut of diet-induced obese rodents.

Role of the satiety factor oleoylethanolamide in alcoholism.

Activity-Based Probe for N-Acylethanolamine Acid Amidase.

Monoglyceride lipase: Structure and inhibitors.

Deficiency of Lipoprotein Lipase in Neurons Decreases AMPA Receptor Phosphorylation and Leads to Neurobehavioral Abnormalities in Mice.

Fasting stimulates 2-AG biosynthesis in the small intestine: role of cholinergic pathways.

Endocannabinoid Modulation of Predator Stress-Induced Long-Term Anxiety in Rats.

A Double Whammy: Targeting Both Fatty Acid Amide Hydrolase (FAAH) and Cyclooxygenase (COX) To Treat Pain and Inflammation.

Endocannabinoid signaling mediates oxytocin-driven social reward.

Acid Ceramidase in Melanoma: EXPRESSION, LOCALIZATION, AND EFFECTS OF PHARMACOLOGICAL INHIBITION.

Effects of fatty acid amide hydrolase (FAAH) inhibitors on working memory in rats.

Benzoxazolone Carboxamides as Potent Acid Ceramidase Inhibitors: Synthesis and Structure-Activity Relationship (SAR) Studies.

Macrophage-derived lipid agonists of PPAR-α as intrinsic controllers of inflammation.

Wagging the Tail: Essential Role of Substrate Flexibility in FAAH Catalysis.

Fluorine nuclear magnetic resonance-based assay in living mammalian cells.

Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies.

Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure-activity relationship (SAR) studies.

A role for the endocannabinoid 2-arachidonoyl-sn-glycerol for social and high-fat food reward in male mice.

Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain.

Vaccenic acid suppresses intestinal inflammation by increasing the endocannabinoid anandamide and non-cannabinoid signaling molecules in a rat model of the metabolic syndrome.

A simple and accurate protocol for absolute polar metabolite quantification in cell cultures using quantitative nuclear magnetic resonance.

Ion mobility mass spectrometry enhances low-abundance species detection in untargeted lipidomics.

Assay of Monoacylglycerol Lipase Activity.

Obesity development in neuron-specific lipoprotein lipase deficient mice is not responsive to increased dietary fat content or change in fat composition.

Absolute nutrient concentration measurements in cell culture media: (1)H q-NMR spectra and data to compare the efficiency of pH-controlled protein precipitation versus CPMG or post-processing filtering approaches.

Second-Generation Non-Covalent NAAA Inhibitors are Protective in a Model of Multiple Sclerosis.

Endogenous N-acyl taurines regulate skin wound healing.

Free-energy studies reveal a possible mechanism for oxidation-dependent inhibition of MGL.

A Primary Cortical Input to Hippocampus Expresses a Pathway-Specific and Endocannabinoid-Dependent Form of Long-Term Potentiation.

Bile Acid Recognition by NAPE-PLD.