Search Results - "Egerland, Ute"

Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia by Grauer, Steven M, Pulito, Virginia L, Navarra, Rachel L, Kelly, Michele P, Kelley, Cody, Graf, Radka, Langen, Barbara, Logue, Sheree, Brennan, Julie, Jiang, Lixin, Charych, Erik, Egerland, Ute, Liu, Feng, Marquis, Karen L, Malamas, Michael, Hage, Thorsten, Comery, Thomas A, Brandon, Nicholas J

“…Following several recent reports that suggest that dual cAMP and cGMP phosphodiesterase 10A (PDE10A) inhibitors may present a novel mechanism to treat positive…”
Get more information

Effect of PDE10A inhibitors on MK-801-induced immobility in the forced swim test by Langen, Barbara, Dost, Rita, Egerland, Ute, Stange, Hans, Hoefgen, Norbert

“…Rational Negative symptoms of schizophrenia are insufficiently treated by current antipsychotics. However, research is limited by the lack of validated models…”
Get full text

Highly Potent, Selective, and Orally Active Phosphodiesterase 10A Inhibitors by Malamas, Michael S, Ni, Yike, Erdei, James, Stange, Hans, Schindler, Rudolf, Lankau, Hans-Joachim, Grunwald, Christian, Fan, Kristi Yi, Parris, Kevin, Langen, Barbara, Egerland, Ute, Hage, Thorsten, Marquis, Karen L, Grauer, Steve, Brennan, Julie, Navarra, Rachel, Graf, Radka, Harrison, Boyd L, Robichaud, Albert, Kronbach, Thomas, Pangalos, Menelas N, Hoefgen, Norbert, Brandon, Nicholas J

“…The identification of highly potent and orally active phenylpyrazines for the inhibition of PDE10A is reported. The new analogues exhibit subnanomolar potency…”
Get full text

Investigation of an 18F-labelled Imidazopyridotriazine for Molecular Imaging of Cyclic Nucleotide Phosphodiesterase 2A by Schröder, Susann, Wenzel, Barbara, Deuther-Conrad, Winnie, Teodoro, Rodrigo, Kranz, Mathias, Scheunemann, Matthias, Egerland, Ute, Höfgen, Norbert, Briel, Detlef, Steinbach, Jörg, Brust, Peter

“…Specific radioligands for in vivo visualization and quantification of cyclic nucleotide phosphodiesterase 2A (PDE2A) by positron emission tomography (PET) are…”
Get full text

Radiosynthesis and biological evaluation of the new PDE10A radioligand [18F]AQ28A by Wagner, Sally, Teodoro, Rodrigo, Deuther‐Conrad, Winnie, Kranz, Mathias, Scheunemann, Matthias, Fischer, Steffen, Wenzel, Barbara, Egerland, Ute, Hoefgen, Norbert, Steinbach, Jörg, Brust, Peter

“…Cyclic nucleotide phosphodiesterase 10A (PDE10A) regulates the level of the second messengers cAMP and cGMP in particular in brain regions assumed to be…”
Get full text

Fluorine-Containing 6,7-Dialkoxybiaryl-Based Inhibitors for Phosphodiesterase 10 A: Synthesis and in vitro Evaluation of Inhibitory Potency, Selectivity, and Metabolism by Schwan, Gregor, Barbar Asskar, Ghadir, Höfgen, Norbert, Kubicova, Lenka, Funke, Uta, Egerland, Ute, Zahn, Michael, Nieber, Karen, Scheunemann, Matthias, Sträter, Norbert, Brust, Peter, Briel, Detlef

“…Based on the potent phosphodiesterase 10 A (PDE10A) inhibitor PQ‐10, we synthesized 32 derivatives to determine relationships between their molecular structure…”
Get full text

Synthesis, 18F-Radiolabelling and Biological Characterization of Novel Fluoroalkylated Triazine Derivatives for in Vivo Imaging of Phosphodiesterase 2A in Brain via Positron Emission Tomography by Schröder, Susann, Wenzel, Barbara, Deuther-Conrad, Winnie, Teodoro, Rodrigo, Egerland, Ute, Kranz, Mathias, Scheunemann, Matthias, Höfgen, Norbert, Steinbach, Jörg, Brust, Peter

“…Phosphodiesterase 2A (PDE2A) is highly and specifically expressed in particular brain regions that are affected by neurological disorders and in certain…”
Get full text

Anti-inflammatory potential of the selective phosphodiesterase 4 inhibitor N-(3,5-dichloro-pyrid-4-yl)-[1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), in human cell preparations by Draheim, Regina, Egerland, Ute, Rundfeldt, Chris

“…AWD 12-281 is a potent (IC(50) = 9.7 nM) and highly selective inhibitor of the phosphodiesterase 4 (PDE4) isoenzyme with low affinity to the high-affinity…”
Get more information

Characterization in rats of the anxiolytic potential of ELB139 [1-(4-chlorophenyl)-4-piperidin-1-yl-1,5-dihydro-imidazol-2-on], a new agonist at the benzodiazepine binding site of the GABAA receptor by Langen, Barbara, Egerland, Ute, Bernöster, Katrin, Dost, Rita, Unverferth, Klaus, Rundfeldt, Chris

“…Benzodiazepines are among the most effective drugs for the treatment of anxiety disorders. However, their use is limited by undesired side effects, including…”
Get more information

Discovery of triazines as potent, selective and orally active PDE4 inhibitors by Gewald, Rainer, Grunwald, Christian, Egerland, Ute

“…Expanding on HTS hit 4 afforded a series of [1,3,5]triazine derivatives as novel PDE4 inhibitors. The SAR development and optimization process with the…”
Get full text

Large-Scale Mining for Similar Protein Binding Pockets: With RAPMAD Retrieval on the Fly Becomes Real by Krotzky, Timo, Grunwald, Christian, Egerland, Ute, Klebe, Gerhard

“…Determination of structural similarities between protein binding pockets is an important challenge in in silico drug design. It can help to understand…”
Get full text

Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines by Wagner, Sally, Scheunemann, Matthias, Dipper, Karolin, Egerland, Ute, Hoefgen, Norbert, Steinbach, Jörg, Brust, Peter

“…Herein we report the synthesis of fluorinated inhibitors of phosphodiesterase 10A (PDE10A) which can be used potentially as lead structure for the development…”
Get full text

Synthesis and structure–activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors by Gewald, Rainer, Rueger, Carla, Grunwald, Christian, Egerland, Ute, Hoefgen, Norbert

“…The synthesis and SAR studies of a series of structurally novel inhibitors of PDE7 are discussed. The best compounds from the series display low nanomolar…”
Get full text

Discovery of Imidazo[1,5-a]pyrido[3,2-e]pyrazines as a New Class of Phosphodiesterase 10A Inhibitiors by Höfgen, Norbert, Stange, Hans, Schindler, Rudolf, Lankau, Hans-Joachim, Grunwald, Christian, Langen, Barbara, Egerland, Ute, Tremmel, Peter, Pangalos, Menelas N, Marquis, Karen L, Hage, Thorsten, Harrison, Boyd L, Malamas, Michael S, Brandon, Nicholas J, Kronbach, Thomas

“…Novel imidazo[1,5-a]pyrido[3,2-e]pyrazines have been synthesized and characterized as both potent and selective phosphodiesterase 10A (PDE10A) inhibitors. For…”
Get full text

New GABA-modulating 1,2,4-oxadiazole derivatives and their anticonvulsant activity by Lankau, Hans-Joachim, Unverferth, Klaus, Grunwald, Christian, Hartenhauer, Helge, Heinecke, Kristina, Bernöster, Katrin, Dost, Rita, Egerland, Ute, Rundfeldt, Chris

“…A series of 3- and 5-aryl-1,2,4-oxadiazole derivatives were prepared and tested for anticonvulsant activity in a variety of models. These 1,2,4-oxadiazoles…”
Get full text

Novel triazines as potent and selective phosphodiesterase 10A inhibitors by Malamas, Michael S., Stange, Hans, Schindler, Rudolf, Lankau, Hans-Joachim, Grunwald, Christian, Langen, Barbara, Egerland, Ute, Hage, Thorsten, Ni, Yike, Erdei, James, Fan, Kristi Yi, Parris, Kevin, Marquis, Karen L., Grauer, Steve, Brennan, Julie, Navarra, Rachel, Graf, Radka, Harrison, Boyd L., Robichaud, Albert, Kronbach, Thomas, Pangalos, Menelas N., Brandon, Nicholas J., Hoefgen, Norbert

“…Novel triazines are potent, selective and orally active Phosphodiestarase 10A inhibitors. The identification of highly potent and orally active triazines for…”
Get full text

Fluorine-Containing 6,7-Dialkoxybiaryl-Based Inhibitors for Phosphodiesterase10A: Synthesis and in vitro Evaluation of Inhibitory Potency, Selectivity, and Metabolism by Schwan, Gregor, BarbarAsskar, Ghadir, Hofgen, Norbert, Kubicova, Lenka, Funke, Uta, Egerland, Ute, Zahn, Michael, Nieber, Karen, Scheunemann, Matthias, Strater, Norbert, Brust, Peter, Briel, Detlef

“…Based on the potent phosphodiesterase10A (PDE10A) inhibitor PQ-10, we synthesized 32 derivatives to determine relationships between their molecular structure…”
Get full text

Investigation of an 18 F-labelled Imidazopyridotriazine for Molecular Imaging of Cyclic Nucleotide Phosphodiesterase 2A by Schröder, Susann, Wenzel, Barbara, Deuther-Conrad, Winnie, Teodoro, Rodrigo, Kranz, Mathias, Scheunemann, Matthias, Egerland, Ute, Höfgen, Norbert, Briel, Detlef, Steinbach, Jörg, Brust, Peter

“…Specific radioligands for in vivo visualization and quantification of cyclic nucleotide phosphodiesterase 2A (PDE2A) by positron emission tomography (PET) are…”
Get full text

Synthesis, Pharmacology, and Structure−Activity Relationships of Novel Imidazolones and Pyrrolones as Modulators of GABAA Receptors by Grunwald, Christian, Rundfeldt, Chris, Lankau, Hans-Joachim, Arnold, Thomas, Höfgen, Norbert, Dost, Rita, Egerland, Ute, Hofmann, Hans-Jörg, Unverferth, Klaus

“…New series of imidazolones and pyrrolones were synthesized. The compounds were tested regarding their anxiolytic properties due to modulation of the GABAA…”
Get full text

Synthesis, Pharmacology, and Structure−Activity Relationships of Novel Imidazolones and Pyrrolones as Modulators of GABA A Receptors by Grunwald, Christian, Rundfeldt, Chris, Lankau, Hans-Joachim, Arnold, Thomas, Höfgen, Norbert, Dost, Rita, Egerland, Ute, Hofmann, Hans-Jörg, Unverferth, Klaus

Get full text