Search Results - "KEHLER, Jan"

PDE10A inhibitors: novel therapeutic drugs for schizophrenia by Kehler, Jan, Nielsen, Jacob

“…Disturbances of the basal ganglia processes is heavily involved in schizophrenia. Phosphodiesterase 10A (PDE10A) is a basal ganglia specific hydrolase, which…”
Get more information

In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1 by Thiesen, Louise, Kehler, Jan, Clausen, Rasmus P, Frølund, Bente, Bundgaard, Christoffer, Wellendorph, Petrine

“…γ-Hydroxybutyric acid (GHB) is a recreational drug, a clinically prescribed drug in narcolepsy and alcohol dependence, and an endogenous substance that binds…”
Get more information

From pan-reactive KV7 channel opener to subtype selective opener/inhibitor by addition of a methyl group by Blom, Sigrid Marie, Rottländer, Mario, Kehler, Jan, Bundgaard, Christoffer, Schmitt, Nicole, Jensen, Henrik Sindal

“…The voltage-gated potassium channels of the KV7 family (KV7.1-5) play important roles in controlling neuronal excitability and are therefore attractive targets…”
Get full text

Discovery of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1 by Jensen, Anders A, Erichsen, Mette N, Nielsen, Christina W, Stensbøl, Tine B, Kehler, Jan, Bunch, Lennart

“…The discovery of the first class of subtype-selective inhibitors of the human excitatory amino acid transporter subtype 1 (EAAT1) and its rat orthologue GLAST…”
Get full text

Discovery and development of 11C-Lu AE92686 as a radioligand for PET imaging of phosphodiesterase10A in the brain by Kehler, Jan, Kilburn, John Paul, Estrada, Sergio, Christensen, Søren Rahn, Wall, Anders, Thibblin, Alf, Lubberink, Mark, Bundgaard, Christoffer, Brennum, Lise Tøttrup, Steiniger-Brach, Björn, Christoffersen, Claus Tornby, Timmermann, Stine, Kreilgaard, Mads, Antoni, Gunnar, Bang-Andersen, Benny, Nielsen, Jacob

“…Phosphodiesterase 10A (PDE10A) plays a key role in the regulation of brain striatal signaling, and several pharmaceutical companies currently investigate…”
Get full text

Synthesis of enantiomerically pure milnacipran analogs and inhibition of dopamine, serotonin, and norepinephrine transporters by Roggen, Heidi, Kehler, Jan, Stensbøl, Tine Bryan, Hansen, Tore

“…Two enantiomeric series of milnacipran analogs have been synthesized and their effects on 5-HT, NE, and DA uptake inhibition have been measured. A series of…”
Get full text

Phosphodiesterase 10A inhibitors: a 2009 - 2012 patent update by Kehler, Jan

“…Inhibitors of the phosphodiesterase enzyme PDE10A have been the target for extensive investigations and huge drug discovery research efforts during the recent…”
Get more information

Patented PDE10A inhibitors: novel compounds since 2007 by Kehler, Jan, Kilburn, John Paul

“…PDE10A inhibition has generated much excitement as a potential novel mechanism for the treatment of the positive symptoms of schizophrenia. PDE10A is only '10…”
Get more information

Phosphodiesterase type 1 inhibition alters medial prefrontal cortical activity during goal-driven behaviour and partially reverses neurophysiological deficits in the rat phencyclidine model of schizophrenia by Hayes, Jessica, Laursen, Bettina, Eneberg, Elin, Kehler, Jan, Rasmussen, Lars Kyhn, Langgard, Morten, Bastlund, Jesper F., Gerdjikov, Todor V.

“…Positive modulation of cAMP signalling by phosphodiesterase (PDE) inhibitors has recently been explored as a potential target for the reversal of cognitive and…”
Get full text

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…”
Get full text

Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors by Dore, Antonio, Asproni, Battistina, Scampuddu, Alessia, Pinna, Gerard Aime, Christoffersen, Claus Tornby, Langgård, Morten, Kehler, Jan

“…Novel pyrazolo[5,1-f][1,6]naphthyridines, pyrazolo[5,1-a][2,6]naphthyridines, pyrazolo[5,1-a][2,7]naphthyridines and pyrazolo[5,1-a]isoquinolines…”
Get full text

Ortho lithiation-in situ borylation of substituted morpholine benzamides by Cederbalk, Anna, Lysén, Morten, Kehler, Jan, Kristensen, Jesper L.

“…Morpholine amides are cheap and safe alternative to Weinreb amides as acylating agents of organometallic species. Herein, the in-situ lithiation/borylation of…”
Get full text

Novel selective PDE type 1 inhibitors cause vasodilatation and lower blood pressure in rats by Laursen, Morten, Beck, Lilliana, Kehler, Jan, Christoffersen, Claus Tornby, Bundgaard, Christoffer, Mogensen, Susie, Mow, Tomas Joachim, Pinilla, Estéfano, Knudsen, Jakob Schöllhammer, Hedegaard, Elise Røge, Grunnet, Morten, Simonsen, Ulf

“…Background and Purpose The PDE enzymes (PDE1–11) hydrolyse and thus inactivate cyclic nucleotides and are important in the regulation of the cardiovascular…”
Get full text

PDE1A inhibition elicits cGMP‐dependent relaxation of rat mesenteric arteries by Khammy, Makhala Michell, Dalsgaard, Thomas, Larsen, Peter Hjørringgaard, Christoffersen, Claus Tornby, Clausen, Dorte, Rasmussen, Lars Kyhn, Folkersen, Lasse, Grunnet, Morten, Kehler, Jan, Aalkjær, Christian, Nielsen, Jacob

“…Background and Purpose PDE1, a subfamily of cyclic nucleotide PDEs consisting of three isoforms, PDE1A, PDE1B and PDE1C, has been implicated in the regulation…”
Get full text

Discovery of 2‑(Imidazo[1,2‑b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ‑Hydroxybutyric Acid (GHB) High-Affinity Binding Sites by Krall, Jacob, Bavo, Francesco, Falk-Petersen, Christina B, Jensen, Claus H, Nielsen, Julie O, Tian, Yongsong, Anglani, Valeria, Kongstad, Kenneth T, Piilgaard, Louise, Nielsen, Birgitte, Gloriam, David E, Kehler, Jan, Jensen, Anders A, Harpsøe, Kasper, Wellendorph, Petrine, Frølund, Bente

“…Gabazine, a γ-aminobutyric acid type A (GABAA) receptor antagonist, has previously been reported to inhibit the binding of [3H]­NCS-382, a representative…”
Get full text

Potentiation of NGF-induced neurite outgrowth in PC12 cells by papaverine: Role played by PLC-γ, IP3 receptors by Itoh, Kanako, Ishima, Tamaki, Kehler, Jan, Hashimoto, Kenji

“…Abstract Papaverine, an inhibitor of phosphodiesterase (PDE) 10A, is gaining attention for its potential in the treatment of neuropsychiatric diseases such as…”
Get full text

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…”
Get full text

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…”
Get full text

Molecular Hybridization of Potent and Selective γ‑Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3‑Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analogs by Krall, Jacob, Jensen, Claus Hatt, Bavo, Francesco, Falk-Petersen, Christina Birkedahl, Haugaard, Anne Stæhr, Vogensen, Stine Byskov, Tian, Yongsong, Nittegaard-Nielsen, Mia, Sigurdardóttir, Sara Björk, Kehler, Jan, Kongstad, Kenneth Thermann, Gloriam, David E, Clausen, Rasmus Prætorius, Harpsøe, Kasper, Wellendorph, Petrine, Frølund, Bente

“…γ-Hydroxybutyric acid (GHB) is a neuroactive substance with specific high-affinity binding sites. To facilitate target identification and ligand optimization,…”
Get full text

Correlating the Metabolic Stability of Psychedelic 5-HT2A Agonists with Anecdotal Reports of Human Oral Bioavailability by Leth-Petersen, Sebastian, Bundgaard, Christoffer, Hansen, Martin, Carnerup, Martin A., Kehler, Jan, Kristensen, Jesper Langgaard

“…2,5-Dimethoxyphenethylamines and their N -benzylated derivatives are potent 5-HT 2A agonists with psychedelic effects in humans. The N -benzylated derivatives…”
Get full text