Výsledky vyhledávání - "Claudia Kratzeisen"

Mapping the Binding Pocket of Dual Antagonist Almorexant to Human Orexin 1 and Orexin 2 Receptors: Comparison with the Selective OX1 Antagonist SB-674042 and the Selective OX2 Antagonist N-Ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA)

Autor: Anne Marcuz, Pari Malherbe, Olivier Roche, Claudia Kratzeisen, Joseph G. Wettstein, Caterina Bissantz

Publikováno v: Molecular Pharmacology. 78:81-93

The orexins and their receptors are involved in the regulation of arousal and sleep–wake cycle. Clinical investigation with almorexant has indicated that this dual OX antagonist is efficacious in inducing and maintaining sleep. Using site-directed

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::195e5c9b026ae9d3fbafdc0bc260a541
https://doi.org/10.1124/mol.110.064584

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Mutational Analysis and Molecular Modeling of the Binding Pocket of the Metabotropic Glutamate 5 Receptor Negative Modulator 2-Methyl-6-(phenylethynyl)-pyridine

Autor: Christophe Fischer, Marie-Théeése Zenner, Nicole A. Kratochwil, Catherine Diener, Claudia Kratzeisen, Porter Richard Hugh Phillip, Jenny Piussi, Pari Malherbe

Publikováno v: Molecular Pharmacology. 64:823-832

Metabotropic glutamate (mGlu) 5 is a G-protein-coupled metabotropic glutamate receptor that plays an important role as a modulator of synaptic plasticity, ion channel activity, and excitotoxicity. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP) is a highl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::927ad161812f783a01a4e6f9f81d7e86
https://doi.org/10.1124/mol.64.4.823

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Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8

Autor: Vincent Mutel, Kenneth Lundstrom, J. Grayson Richards, Claudia Kratzeisen, Richard L.M. Faull, Pari Malherbe

Publikováno v: Molecular Brain Research. 67:201-210

Two new spliced variants of the human metabotropic glutamate receptor 8 (HmGluR8), designated HmGluR8b and HmGluR8c, were identified in a human fetal brain cDNA library. The HmGluR8b and c differ from previously reported HmGluR8a by the out-of-frame

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a673aa25b2b4288a7e8e57290926a0e9
https://doi.org/10.1016/s0169-328x(99)00050-9

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Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and orexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA)

Autor: Pari, Malherbe, Olivier, Roche, Anne, Marcuz, Claudia, Kratzeisen, Joseph G, Wettstein, Caterina, Bissantz

Publikováno v: Molecular pharmacology. 78(1)

The orexins and their receptors are involved in the regulation of arousal and sleep-wake cycle. Clinical investigation with almorexant has indicated that this dual OX antagonist is efficacious in inducing and maintaining sleep. Using site-directed mu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e4309ac6088472546e26e699d9bae702
https://pubmed.ncbi.nlm.nih.gov/20404073

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Me-talnetant and osanetant interact within overlapping but not identical binding pockets in the human tachykinin neurokinin 3 receptor transmembrane domains

Autor: Claus Riemer, Marie-Thérèse Zenner, Hasane Ratni, Pari Malherbe, Claudia Kratzeisen, Joseph G. Wettstein, Anne Marcuz, Will Spooren, Caterina Bissantz

Publikováno v: Molecular pharmacology. 73(6)

Recent clinical trials have indicated that neurokinin 3 receptor antagonists (S)-(+)-N-{{3-[1-benzoyl-3-(3,4-dichlorophenyl)-piperidin-3-yl]prop-1-yl}-4-phenylpiperidin-4-yl}-N-methylacetamine (SR142801; osanetant) and (S)-(-)-N-(alpha-ethylbenzyl)-3

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6e40b9d11eecb84e35528523f9fa7b3
https://pubmed.ncbi.nlm.nih.gov/18308898

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Opposite effects of Zn on the in vitro binding of [3H]LY354740 to recombinant and native metabotropic glutamate 2 and 3 receptors

Autor: Clemens Broger, Pari Malherbe, Jürg Messer, Marie-Thérèse Zenner, J. Grayson Richards, Claudia Kratzeisen, Vincent Mutel, Shigetada Nakanishi

Publikováno v: Journal of neurochemistry. 94(1)

We investigated the effect of Zn on agonist binding to both recombinant and native mGlu2 and mGlu3 receptors. Zn had a biphasic inhibitory effect on recombinant mGlu2 with IC(50) values for the high- and low-affinity components of 60 +/- 10 microM an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f976e07479f8165c956ce3ee387399a
https://pubmed.ncbi.nlm.nih.gov/15953358

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Identification and characterization of a novel splice variant of the metabotropic glutamate receptor 5 gene in human hippocampus and cerebellum

Autor: James N.C. Kew, Pari Malherbe, John A. Kemp, J. Grayson Richards, Marie-Thérèse Zenner, Claudia Kratzeisen, Vincent Mutel, Richard L.M. Faull, Frédéric Knoflach

Publikováno v: Brain research. Molecular brain research. 109(1-2)

The G-protein coupled metabotropic glutamate receptor mGlu5 plays a pivotal role as a modulator of synaptic plasticity, ion channel activity and excitotoxicity. Two splice variants, hmGlu5a and -5b have been reported previously. During screening of a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d79166ce79371c2629f69fe32f73c52
https://pubmed.ncbi.nlm.nih.gov/12531526

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Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor

Autor: Pari Malherbe, Claudia Kratzeisen, Geo Adam, Vincent Mutel, Frédéric Knoflach, Nicole A. Kratochwil, Maerki Hans P, James N.C. Kew, Marie-Thérèse Zenner

Publikováno v: The Journal of biological chemistry. 278(10)

A model of the rmGlu1 seven-transmembrane domain complexed with a negative allosteric modulator, 1-ethyl-2-methyl-6-oxo-4-(1,2,4,5-tetrahydro-benzo[d]azepin-3-yl)- 1,6-dihydro-pyrimidine-5-carbonitrile (EM-TBPC) was constructed. Although the mGlu rec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa644a28bfa2896f9604ae8d1aeea131
https://pubmed.ncbi.nlm.nih.gov/12509432

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Identification of essential residues involved in the glutamate binding pocket of the group II metabotropic glutamate receptor

Autor: Geo Adam, Pari Malherbe, Heinz Stadler, Frédéric Knoflach, John A. Kemp, Vincent Mutel, Clemens Broger, Serge Ohresser, Claudia Kratzeisen

Publikováno v: Molecular pharmacology. 60(5)

Metabotropic glutamate (mGlu) receptors are a family of G-protein-coupled receptors that play central roles as modulators of both glutamatergic and other major neurotransmitter systems in CNS. Using molecular modeling, site-directed mutagenesis, [(3)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d861f25082e7f83363c982ca450cb4e5
https://pubmed.ncbi.nlm.nih.gov/11641422

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Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors

Autor: Serge Ohresser, Thomas Johannes Woltering, Kenneth Lundstrom, Claudia Kratzeisen, Geo Adam, Heinz Stadler, Jürgen Wichmann, Christophe Schweitzer, Vincent Mutel, Pari Malherbe

Publikováno v: Neuropharmacology. 39(10)

The binding properties of [(3)H]-LY354740 were characterized on rat metabotropic glutamate receptors mGlu2 and mGlu3 expressed in Chinese hamster ovary (CHO) cells using Semliki Forest virus vectors. The saturation isotherm gave K(D) values of 20+/-5

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88629df558ea5edfa6342ad1156af035
https://pubmed.ncbi.nlm.nih.gov/10884552

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