Search Results - "Christoffersen, Claus T."

Novel Aza-analogous Ergoline Derived Scaffolds as Potent Serotonin 5‑HT6 and Dopamine D2 Receptor Ligands by Krogsgaard-Larsen, Niels, Jensen, Anders A, Schrøder, Tenna J, Christoffersen, Claus. T, Kehler, Jan

“…By introducing distal substituents on a tetracyclic scaffold resembling the ergoline structure, two series of analogues were achieved exhibiting subnanomolar…”
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A mouse model of the schizophrenia-associated 1q21.1 microdeletion syndrome exhibits altered mesolimbic dopamine transmission by Nielsen, Jacob, Fejgin, Kim, Sotty, Florence, Nielsen, Vibeke, Mørk, Arne, Christoffersen, Claus T., Yavich, Leonid, Lauridsen, Jes B., Clausen, Dorte, Larsen, Peter H., Egebjerg, Jan, Werge, Thomas M., Kallunki, Pekka, Christensen, Kenneth V., Didriksen, Michael

“…1q21.1 hemizygous microdeletion is a copy number variant leading to eightfold increased risk of schizophrenia. In order to investigate biological alterations…”
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Insulin and cortisol promote leptin production in cultured human fat cells by WABITSCH, M, JENSEN, P. B, BLUM, W. F, CHRISTOFFERSEN, C. T, ENGLARO, P, HEINZE, E, RASCHER, W, TELLER, W, TORNQVIST, H, HAUNER, H

“…The aim of this study was to investigate the regulation of leptin expression and production in cultured human adipocytes using the model of in vitro…”
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Phosphodiesterase 1 Bridges Glutamate Inputs with NO- and Dopamine-Induced Cyclic Nucleotide Signals in the Striatum by Betolngar, Dahdjim B, Mota, Élia, Fabritius, Arne, Nielsen, Jacob, Hougaard, Charlotte, Christoffersen, Claus T, Yang, Jun, Kehler, Jan, Griesbeck, Oliver, Castro, Liliana R V, Vincent, Pierre

“…Abstract The calcium-regulated phosphodiesterase 1 (PDE1) family is highly expressed in the brain, but its functional role in neurones is poorly understood…”
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Debenzylative Cycloetherification as a Synthetic Tool in the Diastereoselective Synthesis of 3,6-Disubstituted Hexahydro-2 H -furo[3,2- b ]pyrroles, PDE1 Enzyme Inhibitors with an Antiproliferative Effect on Melanoma Cells by Castán, Alejandro, Badorrey, Ramón, Díez, José A, Christoffersen, Claus T, Rasmussen, Lars K, Kehler, Jan, Köhler, Ralf, Gálvez, José A, Díaz-de-Villegas, María D

“…Two series of novel chiral hexahydro-2 -furo[3,2- ]pyrroles, 4-(7,8-dimethoxyquinazolin-4-yl) series A and 4-(6,7- dimethoxyquinazolin-4-yl) series B, were…”
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Debenzylative Cycloetherification as a Synthetic Tool in the Diastereoselective Synthesis of 3,6-Disubstituted Hexahydro‑2H‑furo[3,2‑b]pyrroles, PDE1 Enzyme Inhibitors with an Antiproliferative Effect on Melanoma Cells by Castán, Alejandro, Badorrey, Ramón, Díez, José A, Christoffersen, Claus T, Rasmussen, Lars K, Kehler, Jan, Köhler, Ralf, Gálvez, José A, Díaz-de-Villegas, María D

“…Two series of novel chiral hexahydro-2H-furo­[3,2-b]­pyrroles, 4-(7,8-dimethoxyquinazolin-4-yl) series A and 4-(6,7- dimethoxyquinazolin-4-yl) series B, were…”
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In vitro and in vivo characterisation of Lu AF64280, a novel, brain penetrant phosphodiesterase (PDE) 2A inhibitor: potential relevance to cognitive deficits in schizophrenia by Redrobe, John P., Jørgensen, Morten, Christoffersen, Claus T., Montezinho, Liliana P., Bastlund, Jesper F., Carnerup, Martin, Bundgaard, Christoffer, Lerdrup, Linda, Plath, Niels

“…Here, we present the pharmacological characterisation of Lu AF64280, a novel, selective, brain penetrant phosphodiesterase (PDE) 2A inhibitor, in in vitro/in…”
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Characterisation of Lu AF33241: A novel, brain-penetrant, dual inhibitor of phosphodiesterase (PDE) 2A and PDE10A by Redrobe, John P., Rasmussen, Lars K., Christoffersen, Claus T., Bundgaard, Christoffer, Jørgensen, Morten

“…Here, we present a preliminary pharmacological characterisation of Lu AF33241, a novel, brain penetrant phosphodiesterase inhibitor of (PDE) 2A and 10A tool…”
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Elucidation of fluorine's impact on pKa and in vitro Pgp-mediated efflux for a series of PDE9 inhibitors by Kasper Fjelbye, Marigo, Mauro, Clausen, Rasmus P, Jørgensen, Erling B, Christoffersen, Claus T, Juhl, Karsten

“…P-Glycoprotein (Pgp)-mediated cellular efflux is recognized as a common challenge in CNS drug discovery. In this study, the influence of replacing a hydrogen…”
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Elucidation of fluorine's impact on p K a and in vitro Pgp-mediated efflux for a series of PDE9 inhibitors by Fjelbye, Kasper, Marigo, Mauro, Clausen, Rasmus P, Jørgensen, Erling B, Christoffersen, Claus T, Juhl, Karsten

“…P-Glycoprotein (Pgp)-mediated cellular efflux is recognized as a common challenge in CNS drug discovery. In this study, the influence of replacing a hydrogen…”
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Poster #S202 CHARACTERIZATION OF A NUMBER OF ATYPICAL ANTIPSYCHOTICS IN VITRO by Christoffersen, Claus T, Holm, K, Ruskov-Nielsen, A, Nielsen, J

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Discovery of novel α1-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands by Jørgensen, Morten, Jørgensen, Pernille N., Christoffersen, Claus T., Jensen, Klaus G., Balle, Thomas, Bang-Andersen, Benny

“…The synthesis and in vitro preclinical profile of a series of 5-heteroaryl substituted analogs of the antipsychotic drug sertindole are presented. Compounds…”
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Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors by Kristensen, Jesper L, Püschl, Ask, Jensen, Martin, Risgaard, Rune, Christoffersen, Claus T, Bang-Andersen, Benny, Balle, Thomas

“…A series of 1-(10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine analogues substituted in the 8-position of the 10,11-dihydrodibenzo[b,f]thiepine…”
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Synthesis and SAR study of a novel series of dopamine receptor agonists by Risgaard, Rune, Jensen, Martin, Jørgensen, Morten, Bang-Andersen, Benny, Christoffersen, Claus T., Jensen, Klaus G., Kristensen, Jesper L., Püschl, Ask

“…The synthesis of a novel series of dopamine receptor agonists are described as well as their in vitro potency and efficacy on dopamine D1 and D2 receptors…”
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Exploring the Neuroleptic Substituent in Octoclothepin: Potential Ligands for Positron Emission Tomography with Subnanomolar Affinity for α1-Adrenoceptors by Kristensen, Jesper L, Püschl, Ask, Jensen, Martin, Risgaard, Rune, Christoffersen, Claus T, Bang-Andersen, Benny, Balle, Thomas

“…A series of 1-(10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine analogues substituted in the 8-position of the 10,11-dihydrodibenzo[b,f]thiepine…”
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Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based ω-acidic amino acids as glutamate receptors ligands by Filosa, Rosanna, Carmela Fulco, M., Marinozzi, Maura, Giacchè, Nicola, Macchiarulo, Antonio, Peduto, Antonella, Massa, Antonio, de Caprariis, Paolo, Thomsen, Christian, Christoffersen, Claus T., Pellicciari, Roberto

“…A novel series of bicyclo[1.1.1]pentane-based ω-acidic amino acids, including (2 S)- and (2 R)-3-(3′-carboxybicyclo[1.1.1]pentyl)alanines ( 8 and 9), (2 S)-…”
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Lu 35-138 ( (+ ) -(S ) -3-{1 -[2 -(1 -acetyl -2,3 -dihydro -1H -indol -3 -yl )ethyl] -3, 6 -dihydro -2H -pyridin -4 -yl} -6 -chloro -1H -indole ), a dopamine D4 receptor antagonist and serotonin reuptake inhibitor : Characterisation of its in vitro profile and pre-clinical antipsychotic potential by HERTEL, Peter, DIDRIKSEN, Michael, DI MAFLEO, Vincenzo, ESPOSITO, Ennio, BANG-ANDERSEN, Benny, ARMT, Jøm, POUZET, Bruno, BRENNUM, Lise T, SØBY, Karina K, LARSEN, Anna Kirstine, CHRISTOFFERSEN, Claus T, RAMIREZ, Teresa, MARCUS, Monica M, SVENSSON, Torgny H

“…The present study describes the pharmacological profile of the putative antipsychotic drug Lu 35-138…”
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Development of an aequorin luminescence calcium assay for high-throughput screening using a plate reader, the LumiLux by Menon, Veena, Ranganathn, Arun, Jorgensen, Vincent H, Sabio, Michael, Christoffersen, Claus T, Uberti, Michelle A, Jones, Kenneth A, Babu, Poda Suresh

“…A luminescence assay using a new plate reader, the LumiLux (PerkinElmer, Waltham, MA), has been validated for high-throughput screening (HTS). In this study,…”
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IRS-4 mediated mitogenic signalling by insulin and growth hormone in LB cells, a murine T-cell lymphoma devoid of IGF-I receptors by Ursø, Birgitte, Ilondo, M.Mapoko, Holst, Patricia A, Christoffersen, Claus T, Ouwens, Margriet, Giorgetti, Sophie, Van Obberghen, E, Naor, David, Tornqvist, Hans, De Meyts, Pierre

“…Insulin and growth hormone (GH) induce mitogenic and metabolic signals in cells, GH either directly or indirectly via IGF-I production. We have studied a…”
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PROGRESS TOWARDS AN A‐SYNUCLEIN PET TRACER by Tempest, Paul, Tai, Chin‐Yin, Ono, Maiko, Skaddan, Marc B, Wilcox, Kyle C, Reed, Aimee, Vaidyanathan, Srirajan, Christoffersen, Claus T, Kallunki, Pekka, Bang‐Andersen, Benny, Margolin, Richard A, Kao, Tzu‐Huei, Higuchi, Makoto, Jang, Ming‐Kuei

“…Background The high value for Parkinson’s disease and related disorders of the availability of a potent, selective, brain penetrant α‐synuclein (α‐Syn) PET…”
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