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.

Biochemical Pharmacology - Tập 62 Số 5 - Trang 517-526 - 2001
Christopher J. Fowler1, Kent-Olov Jonsson2, Gunnar Tiger2
1Department of Pharmacology and Clinical Neuroscience, Umeå University, Sweden
2Department of Pharmacology and Clinical Neuroscience. Umeå University, SE‐901 87 Umeå, Sweden

Tóm tắt

Từ khóa


Tài liệu tham khảo

Mechoulam, 1998, Endocannabinoids, Eur J Pharmacol, 359, 1, 10.1016/S0014-2999(98)00649-9

Lambert, 1999, The palmitoylethanolamide and oleamide enigmas, Curr Med Chem, 6, 757, 10.2174/0929867306666220401153732

Hillard, 2000, Biochemistry and pharmacology of the endocannabinoids arachidonoylethanolamide and 2-arachidonoylglycerol, Prostaglandins Other Lipid Mediat, 61, 3, 10.1016/S0090-6980(00)00051-4

Piomelli, 2000, The endocannabinoid system as a target for therapeutic drugs, Trends Pharmacol Sci, 21, 218, 10.1016/S0165-6147(00)01482-6

Smith, 1994, The pharmacological activity of anandamide, a putative endogenous cannabinoid, in mice, J Pharmacol Exp Ther, 270, 219

Di Marzo, 1998, Endocannabinoids, Trends Neurosci, 21, 521, 10.1016/S0166-2236(98)01283-1

Zygmunt, 1999, Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide, Nature, 400, 452, 10.1038/22761

Lambert, 1999, Analogues and homologues of N-palmitoylethanolamide, a putative endogenous CB2 cannabinoid, as potential ligands for the cannabinoid receptors, Biochim Biophys Acta, 1440, 266, 10.1016/S1388-1981(99)00132-8

Mazzari, 1996, N-(2-Hydroxyethyl)hexadecamide is orally active in reducing edema formation, and inflammatory hyperalgesia by down-modulating mast cell activation, Eur J Pharmacol, 300, 227, 10.1016/0014-2999(96)00015-5

Calignano, 1998, Control of pain initiation by endogenous cannabinoids, Nature, 394, 277, 10.1038/28393

Jaggar, 1998, The anti-hyperalgesic actions of the cannabinoid anandamide and the putative CB2 receptor agonist palmitoylethanolamide in visceral and somatic inflammatory pain, Pain, 76, 189, 10.1016/S0304-3959(98)00041-4

Aloe, 1993, A proposed autacoid mechanism controlling mastocyte behaviour, Agents Actions, 39, C145, 10.1007/BF01972748

Boger, 1998, Oleamide, Curr Pharm Des, 4, 303, 10.2174/138161280404221010152220

Verdon, 2000, Stereoselective modulatory actions of oleamide on GABAA receptors and voltage-gated Na+ channels in vitro, Br J Pharmacol, 129, 283, 10.1038/sj.bjp.0703051

Deutsch, 1993, Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist, Biochem Pharmacol, 46, 791, 10.1016/0006-2952(93)90486-G

Willoughby, 1997, The biodisposition and metabolism of anandamide in mice, J Pharmacol Exp Ther, 282, 243

Natarajan, 1984, Catabolism of N-acylethanolamine phospholipids by dog brain preparations, J Neurochem, 42, 1613, 10.1111/j.1471-4159.1984.tb12750.x

Cravatt, 1996, Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides, Nature, 384, 83, 10.1038/384083a0

Yagen, 2000, Oxidative metabolism of anandamide, Prostaglandins Other Lipid Mediat, 61, 29, 10.1016/S0090-6980(00)00053-8

Compton, 1997, The effect of the enzyme inhibitor phenylmethylsulfonyl fluoride on the pharmacological effect of anandamide in the mouse model of cannabimimetic activity, J Pharmacol Exp Ther, 283, 1138

Wiley, 2000, Influence of phenylmethylsulfonyl fluoride on anandamide brain levels and pharmacological effects, Life Sci, 67, 1573, 10.1016/S0024-3205(00)00749-9

Pertwee, 1995, Effect of phenylmethylsulphonyl fluoride on the potency of anandamide as an inhibitor of electrically evoked contractions in two isolated tissue preparations, Eur J Pharmacol, 272, 73, 10.1016/0014-2999(94)00618-H

Desarnaud, 1995, Anandamide amidohydrolase activity in rat brain microsomes. Identification and partial characterization, J Biol Chem, 270, 6030, 10.1074/jbc.270.11.6030

Matsuda, 1997, Metabolism of anandamide, an endogenous cannabinoid receptor ligand, in porcine ocular tissues, Exp Eye Res, 64, 707, 10.1006/exer.1996.0265

Watanabe, 1998, Distribution and characterization of anandamide amidohydrolase in mouse brain and liver, Life Sci, 62, 1223, 10.1016/S0024-3205(98)00052-6

Maccarrone, 2000, Down-regulation of anandamide hydrolase in mouse uterus by sex hormones, Eur J Biochem, 267, 2991, 10.1046/j.1432-1033.2000.01316.x

Bobrov, 2000, Hydrolysis of anandamide and eicosapentanoic acid ethanolamide in mouse splenocytes, Biochemistry (Mosc), 65, 615

Hillard, 1995, Characterization of the kinetics and distribution of N-arachidonylethanolamine (anandamide) hydrolysis by rat brain, Biochim Biophys Acta, 1257, 249, 10.1016/0005-2760(95)00087-S

Fowler, 1999, Inhibition of anandamide hydrolysis by the enantiomers of ibuprofen, ketorolac and flurbiprofen, Arch Biochem Biophys, 362, 191, 10.1006/abbi.1998.1025

Tsou, 1998, Fatty acid amide hydrolase is located preferentially in large neurons in the rat central nervous system as revealed by immunochemistry, Neurosci Lett, 254, 137, 10.1016/S0304-3940(98)00700-9

Egertová, 2000, Fatty acid amide hydrolase expression in rat choroid plexus, Neurosci Lett, 282, 13, 10.1016/S0304-3940(00)00841-7

Egertová, 1998, A new perspective on cannabinoid signalling, Proc R Soc Lond B Biol Sci, 265, 2081, 10.1098/rspb.1998.0543

Yazulla, 1999, Immunochemical localization of cannabinoid CB1 receptor and fatty acid amide hydrolase in rat retina, J Comp Neurol, 415, 80, 10.1002/(SICI)1096-9861(19991206)415:1<80::AID-CNE6>3.0.CO;2-H

Braud, 2000, Activation of rabbit blood platelets by anandamide through its cleavage into arachidonic acid, FEBS Lett, 471, 12, 10.1016/S0014-5793(00)01359-4

Edgemond, 1998, Human platelets and polymorphonuclear leukocytes synthesize oxygenated derivatives of arachidonylethanolamide (anandamide), Mol Pharmacol, 54, 180, 10.1124/mol.54.1.180

Di Marzo, 1999, Biosynthesis and inactivation of the endocannabinoid 2-arachidonoylglycerol in circulating and tumoral macrophages, Eur J Biochem, 264, 258, 10.1046/j.1432-1327.1999.00631.x

Maccarrone, 2000, Relation between decreased anandamide hydrolase concentrations in human lymphocytes and miscarriage, Lancet, 355, 1326, 10.1016/S0140-6736(00)02115-2

Bisogno, 1997, Occurrence and metabolism of anandamide and related acyl-ethanolamides in ovaries of the sea urchin Paracentrotus lividus, Biochim Biophys Acta, 1345, 338, 10.1016/S0005-2760(97)00009-X

Fowler, 2000, Differences in the pharmacological properties of rat and chicken brain fatty acid amidohydrolase, Br J Pharmacol, 131, 498, 10.1038/sj.bjp.0703569

Bisogno, 1997, Biosynthesis, uptake, and degradation of anandamide, and palmitoylethanolamide in leukocytes, J Biol Chem, 272, 3315, 10.1074/jbc.272.6.3315

Omeir, 1999, Identification of two serine residues involved in catalysis by fatty acid amide hydrolase, Biochem Biophys Res Commun, 264, 316, 10.1006/bbrc.1999.1524

Maccarrone, 2000, Human mast cells take up and hydrolyze anandamide under the control of 5-lipoxygenase and do not express cannabinoid receptors, FEBS Lett, 468, 176, 10.1016/S0014-5793(00)01223-0

Ueda, 1995, Partial purification and characterization of the porcine brain enzyme hydrolyzing and synthesizing anandamide, J Biol Chem, 270, 23823, 10.1074/jbc.270.40.23823

Qin, 1998, Determination of anandamide amidase activity using ultraviolet-active amine derivatives and reverse-phase high-performance liquid chromatography, Anal Biochem, 261, 8, 10.1006/abio.1998.2713

Tiger, 2000, Pharmacological properties of rat brain fatty acid amidohydrolase in different subcellular fractions using palmitoylethanolamide as substrate, Biochem Pharmacol, 59, 647, 10.1016/S0006-2952(99)00373-1

Maurelli, 1995, Two novel classes of neuroactive fatty acid amides are substrates for mouse neuroblastoma ‘anandamide amidohydrolase’, FEBS Lett, 377, 82, 10.1016/0014-5793(95)01311-3

Ueda, 1999, An acid amidase hydrolyzing anandamide as an endogenous ligand for cannabinoid receptors, FEBS Lett, 454, 267, 10.1016/S0014-5793(99)00820-0

Omeir, 1995, Arachidonyl ethanolamide-[1,2-14C] as a substrate for anandamide amidase, Life Sci, 56, 1999, 10.1016/0024-3205(95)00181-5

Fowler, 1997, Ibuprofen inhibits rat brain deamidation of anandamide at pharmacologically relevant concentrations. Mode of inhibition and structure-activity relationship, J Pharmacol Exp Ther, 283, 729

Maccarrone, 1998, Anandamide hydrolysis by human cells in culture and brain, J Biol Chem, 273, 32332, 10.1074/jbc.273.48.32332

Lang, 1999, Substrate specificity and stereoselectivity of rat brain microsomal anandamide amidohydrolase, J Med Chem, 42, 896, 10.1021/jm980461j

Arreaza, 1997, The cloned rat hydrolytic enzyme responsible for the breakdown of anandamide also catalyzes its formation via the condensation of arachidonic acid and etanolamine, Neurosci Lett, 234, 59, 10.1016/S0304-3940(97)00673-3

Katayama, 1999, Equilibrium in the hydrolysis and synthesis of cannabimimetic anandamide demonstrated by a purified enzyme, Biochim Biophys Acta, 1440, 205, 10.1016/S1388-1981(99)00124-9

Goparaju, 1999, Enzymes of porcine brain hydrolyzing 2-arachidonoylglycerol, an endogenous ligand of cannabinoid receptors, Biochem Pharmacol, 57, 417, 10.1016/S0006-2952(98)00314-1

Thumser, 1997, A fluorescence displacement assay for the measurement of arachidonyl ethanolamide (anandamide), and oleoyl amide (octadecenoamide) hydrolysis, Biochem Pharmacol, 53, 433, 10.1016/S0006-2952(96)00720-4

Chebrou, 1996, Study of the amidase signature group, Biochim Biophys Acta, 1298, 285, 10.1016/S0167-4838(96)00145-8

Giang, 1997, Molecular characterization of human and mouse fatty acid amide hydrolases, Proc Natl Acad Sci USA, 94, 2238, 10.1073/pnas.94.6.2238

Goparaju, 1999, Anandamide amidohydrolase of porcine brain, Biochim Biophys Acta, 1441, 77, 10.1016/S1388-1981(99)00143-2

Patricelli, 1999, Chemical and mutagenic investigations of fatty acid amide hydrolase, Biochemistry, 38, 9804, 10.1021/bi990637z

Patricelli, 2000, Clarifying the catalytic roles of conserved residues in the amidase signature family, J Biol Chem, 275, 19177, 10.1074/jbc.M001607200

Koutek, 1994, Inhibitors of arachidonoyl ethanolamide hydrolysis, J Biol Chem, 269, 22937, 10.1016/S0021-9258(17)31599-5

Deutsch, 1997, Fatty acid sulfonyl fluorides inhibit anandamide metabolism and bind to the cannabinoid receptor, Biochem Biophys Res Commun, 231, 217, 10.1006/bbrc.1997.6072

Bisogno, 1998, Arachidonoylserotonin and other novel inhibitors of fatty acid amide hydrolase, Biochem Biophys Res Commun, 248, 515, 10.1006/bbrc.1998.8874

Bisogno, 2000, N-acyl-dopamines, Biochem J, 351, 817, 10.1042/bj3510817

Patterson, 1996, Inhibition of oleamide hydrolase catalyzed hydrolysis of the endogenous sleep-inducing lipid cis-9-octadecenamide, J Am Chem Soc, 118, 5938, 10.1021/ja954064z

Patricelli, 1998, An endogenous sleep-inducing compound is a novel competitive inhibitor of fatty acid amide hydrolase, Bioorg Med Chem Lett, 8, 613, 10.1016/S0960-894X(98)00073-0

Boger, 1999, Trifluoromethyl ketone inhibitors of fatty acid amide hydrolase, Bioorg Med Chem Lett, 9, 265, 10.1016/S0960-894X(98)00734-3

Boger, 2000, Exceptionally potent inhibitors of fatty acid amide hydrolase, Proc Natl Acad Sci USA, 97, 5044, 10.1073/pnas.97.10.5044

Edgemond, 1998, Synthesis and characterization of diazomethylarachidonyl ketone, J Pharmacol Exp Ther, 286, 184

Deutsch, 1997, Methyl arachidonoyl fluorophosphonate, Biochem Pharmacol, 53, 255, 10.1016/S0006-2952(96)00830-1

De Petrocellis, 1997, Novel inhibitors of brain, neuronal and basophilic anandamide amidohydrolase, Biochem Biophys Res Commun, 231, 82, 10.1006/bbrc.1997.6000

Martin, 2000, Cannabinoid properties of methylfluorophosphonate analogues, J Pharmacol Exp Ther, 294, 1209

Fuller, 1978, Selective in vivo inhibition of monoamine oxidase in rat tissues by N-[2-(o-chlorophenoxy)-ethyl]-cyclopropylamine, Proc Soc Exp Biol Med, 158, 323, 10.3181/00379727-158-40197

Ask, 1983, Selective inhibition of monoamine oxidase in monoaminergic neurons in the rat brain, Naunyn Schmiedebergs Arch Pharmacol, 324, 79, 10.1007/BF00497011

Mendelson, 1999, The hypnotic actions of oleamide are blocked by a cannabinoid receptor antagonist, Neuroreport, 10, 3237, 10.1097/00001756-199910190-00021

Fowler, 1997, Ibuprofen inhibits the metabolism of the endogenous cannabimimetic agent anandamide, Pharmacol Toxicol, 80, 103, 10.1111/j.1600-0773.1997.tb00291.x

D’Ambra, 1992, Conformationally restrained analogues of pravadoline, J Med Chem, 35, 124

Stefano, 1998, Anandamide amidase inhibition enhances anandamide-stimulated nitric oxide release in invertebrate neural tissues, Brain Res, 793, 341, 10.1016/S0006-8993(98)00273-X

Natarajan, 1986, N-Acylethanolamine phospholipid metabolism in normal, and ischemic rat brain, Biochim Biophys Acta, 878, 32, 10.1016/0005-2760(86)90341-3

Berdyshev, 2000, Stress-induced generation of N-acylethanolamides in mouse epidermal JB6 P+ cells, Biochem J, 346, 369, 10.1042/bj3460369

Hansen, 2000, Determination of the phospholipid precursor of anandamide and other N-acylethanolamine phospholipids before and after sodium aizde-induced toxicity in cultured neocortical neurons, J Neurochem, 75, 861, 10.1046/j.1471-4159.2000.0750861.x

Skaper, 1996, The ALIAmide palmitoylethanolamide, and cannabinoids, but not anandamide, are protective in a delayed postglutamate paradigm of excitotoxic death in cerebellar granule neurons, Proc Natl Acad Sci USA, 93, 3984, 10.1073/pnas.93.9.3984

Nagayama, 1999, Cannabinoids and neuroprotection in global and focal cerebral ischemia and in neuronal cultures, J Neurosci, 19, 2987, 10.1523/JNEUROSCI.19-08-02987.1999

Sinor, 2000, Endocannabinoids protect cerebral cortical neurons from in vitro ischemia in rats, Neurosci Lett, 278, 157, 10.1016/S0304-3940(99)00922-2

Andersson, 2000, Neurotoxicity of glutamate in chick telencephalon neurons, Arch Toxicol, 74, 161, 10.1007/s002040050669

Baker, 2001, Endocannabinoids control spasticity in a multiple sclerosis model, FASEB J, 15, 300, 10.1096/fj.00-0399fje

Maccarrone, 2000, Anandamide induces apoptosis in human cells via vanilloid receptors. Evidence for a protective role of cannabinoid receptors, J Biol Chem, 275, 31938, 10.1074/jbc.M005722200