Endocannabinoids: synthesis and degradation

Isolation and Structure of a Brain Constituent That Binds to the Cannabinoid Receptor

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Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors

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2-Arachidonoylgylcerol: A Possible Endogenous Cannabinoid Receptor Ligand in Brain

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Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides

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Formation and inactivation of endogenous cannabinoid anandamide in central neurons

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Leptin-regulated endocannabinoids are involved in maintaining food intake

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Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight patients: 1-year experience from the RIO-Europe study

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A second endogenous cannabinoid that modulates long-term potentiation

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Brain monoglyceride lipase participating in endocannabinoid inactivation

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Supersensitivity to anandamide and enhanced endogenous cannabinoid signaling in mice lacking fatty acid amide hydrolase

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Modulation of anxiety through blockade of anandamide hydrolysis

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CB1 Cannabinoid Receptors and On-Demand Defense Against Excitotoxicity

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Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brain

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An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors

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Molecular Characterization of a Phospholipase D Generating Anandamide and Its Congeners

Okamoto, Y., Morishita, J., Tsuboi, K., Tonai, T., & Ueda, N. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m306642200 · Cited by 805

2-Arachidonyl glyceryl ether, an endogenous agonist of the cannabinoid CB 1 receptor

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Endocannabinoid control of food intake and energy balance

Di Marzo, V., & Matias, I. (2005) · Nature Neuroscience · doi:10.1038/nn1457 · Cited by 743

Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist

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Structure and function of fatty acid amide hydrolase

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Heterosynaptic LTD of Hippocampal GABAergic Synapses

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An entourage effect: inactive endogenous fatty acid glycerol esters enhance 2-arachidonoyl-glycerol cannabinoid activity

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Characterization of a Novel Endocannabinoid, Virodhamine, with Antagonist Activity at the CB1 Receptor

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Cannabinoid physiology and pharmacology: 30 years of progress

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Segregation of two endocannabinoid-hydrolyzing enzymes into pre- and postsynaptic compartments in the rat hippocampus, cerebellum and amygdala

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Structural Adaptations in a Membrane Enzyme That Terminates Endocannabinoid Signaling

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The endocannabinoid system: a general view and latest additions

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N-Acylated glycerophospholipids and their derivatives

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A cannabinoid mechanism in relapse to cocaine seeking

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Characterization of the Fatty Acid Amide Hydrolase Inhibitor Cyclohexyl Carbamic Acid 3′-Carbamoyl-biphenyl-3-yl Ester (URB597): Effects on Anandamide and Oleoylethanolamide Deactivation

Fegley, D., Gaetani, S., Duranti, A., Tontini, A., Mor, M., Tarzia, G., & Piomelli, D. (2005) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.104.078980 · Cited by 427

cDNA Cloning, Tissue Distribution, and Identification of the Catalytic Triad of Monoglyceride Lipase

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SR141716, a central cannabinoid (CB1) receptor antagonist, blocks the motivational and dopamine-releasing effects of nicotine in rats

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Occurrence and Biosynthesis of Endogenous Cannabinoid Precursor,N-Arachidonoyl Phosphatidylethanolamine, in Rat Brain

Cadas, H., di Tomaso, E., & Piomelli, D. (1997) · The Journal of Neuroscience · doi:10.1523/jneurosci.17-04-01226.1997 · Cited by 396

Endovanilloids: Putative endogenous ligands of transient receptor potential vanilloid 1 channels

van der Stelt, M., & Di Marzo, V. (2004) · European Journal of Biochemistry · doi:10.1111/j.1432-1033.2004.04081.x · Cited by 389

N-acyl-dopamines: novel synthetic CB1 cannabinoid-receptor ligands and inhibitors of anandamide inactivation with cannabimimetic activity in vitro and in vivo

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Endocannabinoids control spasticity in a multiple sclerosis model

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Metabolism of the endocannabinoids, 2-arachidonylglycerol and anandamide, into prostaglandin, thromboxane, and prostacyclin glycerol esters and ethanolamides

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Biosynthesis and degradation of anandamide and 2-arachidonoylglycerol and their possible physiological significance

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Comparative analysis of fatty acid amide hydrolase and cb1 cannabinoid receptor expression in the mouse brain: evidence of a widespread role for fatty acid amide hydrolase in regulation of endocannabinoid signaling

Egertová, M., Cravatt, B. F., & Elphick, M. R. (2003) · Neuroscience · doi:10.1016/s0306-4522(03)00145-3 · Cited by 347

Cultured Rat Microglial Cells Synthesize the Endocannabinoid 2-Arachidonylglycerol, Which Increases Proliferation via a CB2 Receptor-Dependent Mechanism

Carrier, E. J., Kearn, C. S., Barkmeier, A. J., Breese, N. M., Yang, W., Nithipatikom, K., Pfister, S. L., Campbell, W. B., & Hillard, C. J. (2004) · Molecular Pharmacology · doi:10.1124/mol.65.4.999 · Cited by 336

Molecular Characterization of N-Acylethanolamine-hydrolyzing Acid Amidase, a Novel Member of the Choloylglycine Hydrolase Family with Structural and Functional Similarity to Acid Ceramidase

Tsuboi, K., Sun, Y.-X., Okamoto, Y., Araki, N., Tonai, T., & Ueda, N. (2005) · Journal of Biological Chemistry · doi:10.1074/jbc.m413473200 · Cited by 332

Reversible Inhibitors of Fatty Acid Amide Hydrolase That Promote Analgesia: Evidence for an Unprecedented Combination of Potency and Selectivity

Lichtman, A. H., Leung, D., Shelton, C. C., Saghatelian, A., Hardouin, C., Boger, D. L., & Cravatt, B. F. (2004) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.104.069401 · Cited by 328

Anandamide amidohydrolase reacting with 2‐arachidonoylglycerol, another cannabinoid receptor ligand

Goparaju, S. K., Ueda, N., Yamaguchi, H., & Yamamoto, S. (1998) · FEBS Letters · doi:10.1016/s0014-5793(97)01603-7 · Cited by 328

Endocannabinoids Acting at Cannabinoid-1 Receptors Regulate Cardiovascular Function in Hypertension

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A role for monoglyceride lipase in 2-arachidonoylglycerol inactivation

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Assignment of Endogenous Substrates to Enzymes by Global Metabolite Profiling

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Phospholipase Cβ Serves as a Coincidence Detector through Its Ca2+ Dependency for Triggering Retrograde Endocannabinoid Signal

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Brain Regional Distribution of Endocannabinoids: Implications for Their Biosynthesis and Biological Function

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Partial Purification and Characterization of the Porcine Brain Enzyme Hydrolyzing and Synthesizing Anandamide

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Enhanced levels of endogenous cannabinoids in the globus pallidus are associated with a reduction in movement in an animal model of Parkinson's disease

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Biosynthesis and inactivation of the endocannabinoid 2‐arachidonoylglycerol in circulating and tumoral macrophages

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Analysis of cannabinoid receptor binding and mRNA expression and endogenous cannabinoid contents in the developing rat brain during late gestation and early postnatal period

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Biosynthesis, release and degradation of the novel endogenous cannabimimetic metabolite 2-arachidonoylglycerol in mouse neuroblastoma cells

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Prefrontal Cortex Stimulation Induces 2-Arachidonoyl-Glycerol-Mediated Suppression of Excitation in Dopamine Neurons

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Anandamide and diet: Inclusion of dietary arachidonate and docosahexaenoate leads to increased brain levels of the corresponding N -acylethanolamines in piglets

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Anandamide receptors

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Inhibition of cyclooxygenase-2 potentiates retrograde endocannabinoid effects in hippocampus

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Biosynthesis of anandamide and N-palmitoylethanolamine by sequential actions of phospholipase A2 and lysophospholipase D

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Lipopolysaccharide Induces Anandamide Synthesis in Macrophages via CD14/MAPK/Phosphoinositide 3-Kinase/NF-κB Independently of Platelet-activating Factor

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Anandamide transport is independent of fatty-acid amide hydrolase activity and is blocked by the hydrolysis-resistant inhibitor AM1172

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The FGF receptor uses the endocannabinoid signaling system to couple to an axonal growth response

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Carrier-mediated transport and enzymatic hydrolysis of the endogenous cannabinoid 2-arachidonylglycerol

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RNA Interference Suggests a Primary Role for Monoacylglycerol Lipase in the Degradation of the Endocannabinoid 2-Arachidonoylglycerol

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Disruption of Endocannabinoid Release and Striatal Long-Term Depression by Postsynaptic Blockade of Endocannabinoid Membrane Transport

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Pharmacological Activity of Fatty Acid Amides Is Regulated, but Not Mediated, by Fatty Acid Amide Hydrolase in Vivo

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Functional disassociation of the central and peripheral fatty acid amide signaling systems

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Enzymatic synthesis of anandamide, an endogenous ligand for the cannabinoid receptor, by brain membranes.

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The Pharmacology of Bimatoprost (Lumigan™)

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Lack of CB1 Cannabinoid Receptor Impairs Cocaine Self-Administration

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Enzymes of porcine brain hydrolyzing 2-arachidonoylglycerol, an endogenous ligand of cannabinoid receptors

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The fatty acid amide hydrolase (FAAH)

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Cellular accumulation of anandamide: consensus and controversy

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The endocannabinoid signalling system: Biochemical aspects

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The novel endogenous cannabinoid 2-arachidonoylglycerol is inactivated by neuronal- and basophil-like cells: connections with anandamide

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Two novel classes of neuroactive fatty acid amides are substrates for mouse neuroblastoma ‘anandamide amidohydrolase’

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A role for endocannabinoids in the generation of parkinsonism and levodopa‐induced dyskinesia in MPTP‐lesioned non‐human primate models of Parkinson's disease

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Enzymatic Synthesis of Anandamide, an Endogenous Cannabinoid Receptor Ligand, through N-Acylphosphatidylethanolamine Pathway in Testis: Involvement of Ca2+-Dependent Transacylase and Phosphodiesterase Activities

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P2X7receptors control 2-arachidonoylglycerol production by microglial cells

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Anandamide Uptake by Human Endothelial Cells and Its Regulation by Nitric Oxide

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Low fatty acid amide hydrolase and high anandamide levels are associated with failure to achieve an ongoing pregnancy after IVF and embryo transfer

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Arachidonoylserotonin and Other Novel Inhibitors of Fatty Acid Amide Hydrolase

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Oxidative metabolism of endocannabinoids

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Anandamide, an endogenous cannabinomimetic eicosanoid: ‘Killing two birds with one stone’

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n-3 Polyunsaturated fatty acid (PUFA) deficiency elevates and n-3 PUFA enrichment reduces brain 2-arachidonoylglycerol level in mice

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Monoglyceride lipase-like enzymatic activity is responsible for hydrolysis of 2-arachidonoylglycerol in rat cerebellar membranes

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Fatty acid amide hydrolase: biochemistry, pharmacology, and therapeutic possibilities for an enzyme hydrolyzing anandamide, 2-arachidonoylglycerol, palmitoylethanolamide, and oleamide11Abbreviations: AEA, anandamide, arachidonyl ethanolamide; PEA, palmitoylethanolamide, N-(2-hydroxyethyl) hexadecamide; FAAH, fatty acid amide hydrolase; CB, cannabinoid; PMSF, phenylmethylsulfonyl fluoride; MAFP, methyl arachidonyl fluorophosphonate; methAEA, arachidonyl-1′-hydroxy-2′-propylamide; and NSAIDs, nonsteroidal anti-inflammatory drugs.

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