Search Results - "CESURA, A"

A Synthetic Agonist at the Orphanin FQ/Nociceptin Receptor ORL1: Anxiolytic Profile in the Rat by Jenck, Francois, Wichmann, Juergen, Dautzenberg, Frank M., Moreau, Jean-Luc, Ouagazzal, Abdel M., Martin, James R., Lundstrom, Kenneth, Cesura, Andrea M., Poli, Sonia M., Roever, Stephan, Kolczewski, Sabine, Adam, Geo, Kilpatrick, Gavin

“…The biochemical and behavioral effects of a nonpeptidic, selective, and brain-penetrant agonist at the ORL1 receptor are reported herein. This low molecular…”
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Synthesis and Biochemical Evaluation of N-(4-Phenylthiazol-2-yl)benzenesulfonamides as High-Affinity Inhibitors of Kynurenine 3-Hydroxylase by Röver, Stephan, Cesura, Andrea M, Huguenin, Philipp, Kettler, Rolf, Szente, Andre

“…In this paper we describe the synthesis, structure−activity relationship (SAR), and biochemical characterization of N-(4-phenylthiazol-2-yl)benzenesulfonamides…”
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Synthesis of (1S,3aS)-8-(2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one, a potent and selective orphanin FQ (OFQ) receptor agonist with anxiolytic-like properties by Wichmann, Jürgen, Adam, Geo, Röver, Stephan, Hennig, Michael, Scalone, Michelangelo, Cesura, Andrea M, Dautzenberg, Frank M, Jenck, François

“…The development of 8-(2,3,3a,4,5,6-hexahydro-1H-phenalen1-yl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones 3 starting from…”
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Increased monoamine oxidase B activity in plaque-associated astrocytes of Alzheimer brains revealed by quantitative enzyme radioautography by Saura, J, Luque, J M, Cesura, A M, Da Prada, M, Chan-Palay, V, Huber, G, Löffler, J, Richards, J G

“…The aetiology and pathogenesis of Alzheimer's disease are currently poorly understood, but symptomatic disease is associated with amyloid plaques,…”
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High-Affinity, Non-Peptide Agonists for the ORL1 (Orphanin FQ/Nociceptin) Receptor by Röver, Stephan, Adam, Geo, Cesura, Andrea M, Galley, Guido, Jenck, François, Monsma, Frederick J, Wichmann, Jürgen, Dautzenberg, Frank M

“…The discovery of 8-(5,8-dichloro-1,2,3,4-tetrahydro-naphthalen-2-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one, 1a, as a high-affinity ligand for the human…”
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Regulation of the kynurenine metabolic pathway by interferon-gamma in murine cloned macrophages and microglial cells by Alberati-Giani, D, Ricciardi-Castagnoli, P, Köhler, C, Cesura, A M

“…Several pieces of evidence suggest a major role for brain macrophages in the overproduction of neuroactive kynurenines, including quinolinic acid, in brain…”
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8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists by Wichmann, Jürgen, Adam, Geo, Röver, Stephan, Cesura, Andrea M., Dautzenberg, Frank M., Jenck, François

“…A series of 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives 1 was studied with respect to the binding affinity for the orphanin FQ…”
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The Voltage-dependent Anion Channel Is the Target for a New Class of Inhibitors of the Mitochondrial Permeability Transition Pore by Cesura, Andrea M., Pinard, Emmanuel, Schubenel, Robert, Goetschy, Valerie, Friedlein, Arno, Langen, Hanno, Polcic, Peter, Forte, Michael A., Bernardi, Paolo, Kemp, John A.

“…The relevance of the mitochondrial permeability transition pore (PTP) in Ca2+ homeostasis and cell death has gained wide attention. Yet, despite detailed…”
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Differential regulation of indoleamine 2,3-dioxygenase expression by nitric oxide and inflammatory mediators in IFN-gamma-activated murine macrophages and microglial cells by Alberati-Giani, D, Malherbe, P, Ricciardi-Castagnoli, P, Kohler, C, Denis- Donini, S, Cesura, AM

“…Induction of indoleamine 2,3-dioxygenase (IDO) and nitric oxide synthase (NOS) is involved in the immunomodulatory roles of IFN-gamma and evidence suggests…”
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Expression of the kynurenine enzymes in macrophages and microglial cells: regulation by immune modulators by Alberati-Giani, D, Cesura, A M

“…The regulation of the expression of indoleamine 2,3-dioxygenase (IDO) was studied in cloned murine macrophages (MT2) and microglial (N11) cells. Both cell…”
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The new generation of monoamine oxidase inhibitors by Cesura, A M, Pletscher, A

“…Irreversible and unspecific inhibitors of MAO were the first modern antidepressants, but after an initial success they fell into discredit due to adverse side…”
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ORL1 receptor ligands : Structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4,5]decan-4-ones by ROVER, S, WICHMANN, J, JENCK, F, ADAM, G, CESURA, A. M

“…We have investigated 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-o nes as ligands for the ORL1 receptor. These unsophisticated, achiral compounds show…”
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Biochemistry and pharmacology of moclobemide, a prototype RIMA by HAEFELY, W, BURKARD, W. P, CESURA, A. M, KETTLER, R, LOREZ, H. P, MARTIN, J. R, RICHARDS, J. G, SCHERSCHLICHT, R, DA PRADA, M

“…RIMA is a term for reversible inhibitors of monoamine oxidase (MAO) with preference for MAO-A; moclobemide is a prototype of this new class of antidepressants…”
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Molecular cloning and functional expression of human 3-hydroxyanthranilic-acid dioxygenase by Malherbe, P, Köhler, C, Da Prada, M, Lang, G, Kiefer, V, Schwarcz, R, Lahm, H W, Cesura, A M

“…Increased cerebral levels of the endogenous excitotoxin quinolinic acid (QUIN) have been speculatively linked to neuronal damage following neurological and…”
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Monoamine oxidase-A inhibitors and dopamine metabolism in rat caudatus: evidence that an increased cytosolic level of dopamine displaces reversible monoamine oxidase-A inhibitors in vivo by Colzi, A, D'Agostini, F, Cesura, A M, Borroni, E, Da Prada, M

“…The effects of reversible inhibitors of monoamine oxidase-A (moclobemide, Ro 41-1049, both 20 mg/kg, i.p., and brofaromine, 10 mg/kg, i.p.) on the outflow of…”
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Cloning and characterization of a soluble kynurenine aminotransferase from rat brain: identity with kidney cysteine conjugate beta-lyase by Alberati-Giani, D, Malherbe, P, Köhler, C, Lang, G, Kiefer, V, Lahm, H W, Cesura, A M

“…In this study, we describe the cloning and characterization of a soluble form of kynurenine aminotransferase (KAT, EC 2.6.1.7) present in rat brain. Soluble…”
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The histamine H3 receptor as a therapeutic drug target for CNS disorders by Gemkow, Mark J., Davenport, Adam J., Harich, Silke, Ellenbroek, Bart A., Cesura, Andrea, Hallett, David

“…The histamine H3 receptor plays a regulatory role in the pre-synaptic release of histamine and other neurotransmitters, making it an attractive target for CNS…”
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Characterisation of wild-type and mutant forms of human monoamine oxidase A and B expressed in a mammalian cell line by Gottowik, Jürgen, Cesura, Andrea M., Malherbe, Parichehr, Lang, Gabrielle, Da Prada, Mosé

“…Monoamine oxidase (MAO)-A and MAO-B are FAD-containing mitochondrial enzymes which catabolize biogenic and xenobiotic amines. The N-terminal regions of both…”
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The role of monoamine oxidase and catechol O-methyltransferase in dopaminergic neurotransmission by Napolitano, A, Cesura, A M, Da Prada, M

“…The action of dopamine (DA) released in the synaptic cleft is mainly terminated by its reuptake and catabolism by the enzymes monoamine oxidase (MAO) and…”
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Cloning and functional expression of a soluble form of kynurenine/alpha-aminoadipate aminotransferase from rat kidney by Buchli, R, Alberati-Giani, D, Malherbe, P, Köhler, C, Broger, C, Cesura, A M

“…Several aminotransferases with kynurenine aminotransferase (KAT) activity are able to convert L-kynurenine into kynurenic acid, a putative endogenous modulator…”
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