Arachidonic Acid: An unsaturated, essential fatty acid. It is found in animal and human fat as well as in the liver, brain, and glandular organs, and is a constituent of animal phosphatides. It is formed by the synthesis from dietary linoleic acid and is a precursor in the biosynthesis of prostaglandins, thromboxanes, and leukotrienes.Arachidonic AcidsPhospholipases A2: Phospholipases that hydrolyze the acyl group attached to the 2-position of PHOSPHOGLYCERIDES.Phospholipases A: Phospholipases that hydrolyze one of the acyl groups of phosphoglycerides or glycerophosphatidates.Hydroxyeicosatetraenoic Acids: Eicosatetraenoic acids substituted in any position by one or more hydroxy groups. They are important intermediates in a series of biosynthetic processes leading from arachidonic acid to a number of biologically active compounds such as prostaglandins, thromboxanes, and leukotrienes.Lipoxygenase: An enzyme of the oxidoreductase class primarily found in PLANTS. It catalyzes reactions between linoleate and other fatty acids and oxygen to form hydroperoxy-fatty acid derivatives.12-Hydroxy-5,8,10,14-eicosatetraenoic Acid: A lipoxygenase metabolite of ARACHIDONIC ACID. It is a highly selective ligand used to label mu-opioid receptors in both membranes and tissue sections. The 12-S-HETE analog has been reported to augment tumor cell metastatic potential through activation of protein kinase C. (J Pharmacol Exp Ther 1995; 274(3):1545-51; J Natl Cancer Inst 1994; 86(15):1145-51)Masoprocol: A potent lipoxygenase inhibitor that interferes with arachidonic acid metabolism. The compound also inhibits formyltetrahydrofolate synthetase, carboxylesterase, and cyclooxygenase to a lesser extent. It also serves as an antioxidant in fats and oils.5,8,11,14-Eicosatetraynoic Acid: A 20-carbon unsaturated fatty acid containing 4 alkyne bonds. It inhibits the enzymatic conversion of arachidonic acid to prostaglandins E(2) and F(2a).8,11,14-Eicosatrienoic Acid: A 20-carbon-chain fatty acid, unsaturated at positions 8, 11, and 14. It differs from arachidonic acid, 5,8,11,14-eicosatetraenoic acid, only at position 5.Lipoxygenase Inhibitors: Compounds that bind to and inhibit that enzymatic activity of LIPOXYGENASES. Included under this category are inhibitors that are specific for lipoxygenase subtypes and act to reduce the production of LEUKOTRIENES.Prostaglandins: A group of compounds derived from unsaturated 20-carbon fatty acids, primarily arachidonic acid, via the cyclooxygenase pathway. They are extremely potent mediators of a diverse group of physiological processes.Eicosanoids: A class of compounds named after and generally derived from C20 fatty acids (EICOSANOIC ACIDS) that includes PROSTAGLANDINS; LEUKOTRIENES; THROMBOXANES, and HYDROXYEICOSATETRAENOIC ACIDS. They have hormone-like effects mediated by specialized receptors (RECEPTORS, EICOSANOID).Arachidonate Lipoxygenases: Enzymes catalyzing the oxidation of arachidonic acid to hydroperoxyarachidonates. These products are then rapidly converted by a peroxidase to hydroxyeicosatetraenoic acids. The positional specificity of the enzyme reaction varies from tissue to tissue. The final lipoxygenase pathway leads to the leukotrienes. EC 1.13.11.- .Arachidonate 5-Lipoxygenase: An enzyme that catalyzes the oxidation of arachidonic acid to yield 5-hydroperoxyarachidonate (5-HPETE) which is rapidly converted by a peroxidase to 5-hydroxy-6,8,11,14-eicosatetraenoate (5-HETE). The 5-hydroperoxides are preferentially formed in leukocytes.Prostaglandin-Endoperoxide Synthases: Enzyme complexes that catalyze the formation of PROSTAGLANDINS from the appropriate unsaturated FATTY ACIDS, molecular OXYGEN, and a reduced acceptor.Leukotrienes: A family of biologically active compounds derived from arachidonic acid by oxidative metabolism through the 5-lipoxygenase pathway. They participate in host defense reactions and pathophysiological conditions such as immediate hypersensitivity and inflammation. They have potent actions on many essential organs and systems, including the cardiovascular, pulmonary, and central nervous system as well as the gastrointestinal tract and the immune system.Group IV Phospholipases A2: A cytosolic phospholipase A2 group that plays an important role in the release of free ARACHIDONIC ACID, which in turn is metabolized to PROSTAGLANDINS by the CYCLOOXYGENASE pathway and to LEUKOTRIENES by the 5-LIPOXYGENASE pathway.Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids. It also inhibits the motility of polymorphonuclear leukocytes.Fatty Acids, Unsaturated: FATTY ACIDS in which the carbon chain contains one or more double or triple carbon-carbon bonds.Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.Dinoprostone: The most common and most biologically active of the mammalian prostaglandins. It exhibits most biological activities characteristic of prostaglandins and has been used extensively as an oxytocic agent. The compound also displays a protective effect on the intestinal mucosa.Calcimycin: An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.Leukotriene B4: The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990)Thromboxane B2: A stable, physiologically active compound formed in vivo from the prostaglandin endoperoxides. It is important in the platelet-release reaction (release of ADP and serotonin).4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine: A dual inhibitor of both cyclooxygenase and lipoxygenase pathways. It exerts an anti-inflammatory effect by inhibiting the formation of prostaglandins and leukotrienes. The drug also enhances pulmonary hypoxic vasoconstriction and has a protective effect after myocardial ischemia.Cyclooxygenase Inhibitors: Compounds or agents that combine with cyclooxygenase (PROSTAGLANDIN-ENDOPEROXIDE SYNTHASES) and thereby prevent its substrate-enzyme combination with arachidonic acid and the formation of eicosanoids, prostaglandins, and thromboxanes.Prostaglandins E: (11 alpha,13E,15S)-11,15-Dihydroxy-9-oxoprost-13-en-1-oic acid (PGE(1)); (5Z,11 alpha,13E,15S)-11,15-dihydroxy-9-oxoprosta-5,13-dien-1-oic acid (PGE(2)); and (5Z,11 alpha,13E,15S,17Z)-11,15-dihydroxy-9-oxoprosta-5,13,17-trien-1-oic acid (PGE(3)). Three of the six naturally occurring prostaglandins. They are considered primary in that no one is derived from another in living organisms. Originally isolated from sheep seminal fluid and vesicles, they are found in many organs and tissues and play a major role in mediating various physiological activities.Arachidonate 12-Lipoxygenase: An enzyme that catalyzes the oxidation of arachidonic acid to yield 12-hydroperoxyarachidonate (12-HPETE) which is itself rapidly converted by a peroxidase to 12-hydroxy-5,8,10,14-eicosatetraenoate (12-HETE). The 12-hydroperoxides are preferentially formed in PLATELETS.Eicosanoic Acids: 20-carbon saturated monocarboxylic acids.Phospholipids: Lipids containing one or more phosphate groups, particularly those derived from either glycerol (phosphoglycerides see GLYCEROPHOSPHOLIPIDS) or sphingosine (SPHINGOLIPIDS). They are polar lipids that are of great importance for the structure and function of cell membranes and are the most abundant of membrane lipids, although not stored in large amounts in the system.Docosahexaenoic Acids: C22-unsaturated fatty acids found predominantly in FISH OILS.Fatty Acids: Organic, monobasic acids derived from hydrocarbons by the equivalent of oxidation of a methyl group to an alcohol, aldehyde, and then acid. Fatty acids are saturated and unsaturated (FATTY ACIDS, UNSATURATED). (Grant & Hackh's Chemical Dictionary, 5th ed)Linoleic Acid: A doubly unsaturated fatty acid, occurring widely in plant glycosides. It is an essential fatty acid in mammalian nutrition and is used in the biosynthesis of prostaglandins and cell membranes. (From Stedman, 26th ed)Cyclooxygenase 2: An inducibly-expressed subtype of prostaglandin-endoperoxide synthase. It plays an important role in many cellular processes and INFLAMMATION. It is the target of COX2 INHIBITORS.Cyclooxygenase 1: A constitutively-expressed subtype of prostaglandin-endoperoxide synthase. It plays an important role in many cellular processes.Eicosapentaenoic Acid: Important polyunsaturated fatty acid found in fish oils. It serves as the precursor for the prostaglandin-3 and thromboxane-3 families. A diet rich in eicosapentaenoic acid lowers serum lipid concentration, reduces incidence of cardiovascular disorders, prevents platelet aggregation, and inhibits arachidonic acid conversion into the thromboxane-2 and prostaglandin-2 families.SRS-A: A group of LEUKOTRIENES; (LTC4; LTD4; and LTE4) that is the major mediator of BRONCHOCONSTRICTION; HYPERSENSITIVITY; and other allergic reactions. Earlier studies described a "slow-reacting substance of ANAPHYLAXIS" released from lung by cobra venom or after anaphylactic shock. The relationship between SRS-A leukotrienes was established by UV which showed the presence of the conjugated triene. (From Merck Index, 11th ed)Epoprostenol: A prostaglandin that is a powerful vasodilator and inhibits platelet aggregation. It is biosynthesized enzymatically from PROSTAGLANDIN ENDOPEROXIDES in human vascular tissue. The sodium salt has been also used to treat primary pulmonary hypertension (HYPERTENSION, PULMONARY).6-Ketoprostaglandin F1 alpha: The physiologically active and stable hydrolysis product of EPOPROSTENOL. Found in nearly all mammalian tissue.Linoleic Acids: Eighteen-carbon essential fatty acids that contain two double bonds.Cytochrome P-450 Enzyme System: A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.Blood Platelets: Non-nucleated disk-shaped cells formed in the megakaryocyte and found in the blood of all mammals. They are mainly involved in blood coagulation.Arachidonate 15-Lipoxygenase: An enzyme that catalyzes the oxidation of arachidonic acid to yield 15-hydroperoxyarachidonate (15-HPETE) which is rapidly converted to 15-hydroxy-5,8,11,13-eicosatetraenoate (15-HETE). The 15-hydroperoxides are preferentially formed in NEUTROPHILS and LYMPHOCYTES.Phospholipases: A class of enzymes that catalyze the hydrolysis of phosphoglycerides or glycerophosphatidates. EC 3.1.-.Platelet Aggregation: The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS.Group VI Phospholipases A2: A calcium-independent phospholipase A2 group that may play a role in membrane phospholipid remodeling and homeostasis by controling the levels of PHOSPHATIDYLCHOLINE in mammalian cell membranes.Prostaglandins F: (9 alpha,11 alpha,13E,15S)-9,11,15-Trihydroxyprost-13-en-1-oic acid (PGF(1 alpha)); (5Z,9 alpha,11,alpha,13E,15S)-9,11,15-trihydroxyprosta-5,13-dien-1-oic acid (PGF(2 alpha)); (5Z,9 alpha,11 alpha,13E,15S,17Z)-9,11,15-trihydroxyprosta-5,13,17-trien-1-oic acid (PGF(3 alpha)). A family of prostaglandins that includes three of the six naturally occurring prostaglandins. All naturally occurring PGF have an alpha configuration at the 9-carbon position. They stimulate uterine and bronchial smooth muscle and are often used as oxytocics.Calcium: A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.Fatty Acids, Omega-6: FATTY ACIDS which have the first unsaturated bond in the sixth position from the omega carbon. A typical American diet tends to contain substantially more omega-6 than OMEGA-3 FATTY ACIDS.Cells, Cultured: Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.Phospholipases A2, Cytosolic: A subcategory of phospholipases A2 that occur in the CYTOSOL.Prostaglandins H: A group of physiologically active prostaglandin endoperoxides. They are precursors in the biosynthesis of prostaglandins and thromboxanes. The most frequently encountered member of this group is the prostaglandin H2.Thromboxanes: Physiologically active compounds found in many organs of the body. They are formed in vivo from the prostaglandin endoperoxides and cause platelet aggregation, contraction of arteries, and other biological effects. Thromboxanes are important mediators of the actions of polyunsaturated fatty acids transformed by cyclooxygenase.Prostaglandin Endoperoxides: Precursors in the biosynthesis of prostaglandins and thromboxanes from arachidonic acid. They are physiologically active compounds, having effect on vascular and airway smooth muscles, platelet aggregation, etc.Prostaglandin H2: A cyclic endoperoxide intermediate produced by the action of CYCLOOXYGENASE on ARACHIDONIC ACID. It is further converted by a series of specific enzymes to the series 2 prostaglandins.Prostaglandins G: A group of physiologically active prostaglandin endoperoxides. They are precursors in the biosynthesis of prostaglandins and thromboxanes. Most frequently encountered member of this group is the prostaglandin G2.Chromatography, High Pressure Liquid: Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.Isoenzymes: Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.Thromboxane A2: An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).Alkane 1-Monooxygenase: A P450 oxidoreductase that catalyzes the hydroxylation of the terminal carbon of linear hydrocarbons such as octane and FATTY ACIDS in the omega position. The enzyme may also play a role in the oxidation of a variety of structurally unrelated compounds such as XENOBIOTICS, and STEROIDS.ZymosanEnzyme Activation: Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.Pyrones: Keto-pyrans.Leukotriene A4: (2S-(2 alpha,3 beta(1E,3E,5Z,8Z)))-3-(1,3,5,8-Tetradecatetraenyl)oxiranebutanoic acid. An unstable allylic epoxide, formed from the immediate precursor 5-HPETE via the stereospecific removal of a proton at C-10 and dehydration. Its biological actions are determined primarily by its metabolites, i.e., LEUKOTRIENE B4 and cysteinyl-leukotrienes. Alternatively, leukotriene A4 is converted into LEUKOTRIENE C4 by glutathione-S-transferase or into 5,6-di-HETE by the epoxide-hydrolase. (From Dictionary of Prostaglandins and Related Compounds, 1990)Cytosol: Intracellular fluid from the cytoplasm after removal of ORGANELLES and other insoluble cytoplasmic components.Phospholipase A2 Inhibitors: Compounds that inhibit or block the activity of a PHOSPHOLIPASE A2 enzyme.Neutrophils: Granular leukocytes having a nucleus with three to five lobes connected by slender threads of chromatin, and cytoplasm containing fine inconspicuous granules and stainable by neutral dyes.Thromboxane-A Synthase: An enzyme found predominantly in platelet microsomes. It catalyzes the conversion of PGG(2) and PGH(2) (prostaglandin endoperoxides) to thromboxane A2. EC 5.3.99.5.Kinetics: The rate dynamics in chemical or physical systems.Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.Fatty Acids, Essential: Long chain organic acid molecules that must be obtained from the diet. Examples are LINOLEIC ACIDS and LINOLENIC ACIDS.Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)Rabbits: The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.Fatty Acids, Omega-3: A group of fatty acids, often of marine origin, which have the first unsaturated bond in the third position from the omega carbon. These fatty acids are believed to reduce serum triglycerides, prevent insulin resistance, improve lipid profile, prolong bleeding times, reduce platelet counts, and decrease platelet adhesiveness.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.DiglyceridesMicrosomes: Artifactual vesicles formed from the endoplasmic reticulum when cells are disrupted. They are isolated by differential centrifugation and are composed of three structural features: rough vesicles, smooth vesicles, and ribosomes. Numerous enzyme activities are associated with the microsomal fraction. (Glick, Glossary of Biochemistry and Molecular Biology, 1990; from Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed)Protein Kinase C: An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.Prostaglandins D: Physiologically active prostaglandins found in many tissues and organs. They show pressor activity, are mediators of inflammation, and have potential antithrombotic effects.Group II Phospholipases A2: A subcategory of secreted phospholipases A2 that includes enzymes isolated from a variety of sources. The creation of this group is based upon similarities in the structural determinants of the enzymes including a negatively charged carboxy-terminal segment.Gas Chromatography-Mass Spectrometry: A microanalytical technique combining mass spectrometry and gas chromatography for the qualitative as well as quantitative determinations of compounds.Phosphatidylinositols: Derivatives of phosphatidic acids in which the phosphoric acid is bound in ester linkage to the hexahydroxy alcohol, myo-inositol. Complete hydrolysis yields 1 mole of glycerol, phosphoric acid, myo-inositol, and 2 moles of fatty acids.Lipid Peroxides: Peroxides produced in the presence of a free radical by the oxidation of unsaturated fatty acids in the cell in the presence of molecular oxygen. The formation of lipid peroxides results in the destruction of the original lipid leading to the loss of integrity of the membranes. They therefore cause a variety of toxic effects in vivo and their formation is considered a pathological process in biological systems. Their formation can be inhibited by antioxidants, such as vitamin E, structural separation or low oxygen tension.Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.Bradykinin: A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.gamma-Linolenic Acid: An omega-6 fatty acid produced in the body as the delta 6-desaturase metabolite of linoleic acid. It is converted to dihomo-gamma-linolenic acid, a biosynthetic precursor of monoenoic prostaglandins such as PGE1. (From Merck Index, 11th ed)Fatty Acid Desaturases: A family of enzymes that catalyze the stereoselective, regioselective, or chemoselective syn-dehydrogenation reactions. They function by a mechanism that is linked directly to reduction of molecular OXYGEN.Lysophosphatidylcholines: Derivatives of PHOSPHATIDYLCHOLINES obtained by their partial hydrolysis which removes one of the fatty acid moieties.Phosphatidylcholines: Derivatives of phosphatidic acids in which the phosphoric acid is bound in ester linkage to a choline moiety. Complete hydrolysis yields 1 mole of glycerol, phosphoric acid and choline and 2 moles of fatty acids.Epoxide Hydrolases: Enzymes that catalyze reversibly the formation of an epoxide or arene oxide from a glycol or aromatic diol, respectively.5-Lipoxygenase-Activating Proteins: Scaffolding proteins that play an important role in the localization and activation of 5-LIPOXYGENASE.Phosphatidic Acids: Fatty acid derivatives of glycerophosphates. They are composed of glycerol bound in ester linkage with 1 mole of phosphoric acid at the terminal 3-hydroxyl group and with 2 moles of fatty acids at the other two hydroxyl groups.Cyclohexanones: Cyclohexane ring substituted by one or more ketones in any position.Melitten: Basic polypeptide from the venom of the honey bee (Apis mellifera). It contains 26 amino acids, has cytolytic properties, causes contracture of muscle, releases histamine, and disrupts surface tension, probably due to lysis of cell and mitochondrial membranes.Glycerides: GLYCEROL esterified with FATTY ACIDS.Linolenic Acids: Eighteen-carbon essential fatty acids that contain three double bonds.Lipoxins: Trihydroxy derivatives of eicosanoic acids. They are primarily derived from arachidonic acid, however eicosapentaenoic acid derivatives also exist. Many of them are naturally occurring mediators of immune regulation.Cell Line: Established cell cultures that have the potential to propagate indefinitely.alpha-Linolenic Acid: A fatty acid that is found in plants and involved in the formation of prostaglandins.Type C Phospholipases: A subclass of phospholipases that hydrolyze the phosphoester bond found in the third position of GLYCEROPHOSPHOLIPIDS. Although the singular term phospholipase C specifically refers to an enzyme that catalyzes the hydrolysis of PHOSPHATIDYLCHOLINE (EC 3.1.4.3), it is commonly used in the literature to refer to broad variety of enzymes that specifically catalyze the hydrolysis of PHOSPHATIDYLINOSITOLS.Ionophores: Chemical agents that increase the permeability of biological or artificial lipid membranes to specific ions. Most ionophores are relatively small organic molecules that act as mobile carriers within membranes or coalesce to form ion permeable channels across membranes. Many are antibiotics, and many act as uncoupling agents by short-circuiting the proton gradient across mitochondrial membranes.Linoleoyl-CoA Desaturase: An enzyme that catalyzes the syn-dehydrogenation of linoleol-CoA gamma-linolenoyl-CoA. It was formerly characterized as EC 1.14.99.25.Oxygenases: Oxidases that specifically introduce DIOXYGEN-derived oxygen atoms into a variety of organic molecules.Intramolecular Oxidoreductases: Enzymes of the isomerase class that catalyze the oxidation of one part of a molecule with a corresponding reduction of another part of the same molecule. They include enzymes converting aldoses to ketoses (ALDOSE-KETOSE ISOMERASES), enzymes shifting a carbon-carbon double bond (CARBON-CARBON DOUBLE BOND ISOMERASES), and enzymes transposing S-S bonds (SULFUR-SULFUR BOND ISOMERASES). (From Enzyme Nomenclature, 1992) EC 5.3.Prostaglandin Endoperoxides, Synthetic: Synthetic compounds that are analogs of the naturally occurring prostaglandin endoperoxides and that mimic their pharmacologic and physiologic activities. They are usually more stable than the naturally occurring compounds.Cyclooxygenase 2 Inhibitors: A subclass of cyclooxygenase inhibitors with specificity for CYCLOOXYGENASE-2.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.Rats, Inbred Strains: Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.Receptors, Thromboxane: Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.Naphthalenes: Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.Signal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Thrombin: An enzyme formed from PROTHROMBIN that converts FIBRINOGEN to FIBRIN.Endocannabinoids: Fatty acid derivatives that have specificity for CANNABINOID RECEPTORS. They are structurally distinct from CANNABINOIDS and were originally discovered as a group of endogenous CANNABINOID RECEPTOR AGONISTS.15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid: A stable prostaglandin endoperoxide analog which serves as a thromboxane mimetic. Its actions include mimicking the hydro-osmotic effect of VASOPRESSIN and activation of TYPE C PHOSPHOLIPASES. (From J Pharmacol Exp Ther 1983;224(1): 108-117; Biochem J 1984;222(1):103-110)Fish Oils: Oils high in unsaturated fats extracted from the bodies of fish or fish parts, especially the LIVER. Those from the liver are usually high in VITAMIN A. The oils are used as DIETARY SUPPLEMENTS. They are also used in soaps and detergents and as protective coatings.Dietary Fats, Unsaturated: Unsaturated fats or oils used in foods or as a food.N-Formylmethionine Leucyl-Phenylalanine: A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated.Lipoxygenases: Dioxygenases that catalyze the peroxidation of methylene-interrupted UNSATURATED FATTY ACIDS.Phosphatidylethanolamines: Derivatives of phosphatidic acids in which the phosphoric acid is bound in ester linkage to an ethanolamine moiety. Complete hydrolysis yields 1 mole of glycerol, phosphoric acid and ethanolamine and 2 moles of fatty acids.Seminal Vesicles: A saclike, glandular diverticulum on each ductus deferens in male vertebrates. It is united with the excretory duct and serves for temporary storage of semen. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Prostaglandin D2: The principal cyclooxygenase metabolite of arachidonic acid. It is released upon activation of mast cells and is also synthesized by alveolar macrophages. Among its many biological actions, the most important are its bronchoconstrictor, platelet-activating-factor-inhibitory, and cytotoxic effects.Anthralin: An anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially PSORIASIS. It may cause FOLLICULITIS.Oleic Acid: An unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. (Stedman, 26th ed)Ibuprofen: A nonsteroidal anti-inflammatory agent with analgesic properties used in the therapy of rheumatism and arthritis.Prostaglandin Antagonists: Compounds that inhibit the action of prostaglandins.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Isoprostanes: A series of prostaglandin-like compounds that are produced by the attack of free-radical species on unsaturated fatty acids, especially ARACHIDONIC ACID, of cellular MEMBRANES. Once cleaved from the lipid membrane by the action of phospholipases they can circulate into various bodily fluids and eventually be excreted. Although these compounds resemble enzymatically synthesized prostaglandins their stereoisometric arrangement is usually different than the "naturally occurring" compounds.Chromatography, Gas: Fractionation of a vaporized sample as a consequence of partition between a mobile gaseous phase and a stationary phase held in a column. Two types are gas-solid chromatography, where the fixed phase is a solid, and gas-liquid, in which the stationary phase is a nonvolatile liquid supported on an inert solid matrix.NitrobenzenesInositol Phosphates: Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID.Macrophages: The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.)TritiumMembrane Lipids: Lipids, predominantly phospholipids, cholesterol and small amounts of glycolipids found in membranes including cellular and intracellular membranes. These lipids may be arranged in bilayers in the membranes with integral proteins between the layers and peripheral proteins attached to the outside. Membrane lipids are required for active transport, several enzymatic activities and membrane formation.Carbon Radioisotopes: Unstable isotopes of carbon that decay or disintegrate emitting radiation. C atoms with atomic weights 10, 11, and 14-16 are radioactive carbon isotopes.Polyunsaturated Alkamides: Amides composed of unsaturated aliphatic FATTY ACIDS linked with AMINES by an amide bond. They are most prominent in ASTERACEAE; PIPERACEAE; and RUTACEAE; and also found in ARISTOLOCHIACEAE; BRASSICACEAE; CONVOLVULACEAE; EUPHORBIACEAE; MENISPERMACEAE; POACEAE; and SOLANACEAE. They are recognized by their pungent taste and for causing numbing and salivation.Peroxides: A group of compounds that contain a bivalent O-O group, i.e., the oxygen atoms are univalent. They can either be inorganic or organic in nature. Such compounds release atomic (nascent) oxygen readily. Thus they are strong oxidizing agents and fire hazards when in contact with combustible materials, especially under high-temperature conditions. The chief industrial uses of peroxides are as oxidizing agents, bleaching agents, and initiators of polymerization. (From Hawley's Condensed Chemical Dictionary, 11th ed)Erucic Acids: cis-13-Docosenoic Acids. 22-Carbon monounsaturated, monocarboxylic acids.Mortierella: A genus of zygomycetous fungi of the family Mortierellaceae, order MUCORALES. Its species are abundant in soil and can cause rare infections in humans and animals. Mortierella alpinais is used for production of arachidonic acid.Plasmalogens: GLYCEROPHOSPHOLIPIDS in which one of the two acyl chains is attached to glycerol with an ether alkenyl linkage instead of an ester as with the other glycerophospholipids.Pyrazoles: Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.Chromatography, Thin Layer: Chromatography on thin layers of adsorbents rather than in columns. The adsorbent can be alumina, silica gel, silicates, charcoals, or cellulose. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Leukotriene C4: The conjugation product of LEUKOTRIENE A4 and glutathione. It is the major arachidonic acid metabolite in macrophages and human mast cells as well as in antigen-sensitized lung tissue. It stimulates mucus secretion in the lung, and produces contractions of nonvascular and some VASCULAR SMOOTH MUSCLE. (From Dictionary of Prostaglandins and Related Compounds, 1990)Lipid Metabolism: Physiological processes in biosynthesis (anabolism) and degradation (catabolism) of LIPIDS.Terpenes: A class of compounds composed of repeating 5-carbon units of HEMITERPENES.Endothelium, Vascular: Single pavement layer of cells which line the luminal surface of the entire vascular system and regulate the transport of macromolecules and blood components.Platelet Activation: A series of progressive, overlapping events, triggered by exposure of the PLATELETS to subendothelial tissue. These events include shape change, adhesiveness, aggregation, and release reactions. When carried through to completion, these events lead to the formation of a stable hemostatic plug.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.1-Acylglycerophosphocholine O-Acyltransferase: An enzyme localized predominantly within the plasma membrane of lymphocytes. It catalyzes the transfer of long-chain fatty acids, preferentially unsaturated fatty acids, to lysophosphatides with the formation of 1,2-diacylglycero-3-phosphocholine and CoA. EC 2.3.1.23.Stearic Acids: A group of compounds that are derivatives of octadecanoic acid which is one of the most abundant fatty acids found in animal lipids. (Stedman, 25th ed)Membrane Proteins: Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.Proadifen: An inhibitor of drug metabolism and CYTOCHROME P-450 ENZYME SYSTEM activity.Mass Spectrometry: An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Virulence Factors, Bordetella: A set of BACTERIAL ADHESINS and TOXINS, BIOLOGICAL produced by BORDETELLA organisms that determine the pathogenesis of BORDETELLA INFECTIONS, such as WHOOPING COUGH. They include filamentous hemagglutinin; FIMBRIAE PROTEINS; pertactin; PERTUSSIS TOXIN; ADENYLATE CYCLASE TOXIN; dermonecrotic toxin; tracheal cytotoxin; Bordetella LIPOPOLYSACCHARIDES; and tracheal colonization factor.AcetophenonesF2-Isoprostanes: Isoprostanes derived from the free radical oxidation of ARACHIDONIC ACID. Although similar in structure to enzymatically synthesized prostaglandin F2alpha (DINOPROST), they occur through non-enzymatic oxidation of cell membrane lipids.Catechols: A group of 1,2-benzenediols that contain the general formula R-C6H5O2.Cyclic AMP: An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.Substrate Specificity: A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.Muscle, Smooth, Vascular: The nonstriated involuntary muscle tissue of blood vessels.Stereoisomerism: The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Cattle: Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.Pertussis Toxin: One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.Second Messenger Systems: Systems in which an intracellular signal is generated in response to an intercellular primary messenger such as a hormone or neurotransmitter. They are intermediate signals in cellular processes such as metabolism, secretion, contraction, phototransduction, and cell growth. Examples of second messenger systems are the adenyl cyclase-cyclic AMP system, the phosphatidylinositol diphosphate-inositol triphosphate system, and the cyclic GMP system.Alkaloids: Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed)Sulfonamides: A group of compounds that contain the structure SO2NH2.Anti-Inflammatory Agents, Non-Steroidal: Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions.They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects.Superoxides: Highly reactive compounds produced when oxygen is reduced by a single electron. In biological systems, they may be generated during the normal catalytic function of a number of enzymes and during the oxidation of hemoglobin to METHEMOGLOBIN. In living organisms, SUPEROXIDE DISMUTASE protects the cell from the deleterious effects of superoxides.Egtazic Acid: A chelating agent relatively more specific for calcium and less toxic than EDETIC ACID.Group V Phospholipases A2: A subcategory of secreted phospholipases A2 that contains both a negatively charged carboxy-terminal segment and interfacial-binding region specific for PHOSPHATIDYL CHOLINE-containing membranes. This enzyme group may play a role in the release of ARACHIDONIC ACID from phospholipid membranes.Kidney: Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.RNA, Messenger: RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.Lipid Peroxidation: Peroxidase catalyzed oxidation of lipids using hydrogen peroxide as an electron acceptor.Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.Endothelium: A layer of epithelium that lines the heart, blood vessels (ENDOTHELIUM, VASCULAR), lymph vessels (ENDOTHELIUM, LYMPHATIC), and the serous cavities of the body.Lipids: A generic term for fats and lipoids, the alcohol-ether-soluble constituents of protoplasm, which are insoluble in water. They comprise the fats, fatty oils, essential oils, waxes, phospholipids, glycolipids, sulfolipids, aminolipids, chromolipids (lipochromes), and fatty acids. (Grant & Hackh's Chemical Dictionary, 5th ed)Mixed Function Oxygenases: Widely distributed enzymes that carry out oxidation-reduction reactions in which one atom of the oxygen molecule is incorporated into the organic substrate; the other oxygen atom is reduced and combined with hydrogen ions to form water. They are also known as monooxygenases or hydroxylases. These reactions require two substrates as reductants for each of the two oxygen atoms. There are different classes of monooxygenases depending on the type of hydrogen-providing cosubstrate (COENZYMES) required in the mixed-function oxidation.Oxidation-Reduction: A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).Aristolochic Acids: Nitro-phenanthrenes occurring in ARISTOLOCHIACEAE and other plants. They derive from stephanine (APORPHINES) by oxidative ring cleavage. The nitro group is a reactive alkylator (ALKYLATING AGENTS) that binds to biological macromolecules. Ingestion by humans is associated with nephropathy (NEPHRITIS). There is no relationship to the similar named aristolochene (SESQUITERPENES).Receptors, Prostaglandin: Cell surface receptors that bind prostaglandins with high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin receptor subtypes have been tentatively named according to their relative affinities for the endogenous prostaglandins. They include those which prefer prostaglandin D2 (DP receptors), prostaglandin E2 (EP1, EP2, and EP3 receptors), prostaglandin F2-alpha (FP receptors), and prostacyclin (IP receptors).Enzyme Induction: An increase in the rate of synthesis of an enzyme due to the presence of an inducer which acts to derepress the gene responsible for enzyme synthesis.Phosphorylation: The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.Prostaglandins, Synthetic: Compounds obtained by chemical synthesis that are analogs or derivatives of naturally occurring prostaglandins and that have similar activity.Liver: A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.Biological Factors: Endogenously-synthesized compounds that influence biological processes not otherwise classified under ENZYMES; HORMONES or HORMONE ANTAGONISTS.Group X Phospholipases A2: A secreted phospholipase A2 subtype that contains a interfacial-binding region with specificity for PHOSPHATIDYLCHOLINE. This enzyme group may play a role in eliciting ARACHIDONIC ACID release from intact cellular membranes and from LOW DENSITY LIPOPROTEINS. Members of this group bind specifically to PHOSPHOLIPASE A2 RECEPTORS.Fatty Acids, Nonesterified: FATTY ACIDS found in the plasma that are complexed with SERUM ALBUMIN for transport. These fatty acids are not in glycerol ester form.Potassium Channels, Tandem Pore Domain: Potassium channels that contain two pores in tandem. They are responsible for baseline or leak currents and may be the most numerous of all K channels.Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.Stimulation, Chemical: The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.Receptors, Eicosanoid: Cell surface proteins that bind eicosanoids with high affinity and trigger intracellular changes influencing the behavior of cells. Among the eicosanoid receptors are receptors for the prostaglandins, thromboxanes, and leukotrienes.Phospholipases A2, Secretory: A subcategory of phospholipases A2 that are secreted from cells. They are 14 kDa proteins containing multiple disulfide-bonds and access their substrate via an interfacial binding site that interacts with phospholipid membranes. In addition specific PHOSPHOLIPASE A2 RECEPTORS can bind to and internalize the enzymes.Phospholipase D: An enzyme found mostly in plant tissue. It hydrolyzes glycerophosphatidates with the formation of a phosphatidic acid and a nitrogenous base such as choline. This enzyme also catalyzes transphosphatidylation reactions. EC 3.1.4.4.Autacoids: A chemically diverse group of substances produced by various tissues in the body that cause slow contraction of smooth muscle; they have other intense but varied pharmacologic activities.Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.Tin Compounds: Inorganic compounds that contain tin as an integral part of the molecule.Plant Oils: Oils derived from plants or plant products.Isomerism: The phenomenon whereby certain chemical compounds have structures that are different although the compounds possess the same elemental composition. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)

Stimulation of renin release from rabbit renal cortex by arachidonic acid and prostaglandin endoperoxides. (1/3254)

The mechanism by which renal prostaglandins stimulate renin secretion in vivo is unknown. In this in vitro study we measured the effects of activation of the prostaglandin (PG) system on renin release from slices of rabbit renal cortex. The PG precursor arachidonic acid (C20:4), a natural PG endoperoxide (PGG2), two stable synthetic PG endoperoxide analogues (EPA I and II), PGE2, PGF2alpha, and two different PG synthesis inhibitors [indomethacin and 5,8,11,14-eicosatetraynoic acid (ETA)] were used to evaluate the possibility of a direct action of the cortical PG system on renin secretion. Renin release increased significantly with time after addition of C20:4, PGG2, EPA I, and EPA II to the incubation medium. Stimulation of renin release was se-related for C20:4 in concentrations of 0.6 to 4.5 X 10(-6) M, for EPA I in concentrations of 0.7 to 2.8 X 10(-6) M, and for EPA II in concentrations of 1.4 to 14.0 X 10(-6) M. Indomethacin (10(-4) M) and ETA (10(-4) M) significantly decreased basal renin release as well as the renin release stimulated by C20:4 and EPA I. PGE2(10(-12) to 10(-6) M) had no effect on renin release, whereas PGF2alpha (10(-12) to 10(-6) M) decreased renin release in a dose-dependent manner. These data raise the possibility of a direct action of the renal cortical PG system on renin secretion. The results further indicate that stimulation of renin release by C20:4 may depend more specifically on the action of PG endoperoxides than on the primary prostaglandins.  (+info)

Cytosolic phospholipase A2 in rat decidual cells: evidence for its role in decidualization. (2/3254)

We investigated the existence and possible role of cytosolic phospholipase A2 (cPLA2) in rat decidualized uteri. PLA2 activity in the cytosol of a decidualized uterine horn, induced by intraluminal oil infusion, was significantly higher than that in contralateral intact horn. The activity was almost completely depressed by cPLA2 inhibitors including arachidonyl trifluoromethyl ketone (ATK). The immunoreactive signals for cPLA2 were intense in decidua and glandular epithelial cells. In vivo administration of ATK (0.1-100 microg) caused a dose-dependent inhibition of decidualization. These results show the presence of cPLA2 and its probable implication in decidualization in rat uterus.  (+info)

Recent progress in the neurotoxicology of natural drugs associated with dependence or addiction, their endogenous agonists and receptors. (3/3254)

Nicotine in tobacco, tetrahydrocannabinol (delta 9-THC) in marijuana and morphine in opium are well known as drugs associated with dependence or addiction. Endogenous active substances that mimic the effects of the natural drugs and their respective receptors have been found in the mammalian central nervous system (CNS). Such active substances and receptors include acetylcholine (ACh) and the nicotinic ACh receptor (nAChR) for nicotine, anandamide and CB1 for delta 9-THC, and endomorphins (1 and 2) and the mu (OP3) opioid receptor for morphine, respectively. Considerable progress has been made in studies on neurotoxicity, in terms of the habituation, dependence and withdrawal phenomena associated with these drugs and with respect to correlations with endogenous active substances and their receptors. In this article we shall review recent findings related to the neurotoxicity of tobacco, marijuana and opium, and their toxic ingredients, nicotine, delta 9-THC and morphine in relation to their respective endogenous agents and receptors in the CNS.  (+info)

Stage-specific excitation of cannabinoid receptor exhibits differential effects on mouse embryonic development. (4/3254)

Anandamide (N-arachidonoylethanolamine), an arachidonic acid derivative, is an endogenous ligand for both the brain-type (CB1-R) and spleen-type (CB2-R) cannabinoid receptors. We have previously demonstrated that preimplantation mouse embryos express mRNA for these receptors and that the periimplantation uterus contains the highest level of anandamide yet discovered in a mammalian tissue. We further demonstrated that 2-cell mouse embryos exposed to low levels of anandamide (7 nM) or other known cannabinoid agonists in culture exhibit markedly compromised embryonic development to blastocysts and that this effect is mediated by CB1-R. In contrast, the present study demonstrates that blastocysts exposed in culture to the same low levels of cannabinoid agonists exhibited accelerated trophoblast differentiation with respect to fibronectin-binding activity and trophoblast outgrowth. Again, these effects resulted from activation of embryonic CB1-R. There was a differential concentration-dependent effect of cannabinoids on the trophoblast, with an observed inhibition of differentiation at higher doses. These results provide evidence for the first time that cannabinoid effects are differentially executed depending on the embryonic stage and cannabinoid levels in the environment. Since uterine anandamide levels are lowest at the sites of implantation and highest at the interimplantation sites, the new findings imply that site-specific levels of anandamide and/or other endogenous ligands in the uterus may regulate implantation spatially by promoting trophoblast differentiation at the sites of blastocyst implantation.  (+info)

A role for N-arachidonylethanolamine (anandamide) as the mediator of sensory nerve-dependent Ca2+-induced relaxation. (5/3254)

We tested the hypothesis that an endogenous cannabinoid (CB) receptor agonist, such as N-arachidonylethanolamine (anandamide), is the transmitter that mediates perivascular sensory nerve-dependent Ca2+-induced relaxation. Rat mesenteric branch arteries were studied using wire myography; relaxation was determined after inducing contraction with norepinephrine. Cumulative addition of Ca2+ caused dose-dependent relaxation (ED50 = 2.2 +/- 0.09 mM). The relaxation was inhibited by 10 mM TEA and 100 nM iberiotoxin, a blocker of large conductance Ca2+-activated K+ channels, but not by 5 microM glibenclamide, 1 mM 4-aminopyridine, or 30 nM apamin. Ca2+-induced relaxation was also blocked by the selective CB receptor antagonist SR141716A and was enhanced by pretreatment with 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride (pefabloc; 30 microM), an inhibitor of anandamide metabolism. Anandamide also caused dose-dependent relaxation (ED50 =.72 +/- 0.3 microM). The relaxation was not inhibited by endothelial denudation, 10 microM indomethacin, or 1 microM miconazole, but was blocked by 3 microM SR141716A, 10 mM TEA, precontraction with 100 mM K+, and 100 nM iberiotoxin, and was enhanced by treatment with 30 microM pefabloc. Mesenteric branch arteries were 200-fold more sensitive to the relaxing action of anandamide than arachidonic acid (ED50 = 160 +/- 7 microM). These data show that: 1) Ca2+ and anandamide cause hyperpolarization-mediated relaxation of mesenteric branch arteries, which is dependent on an iberiotoxin-sensitive Ca2+-activated K+ channel, 2) relaxation induced by both Ca2+ and anandamide is inhibited by CB receptor blockade, and 3) relaxation induced by anandamide is not dependent on its breakdown to arachidonic acid and subsequent metabolism. These findings support the hypothesis that anandamide, or a similar cannabinoid receptor agonist, mediates nerve-dependent Ca2+-induced relaxation in the rat.  (+info)

Inhibition of the production of endothelium-derived hyperpolarizing factor by cannabinoid receptor agonists. (6/3254)

1. The endogenous cannabinoid, anandamide, has been reported to induce an 'endothelium-derived hyperpolarizing factor (EDHF)-like' relaxation in vitro. We therefore investigated the effects of cannabinoid CB1 receptor agonists; HU 210, delta9-tetrahydrocannabinol (delta9-THC) and anandamide, and a CB1 antagonist/inverse agonist, SR 141716A, on nitric oxide (NO) and EDHF-mediated relaxation in precontracted rings of porcine coronary, rabbit carotid and mesenteric arteries. 2. In rings of mesenteric artery HU 210 and delta9-THC induced endothelium- and cyclo-oxygenase-independent relaxations which were sensitive to SR 141716A. Anandamide (0.03-30 microM) induced a slowly developing, endothelium-independent relaxation which was abolished by diclofenac and was therefore mediated by cyclo-oxygenase product(s). None of the CB1 agonists tested affected the tone of precontracted rings of rabbit carotid or porcine coronary artery. 3. In endothelium-intact segments, HU 210, delta9-THC and anandamide did not affect NO-mediated responses but under conditions of continuous NO synthase/cyclo-oxygenase blockade, significantly inhibited acetylcholine and bradykinin-induced relaxations which are attributed to the production of EDHF. The effects of HU 210 and delta9-THC were not observed when experiments were performed in the presence of SR 141716A suggesting the involvement of the CB1 receptor. 4. In a patch clamp bioassay of EDHF production, HU 210 decreased the EDHF-mediated hyperpolarization of detector smooth muscle cells when applied to the donor segment but was without effect on the membrane potential of detector cells. The inhibition of EDHF production was unrelated to alterations in Ca2+ -signalling or cytochrome P450 activity. 5. These results suggest that the activation of endothelial CB1 receptors appears to be negatively coupled to the production of EDHF.  (+info)

Insulin but not growth hormone stimulates protein anabolism in skin wound and muscle. (7/3254)

We have measured protein kinetics in the scalded skin and normal muscle in anesthetized rabbits. On the 7th day after ear scald, L-[ring-13C6]phenylalanine was infused as a tracer, and the ear and hindlimb were used as arteriovenous units to reflect skin and muscle protein kinetics. Insulin was infused at 0.6 or 2.3-3.4 mU. kg-1. min-1 in the low-dose and high-dose insulin groups. In the growth hormone group, recombinant human growth hormone was administered at 2 mg. kg-1. day-1 after the ear was scalded. The results were compared with a control group in which the ear was scalded but otherwise was not treated. In the control group, net protein loss in the scalded skin and muscle was 23.1 +/- 21.4 and 3.9 +/- 1.5 micromol. 100 g-1. h-1, respectively. Insulin infusion at either high or low dose reduced net protein loss to near zero by inhibiting proteolysis. In contrast, growth hormone treatment had no anabolic effect on either tissue. In conclusion, insulin but not growth hormone has an anabolic effect on scalded skin and normal muscle; low-dose insulin is as effective in achieving an anabolic effect on both tissues, with less hypoglycemic response than high-dose insulin.  (+info)

Fatty-acid amide hydrolase is expressed in the mouse uterus and embryo during the periimplantation period. (8/3254)

Arachidonoylethanolamide (anandamide) is an endogenous ligand for cannabinoid receptors. We demonstrated previously that the periimplantation mouse uterus has high levels of anandamide and can synthesize and hydrolyse anandamide. In the present investigation, we examined the expression of the recently identified fatty-acid amide hydrolase (FAAH) gene, which is involved in hydrolyzing anandamide to arachidonic acid and ethanolamine, in the periimplantation mouse embryo and uterus. As previously reported, Northern blot hybridization detected a transcript of approximately 2.5 kilobases of FAAH mRNA in whole uterine poly(A)+ RNA samples. The levels of this mRNA were higher in the liver and brain than in the uterus. In the uterus, higher accumulation of FAAH mRNA occurred on Days 1-4 followed by declines on later days (Days 5-8) of pregnancy. In situ hybridization detected this mRNA primarily in uterine luminal and glandular epithelial cells on Days 1-4 of pregnancy. With the progression of implantation (Days 5-8), accumulation of this mRNA was retained in the luminal and glandular epithelia. In addition, implanting blastocysts showed accumulation of this mRNA. FAAH mRNA accumulation was absent or minimal in the myometrium during this period. Western blotting detected an approximately 60-kDa protein in uterine membrane preparations. In preimplantation embryos, FAAH mRNA was present in one-cell and two-cell embryos but was absent in embryos at the eight-cell/morula stage. However, this mRNA was again detected in Day 4 blastocysts. The presence of FAAH mRNA in one- and two-cell embryos reflects accumulation of maternal message, while its presence in blastocysts reflects embryonic gene activation. Collectively, our present and previous results provide evidence that FAAH is expressed in the mouse uterus and embryo during early pregnancy to modulate local levels of anandamide that could be important for embryo development and implantation.  (+info)

Sodium arachidonate, 10(-5) g/kg per minute, was infused into the renal artery of a nonfiltering canine kidney in situ in order to determine the effects of enhanced prostaglandin synthesis on renal blood flow and its distribution in circumstances where prostaglandins produced in the medulla could not gain access to the cortex via tubular fluid. The contralateral normal kidney was also infused with sodium arachidonate and served as control. Radioactive microspheres were used to calculate the hemodynamic effects. In the nonfiltering kidney, the total renal blood flow increased after sodium arachidonate from a mean of 105 ml/min per 100 g to 146 ml/min per 100 g (P less than 0.01). This increase was completely abolished by prior treatment with indomethacin, 8 mg/kg, intravenously. The normal kidney responded qualitatively the same as the nonfiltering side. In both kidneys, blood flow increased significantly to all cortical zones except the outermost (zone 1), but the fractional distribution of ...
N-arachidonoyl glycine (NAGly) is an endogenous signaling lipid with a wide variety of biological activity whose biosynthesis is poorly understood. Two primary biosynthetic pathways have been proposed. One suggests that NAGly is formed via an enzymatically regulated conjugation of arachidonic acid (AA) and glycine. The other suggests that NAGly is an oxidative metabolite of the endogenous cannabinoid, anandamide (AEA), through an alcohol dehydrogenase. Here using both in vitro and in vivo assays measuring metabolites with LC/MS/MS we test the hypothesis that both pathways are present in mammalian cells. The metabolic products of deuterium-labeled AEA, D4AEA (deuterium on ethanolamine), indicated that NAGly is formed by the oxidation of the ethanolamine creating a D2NAGly product in both RAW 264.7 and C6 glioma cells. Significantly, D4AEA produced a D0NAGly product only in C6 glioma cells suggesting that the hydrolysis of AEA yielded AA that was used preferentially in a conjugation reaction. Addition of
Definition of Arachidonic acid cascade with photos and pictures, translations, sample usage, and additional links for more information.
Purified human monocytes release and metabolize endogenous arachidonic acid (20:4) from phospholipid stores when challenged with particulate inflammatory stimuli or the calcium ionophore A23187. Using radiolabeled cultures, the percentage of total [3H]20:4 released was similar with each type of stimulus. However, the spectrum of 20:4 metabolites differed. With opsonized zymosan (OpZ) or Sephadex beads coated with IgG immune complexes (Ig-beads), the predominant product was thromboxane (25% of the total) together with smaller amounts of other cyclo-oxygenase products and lipoxygenase metabolites. Levels of thromboxane synthesis by monocytes were comparable to those by platelets, as measured by radioimmunoassay. In contrast, exposure to the nonspecific agent A23187 led to mainly lipoxygenase products (70% of the total). Monocytes isolated from mononuclear cell fractions of peripheral blood contain platelets specifically rosetted to their surfaces. These platelet contaminants were removed by ...
It is well recognized that the CYP-derived eicosanoids constitute a new member of the arachidonic acid cascade with important implications in the regulation of physiological and pathophysiological processes. These metabolites are formed endogenously in various tissues and exert potent biological effects on cellular functions. Studies of their role in normal and diseased cells and tissues are impeded by the difficulty in selectively targeting their synthesis or their effects, because these metabolites are generated from multiple closely related proteins of the CYP superfamily. Consequently, the development of enzyme inhibitors that target specific isoforms/reactions should aid in the study of their pathophysiological roles.. We have synthesized a series of fatty acid/arachidonic acid analogs and tested their potency and selectivity in inhibiting arachidonic acid epoxidation and ω-hydroxylation reactions in rat renal microsomes. Our study confirms that the widely used, terminal acetylenic ...
BioAssay record AID 3623 submitted by ChEMBL: Inhibition of [14C]arachidonic acid conversion to 5-HETE by broken cell 5-LO isolated from guinea pig PMN.
N-arachidonoyl-dopamine tunes synaptic transmission onto dopaminergic neurons by activating both cannabinoid and vanilloid receptors.: In the present study, we
just read a article about arachidonic acid,,,had sum great info on it,,,,was wondering if anyone here uses it while on / off cycle and does it really work or is
BioAssay record AID 274914 submitted by ChEMBL: Activity at COX1 assessed as inhibition of arachidonic acid-induced PGE2 production in J774 cells at 0.01 uM.
Arachidonic Acids Role in Stress and Shock April 3, 2012 Posted in General.. Comments Off on Arachidonic Acids Role in Stress and Shock ...
ethyl arachidonate 1808-26-0 NMR spectrum, ethyl arachidonate H-NMR spectral analysis, ethyl arachidonate C-NMR spectral analysis ect.
Scientists in Cambridge have discovered that a brain protein called syntaxin enables fatty molecules, used widely in health supplements, to work in the brain to make it function properly. Lead Scientist, Dr Bazbek Davletov and his colleague Dr Colin Rickman from the Medical Research Council (MRC) Laboratory of Molecular Biology in Cambridge, UK report their findings in the journal Chemistry and Biology.. ...
Dumex Dulac Boouc 1 information about active ingredients, pharmaceutical forms and doses by Danone, Dumex Dulac Boouc 1 indications, usages and related health products lists
AuxInfo=1/1/N:1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,19,20,21,22/E:(21,22)/rA:22nCCCCCCCCCCCCCCCCCCCCOO/rB:s1;s2;s3;s4;s5;d6;s7;s8;d9;s10;s11;d12;s13;s14;d15;s16;s17;s18;s19;s20;d20;/rC:-7.3658,-.6188,0;-6.6513,-.2062,0;-5.9368,-.6188,0;-5.2224,-.2062,0;-4.5079,-.6188,0;-3.7934,-.2062,0;-2.9684,-.2062,0;-2.2539,-.6188,0;-1.5395,-.2062,0;-.7145,-.2062,0;0,-.6188,0;.7145,-.2062,0;1.5395,-.2062,0;2.2539,-.6188,0;2.9684,-.2062,0;3.7934,-.2062,0;4.5079,-.6188,0;5.2224,-.2062,0;5.9368,-.6188,0;6.6513,-.2062,0;7.3658,-.6188,0;6.6513,.6188,0 ...
N-Arachidonoyl dopamine (NADA) is an endocannabinoid that acts as an agonist of the CB1 receptor and the transient receptor potential V1 (TRPV1) ion channel. NADA was first described as a putative endocannabinoid (agonist for the CB1 receptor) in 2000 and was subsequently identified as an endovanilloid (agonist for TRPV1) in 2002. NADA is an endogenous arachidonic acid based lipid found in the brain of rats, with especially high concentrations in the hippocampus, cerebellum, and striatum. It activates the TRPV1 channel with an EC50 of approximately of 50nM which makes it the putative endogenous TRPV1 agonist. In mice, NADA was shown to induce the tetrad of physiological paradigms associated with cannabinoids: hypothermia, hypo-locomotion, catalepsy, and analgesia. NADA has been found to play a regulatory role in both the peripheral and central nervous systems, and displays antioxidant and neuroprotectant properties. NADA has also been implicated in smooth muscle contraction and vasorelaxation in ...
Arachidonic acid supplementation in daily doses of 1,000-1,500 mg for 50 days has been well tolerated during several clinical studies, with no significant side effects reported. All common markers of health, including kidney and liver function,[35] serum lipids,[39] immunity,[40] and platelet aggregation[34] appear to be unaffected with this level and duration of use. Furthermore, higher concentrations of ARA in muscle tissue may be correlated with improved insulin sensitivity.[41] Arachidonic acid supplementation of the diets of healthy adults appears to offer no toxicity or significant safety risk. While studies looking at arachidonic acid supplementation in sedentary subjects have failed to find changes in resting inflammatory markers in doses up to 1,500 mg daily, strength-trained subjects may respond differently. One study reported a significant reduction in resting inflammation (via marker IL-6) in young men supplementing 1,000 mg/day of arachidonic acid for 50 days in combination with ...
A recognized feature of psoriasis and other proliferative dermatoses is accumulation in your skin from the unusual arachidonic acidity metabolite, 12hydrogen through the 10-carbon of arachidonate. included regions of epidermis in psoriasis possess PPARG improved concentrations of free of charge arachidonic acid and 12-HETE markedly. Chiral analysis from the 12-HETE in psoriasis revealed that the major enantiomer is 12390C404, encompassing the major M-PFB ions at 391 (unlabeled HETE) and 399 (d8 analogue), essentially as described previously (28). Experiments with Stereospecifically Labeled Arachidonic Acids. The specific activities of the two 10-3H-labeled arachidonic acids were approximately 10,000C20,000 disintegrations per min 3H per g. The pro-[10-3H]arachidonic acid was enriched in tritium by incubation with an 8as described in principle before (29). The stereospecifically labeled arachidonic acids were admixed with [14C]arachidonic acid, which served as an internal standard for measurement ...
In the present study, we investigated whether the protective effect of FK506 and cyclosporin A (CsA) against in vitro ischemic injury of astrocytes might be mediated through attenuation of cytosolic isoform of phospholipase A(2) (cPLA(2)) expression and activity as well as inhibition of arachidonic acid (AA) release. On the 21st day in vitro, cultures of rat astrocytes were subjected to ischemia-simulating conditions (combined oxygen glucose deprivation) for 8 h and exposed to FK506 (10 - 1,000 nM) and CsA (0.25 - 10 microM). Obtained data suggest the cross-talk between the action of 0.25 - 10 microM CsA as well as 1 microM FK506 on calcineurin (CaN) and cPLA(2) in anti-apoptotic signal transduction pathways. Moreover, we have shown that immunosuppressants at these concentrations protected glial cells against ischemia-induced apoptosis through the increase of cell viability, mitochondrial function restoration, and attenuation of oxidative stress. Finally, in our study, low concentrations of FK506 (10
BECA, T; HERNANDEZ, G y BASCONES, A. NSAIDs in the treatment of periodontal disease. Avances en Periodoncia [online]. 2007, vol.19, n.2, pp.101-113. ISSN 2340-3209.. SUMMARY A review about the application of antiinflammatories as an aid for the periodontal treatment is presented. After a brief introduction, we explain the immunological bases of periodontal inflamation and tissue destruction, focusing on arachidonic acid metabolism and the four most important inflammatory mediators now in periodontal tissue resorption: prostaglandin E2 (PGE2), prostaglandin F2a(PGF2a), leucotriene B4 (LTB4) and platelet activation factor (PAF), and explaining their actions and role in inflammation through matrix metalloproteinase (MMPs) and their relation with some other mediators in the inflammatory chain also related with tissue resorption. After, we expound some of the most used drugs for the inhibition of all of these mediators (non-steroid antiinflammatory drugs or NSAIDs, omega3 fatty acids, tetracyclines ...
Yau, T M. and Sun, G Y., "The metabolism of (1-14c)arachidonic acid in the neutral glycerides and phosphoglycerides of mouse brain." (1974). Subject Strain Bibliography 1974. 89 ...
This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and is thought to be the predominant enzyme responsible for epoxidation of endogenous arachidonic acid in cardiac tissue. Multiple transcript variants have been found for this gene. [provided by RefSeq, Jan 2016 ...
Mancuso, P.; Mcnish, R.W.; Peters Golden, M.; Brock, T.G., 2001: Evaluation of phagocytosis and arachidonate metabolism by alveolar macrophages and recruited neutrophils from F344xBN rats of different ages
TY - CONF. T1 - Factors that protect HepG2 cells by anandamide-induced cell death. AU - Giuliano, Michela. AU - Calvaruso, Giuseppe. AU - Pellerito, Ornella. PY - 2006. Y1 - 2006. UR - http://hdl.handle.net/10447/10954. M3 - Other. SP - 45. EP - 54. ER - ...
InChI=1S/C22H36ClNO/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-22(25)24-21-20-23/h6-7,9-10,12-13,15-16H,2-5,8,11,14,17-21H2,1H3,(H,24,25)/b7-6-,10-9-,13-12-,16-15- ...
Series three - made from EPA. The number one function of series 3 prostaglandins is to save you Arachidonic Acid release from cells.. Arachidonic Acid passing thru this pathway will increase irritation and the other problems noted in Series 2. Anything we will do to decrease interest because of the AA pathway is beneficial.. Remember that Omega-threes & Omega-6s can undergo the equal pathway. The Omega-3s are transformed at a lower charge resulting in a decrease quantity. The merchandise of this pathway are then degraded by enzymes.. This machine, like many in the frame, is in constant stability. However, once in a while the manufacturing exceeds metabolism resulting in accelerated inflammation. Omega-3s are inflammatory but to a lesser quantity. Additionally, theyre produced slower ensuing in fewer numbers. This is one of the many blessings of Omega-three fatty acids.. ...
Dutch Lady Step 2 information about active ingredients, pharmaceutical forms and doses by Dutch Lady Milk Industries, Dutch Lady Step 2 indications, usages and related health products lists
Principal Investigator:MAIZUMI Yuji, Project Period (FY):1998 - 1999, Research Category:Grant-in-Aid for Scientific Research (C), Section:一般, Research Field:Biological pharmacy
Check out Boardwalk® Vandalism Mark Remover BWK351AEA and other inexpensive Cleaning Products with friendly customer service from OnTimeSupplies.com!
A new way to enhance the effects of anandamide - a natural, marijuana-like chemical in the body has been identified by Italian researchers.
Looking for online definition of 5,8,11,14-Eicosatetraenoic acid in the Medical Dictionary? 5,8,11,14-Eicosatetraenoic acid explanation free. What is 5,8,11,14-Eicosatetraenoic acid? Meaning of 5,8,11,14-Eicosatetraenoic acid medical term. What does 5,8,11,14-Eicosatetraenoic acid mean?
1. Since ageing has been associated with a decrease in both immune responses and antioxidant defences, this study was undertaken to compare the glutathione peroxidase activity in peripheral blood mononuclear cells of healthy elderly and young donors. The mean value of glutathione peroxidase activity was significantly lower in the aged group (−36%) than that observed in the young control group (n = 10).. 2. This defect was accompanied by a marked increase (+106%) in the oxygenated metabolism of endogenous arachidonic acid by lipoxygenases as judged by the radiolabel associated with hydroxyeicosatetraenoic acids in [3H]arachidonic acid-prelabelled peripheral blood mononuclear cells, whereas the cyclo-oxygenase activity, estimated by the radiolabel associated with thromboxane B2, was not significantly altered.. 3. Upon stimulation by the mitogenic lectin concanavalin A, the radioactivity associated with total eicosanoids (free arachidonic acid plus hydroxyeicosatetraenoic acids plus thromboxane ...
TY - JOUR. T1 - Arachidonic acid inhibits luteinizing hormone-stimulated progesterone production in hen granulosa cells. AU - Johnson, A. L.. AU - Tilly, J. L.. PY - 1990/1/1. Y1 - 1990/1/1. N2 - Arachidonic acid has been proposed to function as a hormone-induced second messenger in a variety of mammalian endocrine tissues. The present studies were conducted to evaluate whether arachidonic acid, either added exogenously or released endogenously following treatment with physiologic (phospholipase A2) or pharmacologic (melittin) agents, influences basal and/or luteinizing hormone (LH)-induced cyclic adenosine 3,5-monophosphate (cAMP) and progesterone production in granulosa cells from domestic hens. Phospholipase A2 (PLA2) and melittin treatments failed to alter basal concentrations of progesterone, whereas arachidonic acid had a slight stimulatory effect (only at the 50-μM dose) on progesterone levels, and no effect on cAMP. By contrast, arachidonic acid, PLA2, and melittin each inhibited ...
It would seem that PGE2 ethanolamide has a similar profile of action to that of PGE2 in that it binds to EP1, EP2, EP3, and EP4 receptors. The affinity of PGE2 ethanolamide for EP receptor subtypes is significantly lower than that of PGE2, being 500-, 500-, 440-, and 651-fold lower than that of PGE2 for hEP1, hEP2, hEP3, and hEP4 receptors, respectively. The inclusion of the FAAH inhibitor PMSF did not alter theKi values for either PGE2 or PGE2 ethanolamide. This suggests that PGE2 ethanolamide is acting on the receptor directly rather than being cleaved to form PGE2. It is notable that Kozak et al. (2001) have demonstrated that PGE2 ethanolamide is subject to little or no hydrolysis in rat or human blood. It has been previously demonstrated that anandamide and other ethanolamides have significant affinity for the vanilloid VR1 receptor (Smart et al., 2000; Ross et al., 2001). However in this study, PGE2ethanolamide seemed to have limited affinity for the VR1 receptor with a Ki value of ,10 μM, ...
The subject of N-acyl amino acid conjugates has been rapidly growing in recent years, especially with regard to their analgesic and anti-inflammatory actions. The field is comprised of a large family of lipid signaling molecules whose importance is only now being fully realized. The most widely studied member is N-arachidonoyl glycine (NAGly), which differs structurally from the endocannabinoid anandamide (N-arachidonoyl ethanolamide) by a single oxygen atom and the two are metabolically related. Topics that are covered in this mini review are: biosynthetic pathways for N-acyl amino acids, receptors for N-acyl amino acids, physiological actions of N-acyl amino acids, pharmacological effects of N-acyl amino acids and molecular mechanisms believed to be responsible for their effects ...
The 5-lipoxygenase (5-LO) product 5-oxo-6,8,11,14-eicosatetraenoic acid (5-oxo-ETE), which is a potent chemoattractant for myeloid cells, is known to promote the survival of prostate cancer cells. In the present study, we found that PC3 prostate cancer cells and cell lines derived from breast (MCF7) and lung (A-427) cancers contain 5-hydroxyeicosanoid dehydrogenase (5-HEDH) activity and have the ability to synthesize 5-oxo-ETE from its precursor 5S-hydroxy-6,8,11,14-eicosatetraenoic acid (5-HETE) when added as an exogenous substrate. H2O2 strongly stimulated the synthesis of 5-oxo-ETE and induced dramatic increases in the levels of both glutathione disulfide and NADP+. The effects of H2O2 on 5-oxo-ETE and NADP+ were blocked by N-ethylmaleimide (NEM), indicating that this effect was mediated by the glutathione reductase-dependent generation of NADP+, the cofactor required by 5-HEDH. 5-Oxo-ETE synthesis was also stimulated by agents that have cytotoxic effects on tumor cells, including ...
It is recommended to use the anandamide supplements if you want to boost your brain capacity. If you want to find the simplest way to increase the anandamide levels in your body then you can eat the dark chocolate. It is possible to regulate the inflammation and neuron signalling with the help of the anandamide supplement. The motivation and happiness can be removed with the help of the cannabinoid receptors in the brain cells. The breakdown of the anandamide supplements can be blocked can be stimulated with the help of the endocannabinoid receptors. The neuron signalling can be regulated in your body based on the inflammation of the anandamide. If you want to get detailed information about the anandamide supplements then you can visit our website. You can prefer to use the supplements if you are ready to make some changes in your life.. Find the right supplements:. The prolonged approach should be followed by the individuals in order to boost the anandamide in your body. The memory and ...
A complex structurally diverse series of eicosanoids arises from the metabolism of arachidonic acid. The metabolic profile is further complicated by the enantioselectivity of eicosanoid formation and the variety of regioisomers that arise. In order to investigate the metabolism of arachidonic acid in vitro or in vivo, targeted methods are advantageous in order to distinguish between the complex isomeric mixtures that can arise by different metabolic pathways. Over the last several years this targeted approach has become more popular, although there are still relatively few examples where chiral targeted approaches have been employed to directly analyze complex enantiomeric mixtures. To efficiently conduct targeted eicosanoid analyses, LC separations are coupled with collision induced dissociation (CID) and tandem mass spectrometry (MS/MS). Product ion profiles are often diagnostic for particular regioisomers. The highest sensitivity that can be achieved involves the use of selected reaction monitoring
Endocannabinoid anandamide induces endothelium-dependent relaxation commonly attributed to stimulation of the G-protein coupled endothelial anandamide receptor. The study addressed the receptor-independent effect of anandamide on large conductance Ca2+-dependent K+ channels expressed in endothelial cell line EA.hy926. Under resting conditions, 10µM anandamide did not significantly influence the resting membrane potential. In a Ca2+-free solution the cells were depolarized by ~10mV. Further administration of 10µM anandamide hyperpolarized the cells by ~8mV. In voltage-clamp mode, anandamide elicited the outwardly rectifying whole-cell current sensitive to paxilline but insensitive to GDPβS, a G-protein inhibitor. Administration of 70µM Mn2+, an agent used to promote integrin clustering, reversibly stimulated whole-cell current, but failed to further facilitate the anandamide-stimulated current. In an inside-out configuration, anandamide (0.1-30µM) facilitated single BKCa channel activity in ...
TY - JOUR. T1 - Chronic exposure to sidestream smoke adversely alters 14C-(AA) arachidonic acid metabolism in platelets and aortas from rats. AU - Lubawy, W. C.. AU - Valentovic, M. A.. PY - 1984/1/1. Y1 - 1984/1/1. UR - http://www.scopus.com/inward/record.url?scp=0021149080&partnerID=8YFLogxK. M3 - Article. AN - SCOPUS:0021149080. VL - 43. SP - no. 2785. JO - Federation Proceedings. JF - Federation Proceedings. SN - 0014-9446. IS - 3. ER - ...
The endocannabinoid system is an important regulator of the nervous, neuroendocrine and immune systems, thus representing a novel therapeutic target for stress-related neuroinflammatory and psychiatric disorders. However, there is a paucity of data relating to the effects of endocannabinoids on neuroinflammatory mediators following an immune stress/challenge in vivo. This study investigated the effects of URB597, a selective inhibitor of fatty acid amine hydrolyase (FAAH), the enzyme that preferentially metabolises anandamide, on lipopolysaccharide (LPS)-induced increases in the expression of immune mediators in the hypothalamus. Systemic administration of URB597 increased the levels of anandamide and the related N-acylethanolamines, N-palmitoyl ethanolamide and N-oleoyl ethanolamide, but not 2-arachidonoyl glycerol, in the hypothalamus and spleen. URB597 attenuated the LPS-induced increase in interleukin (IL)-1Beta expression while concurrently augmenting the LPS-induced increase in suppressor ...
The endocannabinoid system is an important regulator of the nervous, neuroendocrine and immune systems, thus representing a novel therapeutic target for stress-related neuroinflammatory and psychiatric disorders. However, there is a paucity of data relating to the effects of endocannabinoids on neuroinflammatory mediators following an immune stress/challenge in vivo. This study investigated the effects of URB597, a selective inhibitor of fatty acid amine hydrolyase (FAAH), the enzyme that preferentially metabolises anandamide, on lipopolysaccharide (LPS)-induced increases in the expression of immune mediators in the hypothalamus. Systemic administration of URB597 increased the levels of anandamide and the related N -acylethanolamines, N -palmitoyl ethanolamide and N-oleoyl ethanolamide, but not 2-arachidonoyl glycerol, in the hypothalamus and spleen. URB597 attenuated the LPS-induced increase in interleukin (IL)-1? expression while concurrently augmenting the LPS-induced increase in suppressor ...
Arachidonic acid may trigger brain inflammation. High blood levels have been associated with a greater risk of suicide and depressive episodes. On the other hand, diets high in carbohydrate and low in fat and protein (with little or no arachidonic acid) may be associated with lower levels of anxiety and depression, according to epidemiological studies.. In one study, overweight or diabetic employees who went on a whole food, plant-based diet reported increased energy, better sleep patterns and improved mental health compared to a control group given no diet restrictions. Their work productivity also showed improvement.. A similar subsequent study of employees at 10 corporate sites showed notable improvements in depression, anxiety and emotional well-being among those following a meat-free, plant-based diet.. ...
Introduction:. Excessive menstrual bleeding, or menorrhagia, is a common female complaint that may be entirely prevented by a simple herbal prescription - capsules of ginger. The chief cause of functional menorrhagia (i.e., not caused by the presence of uterine fibroids or endometriosis) involves abnormalities in the biochemical processes of the endometrium (the lining of the uterus).. One abnormality commonly found is an alteration in arachidonic acid metabolism. This fatty acid is derived from meat and dairy sources and is converted to hormone-like compounds known as prostaglandins. The endometrium of women who have menorrhagia concentrates arachidonic acid to a much greater extent than normal. The increased arachidonic acid release during menstruation results in increased production of prostaglandin E2 (PGE2), which not only leads to excessive bleeding, but also menstrual cramps.. Background Data:. Historically, the majority of complaints for which ginger (Zingiber officinale) was used ...
Genes Encoding Enzymatic Activities Implicated in the Eicosanoid Cascade of Arachidonic Acid and their Receptors are Expressed at mRNA Levels in Human Meningiomas Abstract.
Lipoxygenases (LOs) constitute a heterogeneous family of enzymes that catalyze the stereoselective dioxygenation of polyunsaturated fatty acids to their corresponding hydroperoxy derivatives.1,2 In mammals, LOs are categorized with respect to their positional specificity of arachidonic acid oxygenation into 5-, 8-, 12-, and 15-LOs.1-3 These enzymes induce structural and metabolic changes in cells during a wide variety of physiological and pathological processes, such as differentiation, carcinogenesis, inflammation, and atherogenesis. Accumulating studies have suggested diverse and opposing roles for the various LO pathways in the pathogenesis of human diseases, particularly cancer and atherosclerosis.2-5 Consistent with the existence of multiple isoforms of LOs, a variety of intermediate and end products of arachidonic acids are found in various cell types, and they in turn activate diverse signaling cascades, resulting in diverse outcomes. Therefore, sophisticated understanding of the ...
In addition to conventional treatment, there are also nutritional means to deal with inflammation. In my practice, I have helped many individuals complaining of pain from various itis diseases. We address the source of the inflammation, rather than attempting to inhibit an enzyme. The real problem may be the over-abundance of Arachidonic acid that is available to enter the PGE2 inflammatory pathway. Therefore, the first step should be to reduce the dietary consumption of Arachidonic acid, which is only found in animal products. Secondly, supplementing with the omega3 fatty acids, such as DHA and EPA, commonly found in fish oil is also beneficial. One important role of omega3 fatty acids is to keep Arachidonic acids from escaping from our own cell membranes. This may account for the anti-inflammatory role that omega three fatty acids are credited with. I have even seen dramatic results when fish oil is used topically over an inflamed area. For example, many have found relief from the pain ...
AACOCF₃ - CAS 149301-79-1 - Calbiochem CAS 149301-79-1 A cell-permeable trifluoromethyl ketone analog of arachidonic acid. - Find MSDS or SDS, a COA, data sheets and more information.
A compound of the formula ##STR1## wherein n is an integer from 2 to 4; m is an integer from 3 to 5; R is OM, OR1 or NR2 R3 where M is a pharmaceutically acceptable cation; R1, R2 and R3 are the same or different and selected from the group consisting of hydrogen, C1 -C12 branched, unbranched or cyclic alkyl, aryl and aralkyl; or R2 and R3 taken together form a group of the formula ##STR2## can be used as an inhibitor of the lipoxygenase pathway of the arachidonic acid cascade in animals.
GPR55, an orphan G‐protein coupled receptor, is activated by lysophosphatidylinositol (LPI) and the endocannabinoid anandamide, as well as by other compounds ...
(2011) Ugajin et al. American Journal of Pathology. Prostaglandin (PG) D2 and PGE2 are arachidonic acid metabolites that are generated though an isomerization reaction catalyzed by PG synthases. PGs have been implicated in immunologic reactions in addition to a wide range of physiological functio...
The IUPHAR/BPS Guide to Pharmacology. anandamide ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
Fatty acid amide hydrolase (FAAH) is responsible for hydrolysis of endocannabinoid, anandamide (AEA), and N-acyl ethanolamines such as palmitoylethanolamine (PEA) and N-oleoylethanolamide (OEA). Genetic deletion or pharmacological inactivation of FAAH shows site-specific elevation of AEA that plays a role in the modulation of pain and other neurodegenerative disorders. The review elaborates recent progress and current status of diverse structural classes of reversible and irreversible FAAH inhibitors. The discussion also addresses ligand-enzyme active site interactions and mechanism of enzyme inactivation, emerging approaches to novel FAAH inhibitors, and ongoing efforts to address gaps in therapeutic utility of FAAH inhibitors.
Anandamide (arachidonoyl ethanolamide, AEA) and 2-arachidonoyl glycerol (2-AG) exert most of their actions by binding to cannabinoid receptors. The effects of the endocannabinoids are short-lived due to rapid cellular accumulation and metabolism, for AEA, primarily by the enzymes fatty acid amide hydrolase (FAAH). This has led to the hypothesis that by inhibition of the cellular processing of AEA, beneficial effects in conditions such as pain and inflammation can be enhanced. The overall aim of the present thesis has been to examine the mechanisms involved in the cellular processing of AEA and how they can be influenced pharmacologically by both synthetic natural compounds.. Liposomes, artificial membranes, were used in paper I to study the membrane retention of AEA. The AEA retention mimicked the early properties of AEA accumulation, such as temperature-dependency and saturability.. In paper II, FAAH was blocked by a selective inhibitor, URB597, and reduced the accumulation of AEA into RBL2H3 ...
As a member of the transient receptor potential (TRP) ion channel superfamily, the ligand-gated ion channel TRPA1 has been implicated in nociceptive function and pain states. The endogenous ligands that activate TRPA1 remain unknown. However, various agonists have been identified, including environmental irritants (e.g., acrolein) and ingredients of pungent natural products [e.g., allyl isothiocyanate (ITC), cinnamaldehyde, allicin, and gingerol]. In general, these agents are either highly reactive, nonselective, or not potent or efficacious, significantly limiting their utilities in the study of TRPA1 channel properties and biological functions. In a search for novel TRPA1 agonists, we identified 3 -carbamoylbiphenyl-3-yl cyclohexylcarbamate (URB597), a potent and systemically active inhibitor of fatty acid amide hydrolase (FAAH). This enzyme is responsible for anandamide degradation and therefore has been pursued as an antinociceptive and antiepileptic drug target. Using Ca influx assays and patch
Trophoblast cells that comprise the placenta play a crucial role in the complex cross-talk between fetus and maternal tissues. Although anandamide and 2-arachidonoylglycerol, the best studied endocannabinoids, affect trophoblast attachment and outgrowth, the functional significance of the endocannabinoid system in the development of placenta has not been established. We investigated the correlation between endocannabinoid levels and the pattern of expression of the receptors and metabolic enzymes of the endocannabinoid system during rat placental development. Here, we showed that all the endocannabinoid machinery is dynamically expressed in the functionally distinct basal and labyrinth zones of the rat placenta. Indeed, endocannabinoid levels are shown to increase with the progression of pregnancy. Together, these data support a role for the endocannabinoid system in normal placental function and evidence for a potential novel cellular target for the deleterious action of cannabis-derived ...
TY - JOUR. T1 - Studies of anandamide accumulation inhibitors in cerebellar granule neurons. T2 - Comparison to inhibition of fatty acid amide hydrolase. AU - Hillard, Cecilia J.. AU - Shi, Leyu. AU - Tuniki, Venugopal Raju. AU - Falck, J R. AU - Campbell, William B.. PY - 2007/9/1. Y1 - 2007/9/1. N2 - The endocannabinoid, N-arachidonylethanolamine (AEA) is accumulated by neurons via a process that has been characterized biochemically but not molecularly. Inhibitors of AEA accumulation have been characterized individually but have not been compared in a single study. Our purpose was to compare the potency of five previously described compounds (AM404, AM1172, VDM11, OMDM-2, and UCM707) both as inhibitors of AEA and N-palmitoylethanolamine (PEA) accumulation by cerebellar granule neurons and as inhibitors of AEA hydrolysis. The compounds all inhibited AEA accumulation; AM404, VDM11 and OMDM-2 with IC50 values of approximately 5 μM, whereas AM1172 and UCM707 exhibited IC50 values of 24 and 30 ...
TY - JOUR. T1 - Mechanism of thrombin-induced arachidonic acid release in osteoblast-like cells. AU - Suzuki, A.. AU - Kozawa, O.. AU - Shinoda, J.. AU - Watanabe-Tomita, Y.. AU - Saito, H.. AU - Oiso, Y.. PY - 1997/6. Y1 - 1997/6. N2 - In a previous study, we have reported that thrombin stimulates phosphatidylcholine hydrolysis by phospholipase (PL) D, but has little effect on phosphoinositide hydrolysis by PLC in osteoblast-like MC3T3-E1 cells. In the present study, we investigated the mechanism of the thrombin-induced arachidonic acid (AA) release in MC3T3-E1 cells. Thrombin stimulated AA release dose dependently in the range between 0.1 and 1 U/ml. Quinacrine, a PLA2 inhibitor, suppressed the thrombin-induced AA release. In addition, quinacrine also suppressed the thrombin-induced prostaglandin E2 synthesis in these cells. On the other hand, propranolol, which is known to inhibit phosphatidic acid phosphohydrolase, did not affect the thrombin-induced AA release. ...
Our endocannabinoid system regulates balance in vital aspects of our biology. When our endocannabinoid system isnt signally and functioning optimally we can suffer from what is called Clinical Endocannabinoid Deficiency (CED).
Fegley, D., Gaetani, S., Duranti, A., Tontini, A., Mor, M. and Tarzia, G. (2005) Characterization of the fatty acid amide hydrolase inhibitor cyclohexyl carbamic acid 3- carbamoyl-biphenyl-3-yl ester (URB597), effects on anandamide and oleoylethanolamide deactivation. Journal of Pharmacology & Experimental Therapeutics, 313, 352-358. doi10.1124/jpet.104.078980
2-Arachidonoylglycerol (2-AG) is a metabolite belonging to the endocannabinoid family. 2-AG is related to palmitoylethanolamide, but seems to have opposite actions in a number if paradigms. It can be released if using ultramicronized PEA as has been described in a recent patent. Recently the endocannabinoid 2-arachidonoyl glycerol was added to cultured chick dorsal root ganglion…
The present findings provide evidence for a novel cardiovascular regulatory mechanism mediated by endocannabinoids acting at CB1, stimulation of which lowers blood pressure through reductions in both cardiac contractility and vascular resistance. In various forms of hypertension, this endocannabinoid system becomes tonically active, probably owing to an upregulation of cardiac and vascular endothelial CB1. Furthermore, increased activation of CB1 through blocking of the metabolic degradation or intracellular uptake of the endocannabinoid anandamide normalizes blood pressure, offering a novel approach for the pharmacotherapy of hypertension.. CB1 antagonists did not affect blood pressure in normotensive rats, and inhibitors of FAAH or anandamide transport were similarly ineffective, which indicates that the cannabinoid system is inactive under normotensive conditions. In contrast, CB1 antagonists elicited sustained further increases in blood pressure in rats with 3 different forms of ...
TY - JOUR. T1 - Cyclooxygenase-2-mediated metabolism of arachidonic acid to 15-oxo-eicosatetraenoic acid by rat intestinal epithelial cells. AU - Seon, Hwa Lee. AU - Rangiah, Kannan. AU - Williams, Michelle V.. AU - Wehr, Angela Y.. AU - DuBois, Raymond N.. AU - Blair, Ian A.. PY - 2007/11. Y1 - 2007/11. N2 - Rat intestinal epithelial cells mat permanently express the cyclooxygenase-2 (COX-2) gene (RIES cells) were used to investigate COX-2-mediated arachidonic acid (AA) metabolism. A targeted chiral lipidomics approach was employed to quantify AA metabolites that were secreted by the cells into the culture media. When intact RIES cells were treated with calcium ionophore A-23187 (1 μM) for 1 h, 11-(R)-hydroxyeicosatetraenoic acid (HETE) was the most abundant metabolite, followed by prostaglandin (PG) E2, 15-(S)-HETE, 15-oxo-eicosatetraenoic acid (ETE), and 15-(R)-HETE. Incubation for a further 23 h after the calcium ionophore was removed resulted in a substantial increase in PGE2 ...
Endogenous cannabinoids (endocannabinoids) serve as retrograde messengers at synapses in various regions of the brain. The family of endocannabinoids includes at least five derivatives of arachidonic acid; the two best characterized are arachydonoyl ethanolamide (anandamide, AEA) and 2-arachydonoil glycerol (2AG). They are released from postsynaptic neurons upon postsynaptic depolarization and/or receptor activation. The released endocannabinoids then activate the CB1 receptors (CB1R) at presynaptic terminals and suppress the release of inhibitory transmitter GABA (depolarization-induced suppression of inhibition, DSI) or excitatory transmitter glutamate (depolarization-induced suppression of excitation, DSE) by inhibiting Ca2+ channels. Besides the well-known expression of the CB1R in the plasma membrane, this receptor is also present in mitochondrial membranes, where it reduces the mitochondrial respiration and contributes to DSI. Whereas DSI and DSE result in short-term synaptic plasticity, ...
TY - JOUR. T1 - Arachidonic acid increases intracellular calcium in erythrocytes. AU - Soldati, Laura. AU - Lombardi, Cinzia. AU - Adamo, Donatella. AU - Terranegra, Annalisa. AU - Bianchin, Cristiana. AU - Bianchi, Giuseppe. AU - Vezzoli, Giuseppe. PY - 2002. Y1 - 2002. N2 - Recently, we have measured in erythrocytes a voltage-modulated and dihydropyridine-inhibited calcium influx. Since arachidonic acid and other polyunsaturated fatty acids influence the activities of most ion channels, we studied their effects on the erythrocyte Ca2+ influx. It was measured on fresh erythrocytes, isolated from healthy donors, using the fluorescent dye Fura 2 as indicator of [Ca2+]i. AA (5-50 μM) and EPA (20-30 μM) stimulated a concentration-dependent increase in [Ca2+]i, deriving from extracellular calcium (1 mM), without affecting the intra- and extracellular pH and membrane voltage. The Ca2+ influx rate varied from 0.5 to 3 nM Ca2+/s in the presence of AA and from 0.9 to 1.7 nM Ca2+/s with EPA. The Ca2+ ...
It turns out your diet directly affects your endocannabinoid system which is responsible for the synthesis of cannabis. A balance of Omega-3 and Omega-6 fatty acids is essential for optimizing the effects of cannabis.
Scientists are beginning to understand the role nutrition plays in keeping your endocannabinoid system healthy. SOL*CBD outlines ways to nurture ECS with diet!
The digestive, nervous, circulatory and respiratory system are some of the well-known systems in the body, but theres a lesser known yet still important system most people havent heard of, the endocannabinoid system. This recently discovered system plays a major role in many of the our bodily functions, and is only b
Lipid comprising polyunsaturated fatty acids | Oral pharmaceutical composition of isotretinoin | Preparation for treatment of a non-oral treatment site comprising an active chlorine compound and amino acids | Compounded solutions of diclofenac and lidocaine and methods | Compositions and methods including leelamine and arachidonyl trifluoromethyl ketone relating to treatment of cancer |
Prostaglandins act as short-lived localized hormones that can be released by any cell of the body during tissue, chemical, or traumatic injury, and can induce fever, inflammation, and pain, once they are present in the intercellular space. Thromboxanes, which are also hormone activators, can regulate blood vessel tone, platelet aggregation, and clot formation to increase the inflammatory response.[92,82] The inflammatory pathway is a complex biochemical pathway which, once stimulated by injury, leads to the production of these and other inflammatory mediators whose initial effect is pain and tissue destruction, followed by healing and recovery.[34,51] A major component of the inflammatory pathway is called the arachidonic acid pathway because arachidonic acid is immediately released from traumatized cellular membranes. Membrane-based arachidonic acid is transformed into prostaglandins and thromboxanes partly through the enzymatic action of cyclooxygenase (COX)[34,57]. There are two types of COX ...
The chart below can be a summary of knowledge out there on the endocannabinoid procedure in individuals with Alzheimers disease from the evaluate "The impact of cannabinoids on generic attributes of neurodegeneration", Fagan & Campbell, 2014. Notice: "CB1″ and "CB2″ receptors are People to which cannabinoids bind and thereby exert their consequences, "DGL" is diacylglycerol lipase (an enzyme involved with the formation of 2AG, an endocannabinoid, a cannabinoid found naturally in the body), the "cortex" is definitely the outermost layer of neuronal brain tissue, "AEA" is anandamide (an endocannabinoid), FAAH is surely an enzyme that acts to improve levels of AEA ...
Arachidonic acid is an unsaturated twenty-carbon fatty acid precursor to a number of molecules like the prostaglandins, thromboxanes, prostacyclins and leukotrienes. The whole lot of these compounds go by the general label of eicosanoids simply because they are all 20-carbon molecules; eikoisi is Greek for twenty. Arachidonate is "stored" as an esterified fatty acid in membranes. When released by the action of lipases, metabolites of arachidonate are used to mediate various biological processes such as pain perception and blood pressure, to name two. Aspirins analgesia is due largely to the fact that aspirin inhibits the enzyme cyclooygenase and transiently blocks the formation of metabolites of arachidonic acid that mediate inflammation. Theres more that can be said about the metabolites of arachidonate, but it would take a lot of time and space to cover all of them so Ill just stop here. If you can get ahold of a college-level biochemistry textbook you can find out more than you ...
12-keto-eicosatetraenoic acid is a biologically active eicosanoid in the nervous system of Aplysia.It is a metabolite of 12-HPETE formed by Aplysia nervous tissue. 12-KETE was identified in incubations of the tissue with arachidonic acid using HPLC, UV spectrometry, and gas-chromatography/mass spectrometry. [3H]12-KETE is formed from endogenous lipid stores in nervous tissue, labeled with [3H]arachidonic acid upon stimulation by application of histamine. In L14 and L10 cells, identified neurons in the abdominal ganglion, applications of 12-KETE elicit changes in membrane potential similar to those evoked by histamine.[PMID:2774398 ...
2Endogenous membrane bound phospholipase A2 was measured with labelled phospholipids used as substrates. The enzyme activity with phosphatidylcholine and phosphatidylethanolamine as substrates was inhibited by 27.0 ± 8.3% and 23.3 ± 11.1% (n = 4) respectively, in dexamethasone-treated macrophages compared to control cells. Neither the distribution of radiolabelled arachidonic acid among the different phospholipid species nor the release of arachidonic acid from prelabelled cells were significantly impaired by pretreatment of the macrophages with dexamethasone (1 μm ...
The endocannabinoid system is comprised of the CB1 and CB2 receptors, the naturally occurring endogenous ligands, anandamide (AEA) and 2-arachidonyl glycerol (2-AG); and the enzymes involved in their synthesis and ...
Chemicals. Retinol, retinal, retinoic acid, and arachidonic acid were purchased from Sigma-Aldrich (St. Louis. MO). 14C-labeled substrates were purchased from PerkinElmer Life and Analytical Sciences (Boston, MA), and 3H-DMBA was obtained from Amersham Biosciences Inc. (Piscataway, NJ). Complete Protease Inhibitor Tablets were obtained from Roche Diagnostics (Indianapolis, IN). The QuikChange Site-Directed Mutagenesis Kit was obtained from Stratagene (La Jolla, CA). Human CYP1A1 and CYP1B1 Supersomes were obtained from BD Gentest (Woburn, MA). Arachidonate metabolite standards 20-HETE, 15-HETE, 11-HETE, 9-HETE, 5-HETE, 8-HETE, and 12-HETE; and 14,15-EET, 11,12-EET, 8,9-EET, and 5,6-EET were obtained from Cayman Chemical (Ann Arbor, MI).. Expression and Purification of CYP1B1 and Cyp1b1. Human CYP1B1 was expressed and purified as described earlier (Jansson et al., 2001). The mouse Cyp1b1 transcript was prepared from a cDNA library using primers with modification at the 5′ end containing the ...
I am Susan Kistler, the American Evaluation Associations Executive Director and aea365 regular Saturday contributor. Here in the AEA offices, were counting down the days to Evaluation 2012. This time next week, well already be in Minneapolis, getting things set up and looking forward to seeing old friends and making new ones.. It is busy busy busy, but a number of items have come across my desk in the past week to share.. Rad Resource - AEA on YouTube: Weve got an AEA YouTube channel! There, you can find the set of Ignite presentations from Evaluation 2011 as well as the historic rendition of Evaluation Pie from the culminating session. Ill share more as it expands. We hope to post the 50+ Ignite presentations from Evaluation 2012 there.. On another front, AEA is Setting Records (we think): We believe that Ignite AEA 2012, with its 50 ignite presentations across two days, will represent the largest single OReilly recognized Ignite event!. Hot Tip - Twitter: If you are Tweeting about ...
While reading up on vitamin K2 recently, Ive noticed a number of connections that have me wondering if one of the culprits behind several widely occurring neurological diseases might be a relative scarcity of this vitamin in many peoples diets. … Continue reading →. ...
A research team has shown that blocking the degradation of two naturally occurring cannabinoids in the endocannabinoid signaling pathway of the brain produces marijuana-like behavioral effects in...
Thromboxane A2 (TXA2) is an arachidonic acid metabolite that is released during tissue trauma and elicits platelet aggregation and vascular smooth muscle contraction. Previous research has shown that TXA2 stimulates pulmonary ...
LTC4, LTD4, and LTE4 are leukotrienes (cys-LTs) derived from arachidonic acid as a result of immune or inflammatory stimuli. The above mentioned…
Several factors contribute to the deterioration in synaptic plasticity which accompanies age and one of these is neuroinflammation. This is characterized by increased microglial activation associated with increased production of proinflammatory cytokines like interleukin-1β (IL-1β). In aged rats these neuroinflammatory changes are associated with a decreased ability of animals to sustain long-term potentiation (LTP) in the dentate gyrus. Importantly, treatment of aged rats with agents which possess anti-inflammatory properties to decrease microglial activation, improves LTP. It is known that endocannabinoids, such as anandamide (AEA), have anti-inflammatory properties and therefore have the potential to decrease the age-related microglial activation. However, endocannabinoids are extremely labile and are hydrolyzed quickly after production. Here we investigated the possibility that inhibiting the degradation of endocannabinoids with the fatty acid amide hydrolase (FAAH) inhibitor, URB597, could
The present study investigated the role of arachidonic acid and acetylcholine in mediating endothelium-dependent relaxations of rabbit aorta. Isolated thoracic aortic rings were precontracted with a submaximal concentration of norepinephrine, and the effect of various agents on arachidonic acid- and acetylcholine-induced relaxations was examined. Arachidonic acid elicited a concentration-related relaxation that was potentiated by the cyclooxygenase inhibitor indomethacin. Treatment with the lipoxygenase inhibitor nordihydroguaiaretic acid completely blocked but the cytochrome P450 inhibitor metyrapone had no effect on arachidonic acid-induced relaxation. NG-Monomethyl-L-arginine and nitro-L-arginine, compounds that inhibit the nitric oxide-like endothelium-derived relaxing factor, had little or no effect on arachidonic acid-induced relaxations. In contrast, nordihydroguaiaretic acid, metyrapone, NG-monomethyl-L-arginine, and nitro-L-arginine all attenuated the relaxation to acetylcholine; ...
The endocannabinoids anandamide and 2-arachidonoylglycerol are metabolised by both hydrolytic enzymes (primarily fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL)) and oxygenating enzymes (e.g. cyclooxygenase-2, COX-2). In the present article, the in vivo data for compounds inhibiting endocannabinoid metabolism have been reviewed, focussing on inflammation and pain. Potential reasons for the failure of an FAAH inhibitor in a clinical trial in patients with osteoarthritic pain are discussed. It is concluded that there is a continued potential for compounds inhibiting endocannabinoid metabolism in terms of drug development, but that it is wise not to be unrealistic in terms of expectations of success.. ...
2-Arachidonoylglycerol plays a major role in endocannabinoid signaling, and is tightly regulated by the monoacylglycerol lipase (MAGL). Here we report the crystal structure of human MAGL. The protein crystallizes as a dimer, and despite structural homologies to haloperoxidases and esterases, it distinguishes itself by a wide and hydrophobic access to the catalytic site. An apolar helix covering the active site also gives structural insight into the amphitropic character of MAGL, and likely explains how MAGL interacts with membranes to recruit its substrate. Docking of 2-arachidonoylglycerol highlights a hydrophobic and a hydrophilic cavity that accommodate the lipid into the catalytic site. Moreover, we identified Cys201 as the crucial residue in MAGL inhibition by N-arachidonylmaleimide, a sulfhydryl-reactive compound. Beside the advance in the knowledge of endocannabinoids degradation routes, the structure of MAGL paves the way for future medicinal chemistry works aimed at the design of new ...
Title:Biosynthetic Pathways of Bioactive N-Acylethanolamines in Brain. VOLUME: 12 ISSUE: 1. Author(s):Kazuhito Tsuboi, Natsuki Ikematsu, Toru Uyama, Dale G. Deutsch, Akira Tokumura and Natsuo Ueda. Affiliation:Department of Biochemistry, Kagawa University School of Medicine, 1750-1 Ikenobe, Miki, Kagawa 761-0793, Japan.. Keywords:N-Acylethanolamine, anandamide, biosynthesis, NAPE-PLD, oleoylethanolamide, palmitoylethanolamide, phospholipid, plasmalogen. Abstract:Ethanolamides of long-chain fatty acids are a class of endogenous lipid mediators generally referred to as Nacylethanolamines (NAEs). NAEs include anti-inflammatory and analgesic palmitoylethanolamide, anorexic oleoylethanolamide, and the endocannabinoid anandamide. Since the endogenous levels of NAEs are principally regulated by enzymes responsible for their biosynthesis and degradation, these enzymes are expected as targets for the development of therapeutic agents. Thus, a better understanding of these enzymes is indispensable. The ...
Fatty acid amide hydrolase (FAAH) terminates the endocannabinoid signaling pathway that regulates numerous neurobehavioral processes in animals by hydrolyzing a class of lipid mediators, N-acylethanolamines (NAEs). Recent identification of an Arabidopsis FAAH homologue (AtFAAH) and several studies, especially those using AtFAAH overexpressing and knock-out lines suggest that a FAAH-mediated pathway exists in plants for the metabolism of endogenous NAEs. Here, I provide evidence to support this concept by identifying candidate FAAH cDNA sequences in diverse plant species. NAE amidohydrolase assays confirmed that several of the proteins encoded by these cDNAs indeed catalyzed the hydrolysis of NAEs in vitro. Kinetic parameters, inhibition properties, and substrate specificities of the plant FAAH enzymes were very similar to those of mammalian FAAH. Five amino acid residues determined to be important for catalysis by rat FAAH were absolutely conserved within the plant FAAH sequences. Site-directed mutation
Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. Genetic or pharmacological inactivation of FAAH leads to analgesic and anti-inflammatory phenotypes in rodents without s …
TY - JOUR. T1 - Platelet membrane glycoprotein IV (CD36) is involved in arachidonic acid induced-platelet aggregation. AU - Dutta-Roy, Asim K. AU - Crosbie, Lynn. AU - Gordon, Margaret Jane. AU - Campbell, Fiona Margaret. PY - 1996/5/1. Y1 - 1996/5/1. KW - Antibodies, Monoclonal. KW - Antigens, CD. KW - Antigens, CD36. KW - Arachidonic Acid. KW - Blood Platelets. KW - Humans. KW - Platelet Aggregation. M3 - Article. C2 - 8736825. VL - 24. SP - 167S. JO - Biochemical Society Transactions. JF - Biochemical Society Transactions. SN - 0300-5127. IS - 2. ER - ...
Arachidonic acid is arguably the most important PUFA associated with membrane phospholipids. Upon release, AA can be enzymatically metabolized to a myriad of bioactive derivatives, eicosanoids, known to contribute to a variety of chronic diseases, but are also known to be involved in tissue homeostasis and the resolution of inflammation [1-4, 22]. The relative abundance of AA in membrane phospholipids positively influences eicosanoid production [23]. It is well known that dietary PUFA can affect tissue AA levels; however, what is uncertain and controversial is whether modifying current intakes of dietary LA will result in concomitant changes in tissue AA content, i.e., increasing LA intake results in an increase in tissue AA content and decreasing LA has the opposite effect [8]. The goal of this paper was to ascertain the relationship between dietary LA and tissue AA content (phospholipid pools of plasma/serum and erythrocytes) in adults consuming a Western-style background diet. It was not ...
Research supports the hypothesis that GPR18 is the abnormal cannabidiol receptor and N-arachidonoyl glycine, the endogenous lipid metabolite of anandamide, initiates directed microglial migration in the CNS through activation of GPR18,[10] though recent evidence demonstrates that NAGly was not shown to be a GPR18 agonist in rat sympathetic neurons.[11]. Resolvin D2 (RvD2), a member of the specialized proresolving mediators (SPM) class of polyunsaturated fatty acid metabolites, is an activating ligand for GPR18; RvD2 and its activation of GPR18 contribute to the resolution of inflammatory responses as well as inflammation-based and other diseases in animal models and are proposed to do so in humans.[12] Furthermore, RvD2 is a metabolite of the omega-3 fatty acid, docosahexaenoic acid (DHA); the metabolism of DHA to RvD2 and RvD2s activation of GPR18 is proposed to one among many other mechanisms for the anti-inflammatory and other beneficial effects attributed to omega-3 fatty acid-rich ...
There has been a considerable increase in our understanding of the role of arachidonic acid metabolites in asthma over the last decade. Arachidonic acid provides a source for both leukotrienes and prostanoids which have a diverse range of properties that are important in regulating the airway inflammatory response. It is clear that cysteinyl leukotrienes are important pro-inflammatory mediators in asthma which act to enhance bronchoconstriction. This has led to the development of a number of agents which either target the enzymes involved in leukotriene synthesis or are antagonists at specific leukotriene receptors. The development of these agents has allowed the role of leukotrienes in different variants of asthma to be studied. The other arm of arachidonic acid metabolism is the cyclo-oxygenase pathway. Cyclo-oxygenase exists in two forms-a constitutive form, COX-1, responsible for the production of housekeeping prostaglandins, and an inducible form, COX-2, which is involved in inflammatory ...
TrendTerms displays relevant terms of the abstract of this publication and related documents on a map. The terms and their relations were extracted from ZORA using word statistics. Their timelines are taken from ZORA as well. The bubble size of a term is proportional to the number of documents where the term occurs. Red, orange, yellow and green colors are used for terms that occur in the current document; red indicates high interlinkedness of a term with other terms, orange, yellow and green decreasing interlinkedness. Blue is used for terms that have a relation with the terms in this document, but occur in other documents ...
A free platform for explaining your research in plain language, and managing how you communicate around it - so you can understand how best to increase its impact.
Our previous studies suggested that enhanced pulmonary artery contractions to arachidonic acid in females compared with males were mediated by an LO metabolite.6 The purpose of the current study was to systematically characterize the LO pathways in female and male pulmonary arteries. First, it was shown that the protein expression of both 15- and 5-LO was greater in females compared with males. Although pulmonary arteries from both male and females produced the corresponding LO metabolites, 15- and 5-HETE, only the synthesis of 15-HETE was enhanced in females. The increase in 15-HETE was correlated with an increased 15-HETE-mediated pulmonary artery vasoconstriction in females compared with males. These findings are significant because it is the first report that the 15-LO pathway is regulated in a sex-specific way. These results may impact what is known about the sex differences in the incidence of PAH.. The enhanced vasoconstriction in females compared with males could be because of increased ...
Cite this article as:. Mauro Maccarrone, " Editorial [Hot Topic:The Endocannabinoid System in the Brain: From Biology to Therapy (Guest Editor: Mauro Maccarrone)]", Current Drug Targets - CNS & Neurological Disorders (2005) 4: 613. https://doi.org/10.2174/156800705774933078 ...
Antibodies for proteins involved in arachidonic acid epoxygenase activity pathways, according to their Panther/Gene Ontology Classification
Complete information for FAAH2 gene (Protein Coding), Fatty Acid Amide Hydrolase 2, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
Nephron function is segmented. Each segment has characteristic transport mechanisms and individual eicosanoid profiles [1,[2]]. Mapping the distribution of AA metabolizing enzymes within the nephron...
The endocannabinoid system and their refers to a group of neuromodulatory receptors that are involved in a variety of physiological processes. - Endocannabinoid chemical biology - Harm reduction, the cannabis paradox
FAAH antibody (fatty acid amide hydrolase) for IHC-P, WB. Anti-FAAH pAb (GTX55611) is tested in Human, Mouse, Rat samples. 100% Ab-Assurance.
Arachidonic acid[edit]. ALOX5 metabolizes the omega-6 fatty acid, Arachidonic acid (AA, i.e. 5Z,8Z,11Z,15Z-eicosatrienoic acid ... Eicosapentaenoic acid[edit]. ALOX5 metabolizes the omega-3 fatty acid, Eicosapentaenoic acid (EPA, i.e. 4Z,8Z,11Z,14Z,17Z- ... Mead acid[edit]. Mead acid (i.e. 5Z,8Z,11Z-eicosatrienoic acid) is identical to AA except that has a single rather than double ... Docosahexaenoic acid[edit]. ALOX5 acts in series with ALOX15 to metabolize the omega 3 fatty acid, docosahexaenoic acid (DHA, i ...
General: Arachidonic acid. *DAG (PKC, TRPC). *IP3 (IP3R, RyR) ... Vedaprofen; Anthranilic acids (fenamic acids): Etofenamic acid ... Since diacylglycerol is synthesized via phosphatidic acid, it will usually contain a saturated fatty acid at the C-1 position ... or free fatty acids.(See Dietary sources of fatty acids, their digestion, absorption, transport in the blood and storage for ... to form lysophosphatidic acid, which is then acylated with another molecule of acyl-CoA to yield phosphatidic acid. ...
... -A synthase, an enzyme found in platelets, converts the arachidonic acid derivative prostaglandin H2 to thromboxane ... Omega-3 fatty acids are metabolized to produce higher levels of TxA,3 which is relatively less potent than TxA2 and PGI3; ... Tiaprofenic acid (tiaprofenate). *Vedaprofen; Anthranilic acids (fenamic acids): Etofenamic acid (etofenamate). *Floctafenic ...
These convert arachidonic acid to prostaglandin H2 (PGH2), the immediate precursor of prostacyclin. Since thromboxane (an ... PGI2 is derived from the ω-6 arachidonic acid. PGI3 is derived from the ω-3 EPA. ... Z)-5-[(4R,5R)-5-Hydroxy-4-((S,E)-3-hydroxyoct-1-enyl)hexahydro-2H-cyclopenta[b]furan-2-ylidene]pentanoic acid ... Fischer S, Weber PC (1985). "Thromboxane (TX)A3 and prostaglandin (PG)I3 are formed in man after dietary eicosapentaenoic acid ...
Increased arachidonic acid turnover[23]. *Increased cytokine synthesis[26]. Imaging studies have shown that the left amygdala ...
This enzyme participates in arachidonic acid metabolism. Catalyzed reaction[edit]. The chemical reaction catalyzed by LTA4H. ... Enzymatic conversion into 5,6-dihydroxy-7,9,11,14-eicosatetraenoic acid by mouse liver cytosolic epoxide hydrolase". J. Biol. ... "Molecular cloning and amino acid sequence of leukotriene A4 hydrolase". Proc. Natl. Acad. Sci. U.S.A. 84 (19): 6677-81. doi ...
Arachidonic acid (AA), i.e. 5Z, 8Z,11Z,14Z-eicosatetraenoic acid is ω-6 fatty acid, with four double bonds in the cis ... all of which are less active than there arachidonic acid analogs. Since eicosapentaenoic acid competes with arachidonic acid ... Arachidonic acid (AA; 20:4 ω-6) sits at the head of the "arachidonic acid cascade" - more than twenty eicosanoid-mediated ... arachidonic acid viz., 5,6-epoxy-eicsattrienoic acid (5,6-EET), 8,9-EET, 11,12-EET, and 14,15-EET (see Epoxyeicosatrienoic acid ...
Piomelli, Daniele (2000). „Arachidonic Acid". Neuropsychopharmacology: The Fifth Generation of Progress. Приступљено 3. 3. 2006 ... Fatty Acids. 61 (1): 55-64. PMID 10477044. doi:10.1054/plef.1999.0074.. ,access-date=. захтева ,url=. (помоћ) ... DeCaterina, R & Basta, G (2001). „n-3 Fatty acids and the inflammatory response - biological background" (PDF). European Heart ... Nutrigenomic approach to understanding the mechanisms by which dietary long-chain fatty acids induce gene signals and control ...
Eicosanoids act as neuromodulators via the Arachidonic acid cascade. Orexins (-A and -B) are involved in a number of cognitive ... "Arachidonic Acid". Neuropsychopharmacology: The Fifth Generation of Progress. Retrieved 2006-03-03. "Neurotrophic factors". ...
... works by preventing the synthesis of another omega metabolite known as arachidonic acid.[12] Arachidonic acid is an omega 6, ... Essential fatty acids[edit]. Further information: Coat (dog). Many canine skin disorders can have a basis in poor nutrition. ... A group of dogs supplemented with omega 3 fatty acids (660 mg/kg [300 mg/lb] of body weight/d) not only improved the condition ... The supplementation of both omega fatty acids 3 and 6 have been shown to mediate the inflammatory skin response seen in chronic ...
Capric acid,[1] n-Capric acid, n-Decanoic acid, Decylic acid, n-Decylic acid, C10:0 (Lipid numbers) ... Decanoic acid (capric acid, C10:0) is a saturated fatty acid. Its formula is CH3(CH2)8COOH. Salts and esters of decanoic acid ... Two other acids are named after goats: caproic (a C6:0 fatty acid) and caprylic (a C8:0 fatty acid). Along with decanoic acid, ... Nonanoic acid, a medium-chain fatty acid, also with antiseizure activity. References[edit]. *^ a b c d n-Decanoic acid in ...
... is the first fatty acid produced during fatty acid synthesis and is the precursor to longer fatty acids. As a ... Palmitic acid, or hexadecanoic acid in IUPAC nomenclature, is the most common saturated fatty acid found in animals, plants and ... Palmitic acid strongly boosts metastasis in mouse models of human oral cancer cells. Among all fatty acids, it has the ... Aluminium salts of palmitic acid and naphthenic acid were combined during World War II to produce napalm. The word "napalm" is ...
... to the n-6 highly unsaturated fatty acid (n-6HUFA), arachidonic acid (20:4n-6), competitively displaces n-3 HUFA from tissue ... 2015 Alan Brash from Vanderbilt University on arachidonic acid metabolites and their role in pathophysiological processes ... "Omega-3 PUFAs lower the propensity for arachidonic acid cascade over-reactions". BioMed Res Int. 2015: 555. doi:10.1155/2015/ ... "Prostaglandins Leukot Essent Fatty Acids. 99: 19-23. doi:10.1016/j.plefa.2015.04.005. PMID 26002802.. ...
Mortierella alpina Strain: ATCC 32222, commercial source of arachidonic acid (2011[119]) ...
Inhibition of receptor-mediated release of arachidonic acid by pertussis toxin. Cell. 1984 Dec;39(2 Pt 1):301-8. PMID 6094010. ... Adenylyl cyclase amino acid sequence: possible channel- or transporter-like structure. Science. 1989 Jun 30;244(4912):1558-64. ...
First, Phospholipase A2 (PLA2) facilitates the conversion of phospholipids to Arachidonic Acid, the framework from which all ... The Arachidonic Acid then reacts with two Cyclooxygenase (COX) receptors, COX-1 and COX-2 to form Prostaglandin H2, an ... Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(E,3S)- 3-hydroxyoct-1-enyl]cyclopentyl]hept-5-enoic acid ... Tiaprofenic acid (tiaprofenate). *Vedaprofen; Anthranilic acids (fenamic acids): Etofenamic acid (etofenamate). *Floctafenic ...
γ-Linolenic acid (gamolenic acid). *Dihomo-γ-linolenic acid. *Diacylglycerol. *Arachidonic acid ... Tafluprost acid is inactivated by beta oxidation to 1,2-dinortafluprost acid, 1,2,3,4-tetranortafluprost acid, and its lactone ... Tafluprost, as a lipophilic ester, easily penetrates the cornea and is then activated to the carboxylic acid, tafluprost acid. ... From left to right: tafluprost, tafluprost acid (the active metabolite), 1,2-dinortafluprost acid, 1,2,3,4-tetranortafluprost ...
This enzyme participates in arachidonic acid metabolism. Watanabe K, Shimizu T, Iguchi S, Wakatsuka H, Hayashi M, Hayaishi O ( ...
Regulation of arachidonic acid metabolites in macrophages. J. Exp. Med. 152:324-335. 1982 With W. A. Scott, N. A. Pawlowski, H ... Regulation of arachidonic acid metabolism by macrophage activation. J. Exp. Med. 155:1148-1160. With W. C. Van Voorhis, G. ... Bacterial lipopolysaccharides prime macrophages for enhanced release of arachidonic acid metabolites. J. Exp. Med. 164:165-179 ...
This enzyme participates in arachidonic acid metabolism. It employs one cofactor, heme. Romano MC, Eckardt RD, Bender PE, ...
This enzyme participates in arachidonic acid metabolism. Sok DE, Kang JB, Shin HD (1988). "15-Hydroxyeicosatetraenoic acid ... H+ The 3 substrates of this enzyme are 15-Hydroxyicosatetraenoic acid (i.e. 15(S)-15-hydroxy-5,8,11-cis-13-trans- ...
Bundy GL, Nidy EG, Epps DE, Mizsak SA, Wnuk RJ (1986). "Discovery of an arachidonic acid C-8 lipoxygenase in the gorgonian ... This enzyme participates in arachidonic acid metabolism. As of late 2007, only one structure has been solved for this class of ...
When these cytokine factors bind, the arachidonic acid pathway is then activated. One model for the mechanism of fever caused ... PGE2 release comes from the arachidonic acid pathway. This pathway (as it relates to fever), is mediated by the enzymes ... In other words, exogenous factors cause release of endogenous factors, which, in turn, activate the arachidonic acid pathway. ...
Conversion of arachidonic acid to 15-S-hydroperoxy-eicosatetraenoic acid". J. Biol. Chem. 257: 6050-6055. PMID 6804460.. CS1 ... Narumiya, S. & Salmon, J.A. (1982). „Arachidonic acid-15-lipoxygenase from rabbit peritoneal polymorphonuclear leukocytes". ... Oliw, E.H. & Sprecher, H. (1989). „Metabolism of polyunsaturated fatty acids by an (n-6)-lipoxygenase associated with human ...
Fish oils provide alternative fatty acids to arachidonic acid. These acids can be turned into some anti-inflammatory ... "Conversion of acetaminophen to the bioactive N-acylphenolamine AM404 via fatty acid amide hydrolase-dependent arachidonic acid ... Arachidonic acid Cyclooxygenase 1 Cyclooxygenase 2 NSAID Discovery and development of COX-2 selective inhibitors COX-2 ... amino acid sequence homology and near-identical catalytic sites. The most significant difference between the isoenzymes, which ...
... which catalyzes the conversion of arachidonic acid to leukotriene B4 (LTB4).[45] LTB4 promotes skin inflammation by acting on ... Salicylic acid[edit]. Salicylic acid is a topically applied beta-hydroxy acid that stops bacteria from reproducing and has ... "Topical azelaic acid, salicylic acid, nicotinamide, sulphur, zinc and fruit acid (alpha-hydroxy acid) for acne". Cochrane ... lactic acid, salicylic acid, Jessner's solution, or a lower concentration (20%) of trichloroacetic acid. These peels only ...
Arachidonic acid (AA) is a 20-carbon ω-6 conditionally essential fatty acid. It sits at the head of the "arachidonic acid ... In the arachidonic acid cascade, dietary linoleic acid (18:2 ω-6) is desaturated and lengthened to form arachidonic acid, ... Daniele Piomelli Arachidonic Acid The arachidonic acid cascade proceeds somewhat differently in the brain. Neurohormones, ... IV Supplementation with gamma-linolenic acid increased serum GLA but did not increase the plasma percentage of arachidonic acid ...
Health effects of arachidonic acid supplementation[edit]. Arachidonic acid supplementation in daily doses of 1,000-1,500 mg for ... Arachidonic acid is not one of the essential fatty acids. However, it does become essential if a deficiency in linoleic acid ... Arachidonic acid is also used in the biosynthesis of anandamide.[17]. *Some arachidonic acid is converted into ... Dietary arachidonic acid and inflammation[edit]. Increased consumption of arachidonic acid will not cause inflammation during ...
A polyunsaturated fatty acid, CH3(CH2)3(CH2CH:CH)4(CH2)3COOH, that is essential for growth in mammals (see eicosanoid [1]). It ... arachidonic acid A long chain polyunsaturated fatty acid (20 : 4 ω6). Not strictly an essential fatty acid, since it can be ... arachidonic acid A polyunsaturated fatty acid, CH3(CH2)3(CH2CH:CH)4(CH2)3COOH, that is essential for growth in mammals (see ... arachidonic acid (ă-rak-i-don-ik) n. see essential fatty acid. ... "arachidonic acid." A Dictionary of Biology. . Encyclopedia.com. ...
I spend a lot of time highlighting the importance of omega-3 fatty acids and downplaying their poly cohorts, omega-6s. Of ... If youre getting plenty of linoleic acid in your diet, your body can make arachidonic acid. First, linoleic acid, abundant in ... Actually, arachidonic acid may have little to do with ones intake of linoleic acid. All the same then, it probably isnt the ... Arachidonic acid is both a product of the bodys natural linoleic acid conversion and, as the question notes, an existing (but ...
... releases arachidonic acid. ANSWER QUESTION: What enyzme acts on arachidonic acid and begins the process through which ... Derivatives of an n-6 Polyunsaturated Fatty Acid. An important family of regulatory molecules is derived from arachidonic acid ... QUESTION: What molecule is the source of arachidonic acid and where is it found? ANSWER QUESTION: Name the enzyme that, when ... Derivatives of n-3 Polyunsaturated Fatty Acids. The above introduces regulatory molecules derived from arachidonic acid. These ...
Arachidonic Acid News and Research. RSS Arachidonic acid is an omega-6 fatty acid that is present in the phospholipids ( ... Fatty acids may be the culprit in Alzheimers According to new research from the U.S. controlling the level of a fatty acid in ... Fatty acids such as those found in corn oil turn on genes that stimulate tumor growth Omega-6 fatty acids--such as those found ... Altering fatty acid levels in diet may reduce prostate cancer growth rate UCLA researchers found that altering the fatty acid ...
Arachidonic acid is also used in the biosynthesis of anandamide.[17]. *Some arachidonic acid is converted into ... Health effects of arachidonic acid supplementationEdit. Arachidonic acid supplementation in daily dosages of 1,000-1,500 mg for ... Dietary arachidonic acid and inflammationEdit. Increased consumption of arachidonic acid will not cause inflammation during ... and phosphatidic acid. BrainEdit. Arachidonic acid is one of the most abundant fatty acids in the brain, and is present in ...
... polyunsaturated fatty acid or n-6 PUFA. It is made in the body from shorter omega-6 fatty acids found in vegetable oils, or ... Arachidonic acid, AA and sometimes ARA, is a 20 carbon long, omega-6, ... Arachidonic acid, AA and sometimes ARA, is a 20 carbon long, omega-6, polyunsaturated fatty acid or n-6 PUFA. It is made in the ... The Journal of the International Society of Sports Nutrition: Effects Of Arachidonic Acid Supplementation On Training ...
These are saturated fats, trans fats and (AA) arachidonic acid. I consider these to be really bad fats. Arachidonic acids are ... arachidonic acid into the same rabbits they are dead within three minutes. The human body needs some arachidonic acid, but ... Understanding (AA) Arachidonic Acid - (Omega 6 - Pro Inflammatory Fat). Dr. Barry Sears. Zone Living. CBN.com There are two ... is stimulated to make increased levels of arachidonic acid. (AA) is a long-chain omega-6 fatty acid. Enchaned production of ...
Hanna, V. S., Gawish, A., Abou El-Dahab, M., Tallima, H., & El Ridi, R. (2018). Is arachidonic acid an endoschistosomicide? ... mansoni infection might be ascribed to stores of arachidonic acid (ARA)-rich lipids in liver. Several reports have previously ...
T 2370/09 (Arachidonic acid/MARTEK) of 26.5.2014. European Case Law Identifier:. ECLI:EP:BA:2014:T237009.20140526. ...
Get to know arachidonic acid and experience gains like the old days! ... Arachidonic acid isnt considered an essential fatty acid, because your body can synthesize it from linoleic acid in the liver ... Rett, B., & Whelan, J. (2011). Increasing Dietary Linoleic Acid Does Not Increase Tissue Arachidonic Acid Content in Adults ... WHAT IS ARACHIDONIC ACID?. Basically, ARA is the primary fatty acid responsible for inflammation in muscle tissue. This 20- ...
... acid, were also indetectable in these lipids. On the basis of these results, it appears that the arachidonic acid cascade is ... Evidence that arachidonic acid is deficient in phosphatidylinositol of Drosophila heads.. Yoshioka T, Inoue H, Kasama T, Seyama ... Since arachidonic acid is considered to be a key molecule in phosphatidylinositol turnover in the brain, it is of interest that ... We have found that arachidonic (20 : 4) acid is indetectable in phosphatidylinositol and diacyglycerol extracted from ...
Naturally occurring, weight training can reduce levels creating a need for supplemental Arachidonic Acid. ... Arachidonic Acid is an Omega-6 fatty acid essential for muscle hypotrophy. ... Arachidonic Acid Chemical Composition. (5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoic acid. Formula: C20 H32 O2 ... Arachidonic acid (AA) is a naturally occurring omega-6 essential fatty acid. Its the principle building block for the synthesis ...
Arachidonic acid (ARA) is one of the two main polyunsaturated fatty acids (PUFAs) in the brain, especially in neuronal cells, ... Arachidonic Acid: Sources, Biosynthesis and Health Effects. Jason M. OKeefe (Editor). Series: Biochemistry Research Trends. ... Home / Shop / Books / Science and Technology / Chemistry / Arachidonic Acid: Sources, Biosynthesis and Health Effects. ... Chapter 4 - Arachidonic Acid, Cyclooxygenase and Hepatic Inflammation (pp. 127-134). Sura Wanessa Santos Rocha and Christina ...
Arachidonic acid and acetylcholine had no effect on denuded rabbit aorta. Incubation of rabbit aorta with [14C]arachidonic acid ... and the effect of various agents on arachidonic acid- and acetylcholine-induced relaxations was examined. Arachidonic acid ... had little or no effect on arachidonic acid-induced relaxations. In contrast, nordihydroguaiaretic acid, metyrapone, NG- ... Arachidonic acid- and acetylcholine-induced relaxations of rabbit aorta.. S L Pfister, W B Campbell ...
K. Yang, W. Ma, H. Liang, Q. Ouyang, C. Tang, and L. Lai, "Dynamic simulations on the arachidonic acid metabolic network," PLoS ... S. H. Hong, I. Avis, M. D. Vos, A. Martínez, A. M. Treston, and J. L. Mulshine, "Relationship of arachidonic acid metabolizing ... Y. Cao, A. T. Pearman, G. A. Zimmerman, T. M. McIntyre, and S. M. Prescott, "Intracellular unesterified arachidonic acid ... In devising therapeutic strategies, with the arachidonic acid products, greater attention to the impact of levels of mediators ...
Evidence that proline-directed phosphorylation is not required for mobilization of arachidonic acid by cPLA," Journal of ... M. A. Balboa, J. Balsinde, and E. A. Dennis, "Involvement of phosphatidase phosphohydrolase in arachidonic acid mobilization in ... LysoPC and PAF Trigger Arachidonic Acid Release by Divergent Signaling Mechanisms in Monocytes. ... "Phosphorylation of cytosolic phospholipase A and the release of arachidonic acid in human neutrophils," Journal of Immunology, ...
Arachidonic acid is found in animal products, like poultry and eggs. The amount of arachidonic acid found in just one egg a day ... Arachidonic Acid and Mental Health. Arachidonic acid may trigger brain inflammation. High blood levels have been associated ... Inflammatory Remarks about Arachidonic Acid. Arachidonic acid may play a role in cancer, asthma, inflammatory bowel disease, ... Arachidonic acid is an inflammatory omega-6 fatty acid. Our bodies produce this nutrient, and its excess may lead to ...
Arachidonic Acid in Cell Signaling has 2 available editions to buy at Alibris ... Arachidonic Acid in Cell Signaling by Daniele Piomelli starting at $61.69. ... Arachidonic acid may serve as an intracellular second messenger in many cell types, as well as precursor for biologically ... Arachidonic acid may serve as an intracellular second messenger in many cell types, as well as precursor for biologically ...
Arachidonic acid may play a role in cancer, asthma, inflammatory bowel disease, rheumatoid arthritis, and other autoimmune ... Arachidonic acid is produced in the body from linoleic acid (LA) by three enzymes. More arachidonic acid is made if the ratio ... Is there enough arachidonic acid & palmitic acid in peanuts to justify limiting their consumption? ... This, coupled with a diet rich in vegetable oils, means the mutated gene turns fatty acids into arachidonic acid. ...
Crystall Swarbrick, Noelia Roman and Jade K. Forwood (December 16th 2011). Role of ACOT7 in Arachidonic Acid Production and ... Crystall Swarbrick, Noelia Roman and Jade K. Forwood (December 16th 2011). Role of ACOT7 in Arachidonic Acid Production and ... Role of ACOT7 in Arachidonic Acid Production and Inflammation. By Crystall Swarbrick, Noelia Roman and Jade K. Forwood ... www.intechopen.com/embed/inflammatory-diseases-a-modern-perspective/role-of-acot7-in-arachidonic-acid-production-and- ...
Arachidonic acid 5-hydroperoxide (5-hydroperoxyeicosatetraenoic acid, 5-HPETE) is an intermediate in the metabolism of ... 5-Hydroxyicosatetraenoic acid and 5-oxo-eicosatetraenoic acid; or c) the specialized pro-resolving mediators of inflammation, ... arachidonic acid by the ALOX5 enzyme in humans or Alox5 enzyme in other mammals. The intermediate is then further metabolized ...
... arachidonic acid; cyclooxygenase; cytochrome P-450; dihydroxyeicosatetraenoic acid; epoxyeicosatrienoic acid; ... Role of arachidonic acid metabolites on the control of non-differentiated intestinal epithelial cell growth.. Cabral M1, Martín ... Increasingly evidence indicates that enzymes, receptors and metabolites of the arachidonic acid (AA) cascade play a role in ... 12 and 15-hydroxyeicosatetraenoic acid (HETE) but not LTD4, 20-HETE and epoxyeicosatrienoic acids. We also found that ...
Antibodies for proteins involved in arachidonic acid epoxygenase activity pathways, according to their Panther/Gene Ontology ... Antibodies for proteins involved in arachidonic acid epoxygenase activity pathways; according to their Panther/Gene Ontology ...
  • Today, the usual diet in industrial countries contains much less ω-3 fatty acids than the diet of a century ago and a much greater amount of air pollution on a daily basis that evokes the inflammatory response. (wikipedia.org)
  • In response to a variety of inflammatory signals, these EFAs are cleaved out of the phospholipid and released as free fatty acids. (wikipedia.org)
  • Glutamate is the most extensively distributed excitatory amino acid neurotransmitter in the cerebral cortex. (ahajournals.org)
  • LTBR1 and LTBR2 encode for proteins with 45% amino acid identity that belong to the G protein-coupled receptor superfamily. (wikipedia.org)
  • Two BLT2-like receptors, Blt2a and Blt2b, with 49% amino acid identity to each other and 34% and 29%, respectively, amino acid identities to human BLT2 have been cloned from Zebrafish embryos. (wikipedia.org)
  • The latter citation presents a phylogenic tree on the amino acid relateness of these two receptors as well as those from humans, monkeys, dogs, rats and mice to each other. (wikipedia.org)
  • In terms of their molecular biology, COX-1 and COX-2 are of similar molecular weight, approximately 70 and 72 kDa, respectively, and having 65% amino acid sequence homology and near-identical catalytic sites. (wikipedia.org)
  • the membrane-binding domain consists of a series of amphipathic α helices with several hydrophobic amino acids exposed to a membrane monolayer. (wikipedia.org)
  • The human CysLTR1 gene maps to the X chromosome at position Xq13-Xq21, contains three exons with the entire open reading frame located in exon 3, and codes for a protein composed of 337 amino acids. (wikipedia.org)
  • Binding of calmodulin occurs between amino acids 420 and 437 in CERK at a putative 1-8-14B calmodulin binding motif. (wikipedia.org)
  • The binding motif in CERK contains leu-422, phe-429, and leu-435 which respectively correspond to the 1st, 8th, and 14th hydrophobic amino acids where calmodulin binds. (wikipedia.org)
  • Human PRKCE gene (Ensembl ID: ENSG00000171132) encodes the protein PKCε (Uniprot ID: Q02156), which is 737 amino acids in length with a molecular weight of 83.7 kDa. (wikipedia.org)
  • specifically, the C2 domain of PKCε at amino acids 14-21 (also known as εV1-2) binds RACK2, and peptide inhibitors targeting εV1-2 inhibit PKCε translocation and function in cardiomyocytes, while peptide agonists augment translocation. (wikipedia.org)
  • The originally cloned TP from placenta (343 amino acids in length) is known as the α isoform and the splice variant cloned from endothelium (with 407 amino acids), termed the β isoform. (wikipedia.org)
  • The first 328 amino acids are the same for both isoforms, but the β isoform exhibits an extended C-terminal cytoplasmic domain. (wikipedia.org)
  • This 11 kilobase pair gene consists of 14 exons and 13 introns coding for a 75 kiloDalton protein composed of 662 amino acids. (wikipedia.org)
  • The ALOX5 gene, which occupies 71.9 kilobase pairs (kb) on chromosome 10 (all other human lipoxygenases are clustered together on chromosome 17), is composed of 14 exons divided by 13 introns encoding the mature 78 kilodalton (kD) ALOX5 protein consisting of 673 amino acids. (wikipedia.org)
  • Human ALOX5 is a soluble, monomeric protein consisting of 673 amino acids with a molecular weight of ~78 kDa. (wikipedia.org)
  • This width appears to be maintained by hydrogen bonding and van der Waals forces within a sheet of aromatic amino acid residues surrounding the selectivity filter. (wikipedia.org)
  • Its 148-amino acid preproprotein, following cleavage of a signal peptide, is further processed to produce either the 27-amino acid gastrin-releasing peptide or the 10-amino acid neuromedin C. These smaller peptides regulate numerous functions of the gastrointestinal and central nervous systems, including release of gastrointestinal hormones, smooth muscle cell contraction, and epithelial cell proliferation. (wikipedia.org)
  • The current nomenclature guidelines suggest that members of new CYP families share at least 40% amino acid identity, while members of subfamilies must share at least 55% amino acid identity. (wikipedia.org)
  • citation needed] LTC4, LTD4, LTE4 and LTF4 are often called cysteinyl leukotrienes due to the presence of the amino acid cysteine in their structure. (wikipedia.org)
  • ALOX12 is 75 kilodalton protein composed of 663 amino acids. (wikipedia.org)
  • Thereafter the glucose that is released into the blood by the liver for general use by the body tissues, has to be synthesized from the glucogenic amino acids and a few other gluconeogenic substrates, which do not include fatty acids. (wikipedia.org)
  • Whereas, by virtue of its exclusive location on maternal side of placental trophoblasts and its preference for long chain polyunsaturated fatty acids (LCPUFAs), placenta specific plasma membrane fatty acid-binding protein ( p-FABPpm) sequesters maternal plasma DHA/ARA to the placenta for fetal supply. (wikipedia.org)
  • CYP2C18 also possesses epoxygenase activitiy: it can attack various long-chain polyunsaturated fatty acids at their double (i.e. alkene) bonds to form epoxide products that act as signaling agents. (wikipedia.org)
  • Abstract Recent evidence has suggested that arachidonic acid (AA) may be an important signaling molecule in cardiac excitation-contraction coupling. (ahajournals.org)
  • 8R-hydroxy,11R,12R-epoxy-hepoxilin A3 is further metabolized by soluble Epoxide hydrolase 2 (sEH) to 8R,11R,12R-trihydroxy-5Z,9E,14Z-eicosatetraenoic acid. (wikipedia.org)
  • Cellular cytochrome P450 epoxygenases metabolize various polyunsaturated fatty acids to epoxide-containng products. (wikipedia.org)
  • Cytochrome P450 epoxygenases attack these double bonds to form their respective eicosatrienoic acid epoxide regioisomers (see Structural isomer, section on position isomerism (regioisomerism)) viz. (wikipedia.org)
  • Employing a monoclonal antibody directed against human PR3 and ANCA-positive serum from WG patients with specificity for PR3, we now investigated the role of free arachidonic acid (AA) in autoantibody-related human neutrophil activation. (rupress.org)
  • On the other hand, diets high in carbohydrate and low in fat and protein (with little or no arachidonic acid) may be associated with lower levels of anxiety and depression , according to epidemiological studies. (nutritionfacts.org)
  • Protein kinases C translocation responses to low concentrations of arachidonic acid. (springer.com)
  • Heart microsomal protein from control or isoproterenol treated rats was incubated with 50 μM arachidonic acid, and arachidonic acid metabolites were determined by liquid chromatography-electron spray ionization-mass spectrometry. (aspetjournals.org)
  • Hydroxycarboxylic acid receptor 2 (HCA2), also known as niacin receptor 1 (NIACR1) and GPR109A, is a protein which in humans is encoded by the HCAR2 gene. (wikipedia.org)
  • HCA2 is a high-affinity Gi/Go-coupled G protein-coupled receptor (GPCR) for nicotinic acid (niacin), and is a member of the nicotinic acid receptor family of GPCRs. (wikipedia.org)
  • The location of fatty acid translocase (FAT) and fatty acid transporter protein (FATP) on both sides of the bipolar placental trophoblast cells and the lack of specificity for particular types of free fatty acids (FFA) allows transport by all FFAs (non-essential, essential and long-chain PUFAs) bidirectionally, i.e. from the mother to the fetus and vice versa. (wikipedia.org)
  • When compared to other macronutrient classes (carbohydrates and protein), fatty acids yield the most ATP on an energy per gram basis, when they are completely oxidized to CO2 and water by beta oxidation and the citric acid cycle. (wikipedia.org)
  • Long chain free fatty acids enter the metabolizing cells (i.e. most living cells in the body except red blood cells and neurons in the central nervous system) through specific transport proteins, such as the SLC27 family fatty acid transport protein. (wikipedia.org)
  • In animals, as well as some fungi such as yeast, these same reactions occur on fatty acid synthase I (FASI), a large dimeric protein that has all of the enzymatic activities required to create a fatty acid. (wikipedia.org)
  • Substrate activation by longchain fatty acid. (springer.com)
  • The median of 8,9-EET and 14,15-EET was 14.5 and 17.7 ng 10(-6) cells, respectively, whereas 5,6-EET and 11,12-EET were below 2 ng 10(-6) cells in a 5-min incubation assay at a 30 microM arachidonic acid substrate concentration. (fraunhofer.de)
  • The most thoroughly studied substrate of the CYP epoxylgenases is arachidonic acid. (wikipedia.org)
  • Note that the eicosatetraenoate substrate loses one double bound to become an eicosatrienoic acid with three double bonds and that the epoxygenases typically form a mixture of R/S enantiomers at the attacked double bound position. (wikipedia.org)
  • Cellular Proteins and Their Fatty Acids in Health and Disease Human Placental Trophoblasts: Impact of Maternal Nutrition Early Nutrition and Lifestyle Factors: Effects on First Trimester Placenta Human Blood Platelet Function: Applications in Cardiovascular Health Dutta-Roy, Asim K. (wikipedia.org)
  • Low Ca 2+ concentrations activated only oleic acid conversion. (biochemj.org)
  • The data are consistent with the hypothesis that Mg 2+ has a direct effect on fatty acyl-CoA synthetase activity, and suggest that preference for oleic acid and arachidonic acid can be influenced by the ionic milieu. (biochemj.org)