Výsledky vyhledávání - "Graven Sams A"

Improvement of sensory deficits in Fragile X mice by increasing cortical interneuron activity after the critical period

Autor: Nazim Kourdougli, Anand Suresh, Benjamin Liu, Pablo Juarez, Ashley Lin, David T. Chung, Anette Graven Sams, Michael Gandal, Verónica Martínez-Cerdeño, Dean V. Buonomano, Benjamin J. Hall, Cédric Mombereau, Carlos Portera-Cailliau

SUMMARYChanges in the function of inhibitory interneurons (INs) during cortical development could contribute to the pathophysiology of neurodevelopmental disorders. Using all-optical in vivo approaches in postnatal mouse somatosensory cortex (S1), we

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a49a97dd2a7f48c78eb33fcd2ea43f10
https://doi.org/10.1101/2022.05.17.492368

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In vitro and in vivo characterization of Lu AA41178: A novel, brain penetrant, pan-selective Kv7 potassium channel opener with efficacy in preclinical models of epileptic seizures and psychiatric disorders

Autor: Mario Rottländer, Morten Grupe, Vibeke Nielsen, Anette Graven Sams, Anne-Marie Jacobsen, Henrik Sindal Jensen, Morten Grunnet, Jesper F. Bastlund, Kristen Frederiksen, Tau Benned-Jensen, Lasse Skibsbye, Bo Hjorth Bentzen

Publikováno v: European journal of pharmacology. 887

Activation of the voltage-gated Kv7 channels holds therapeutic promise in several neurological and psychiatric disorders, including epilepsy, schizophrenia, and depression. Here, we present a pharmacological characterization of Lu AA41178, a novel, p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f11517e28c5ef13a23733b29015ce53b
https://pubmed.ncbi.nlm.nih.gov/32745603

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Efficacy switching SAR of mGluR5 allosteric modulators: Highly potent positive and negative modulators from one chemotype

Autor: Anette Graven Sams, Gitte Mikkelsen, Andreas Ritzen, Xiaosui Pu, Robbin Brodbeck

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:3407-3410

A series of metabotropic glutamate 5 receptor (mGluR5) allosteric ligands with positive, negative or no modulatory efficacy is described. The ability of this series to yield both mGluR5 PAMs and NAMs with single-digit nanomolar potency is unusual, an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8240f41d29dcca0e37700b370af03a93
https://doi.org/10.1016/j.bmcl.2011.03.103

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Discovery of Phosphoric Acid Mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} Ester (Lu AA47070): A Phosphonooxymethylene Prodrug of a Potent and Selective hA2A Receptor Antagonist

Autor: Christoffer Bundgaard, Tenna Juul Schrøder, Lise T. Brennum, Anette Graven Sams, Mads Kreilgård, Lars Torup, Erling B. Jørgensen, Benny Bang-Andersen, Gitte Mikkelsen, Mogens Larsen, Mark Howells, Morten Langgård

Publikováno v: Journal of Medicinal Chemistry. 54:751-764

The discovery and structure-activity relationship of a series of hA(2A) receptor antagonists is described. Compound 28 was selected from the series as a potent and selective compound and was shown to be efficacious in an in vivo model of Parkinson's

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::39cb3c48de111fdebe006a572f20aa86
https://doi.org/10.1021/jm1008659

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Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential

Autor: Gitte Mikkelsen, Klaus Gjervig Jensen, Morten Hentzer, Benny Bang-Andersen, Krestian Larsen, Claus Tornby Christoffersen, Kristen Frederiksen, Anette Graven Sams

Publikováno v: Bioorganicmedicinal chemistry letters. 22(15)

We describe the discovery of a series of compounds based on 1-{3-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-propyl}-3,4-dihydro-1H-quinolin-2-one (3), showing combined D2 receptor affinity and M1 receptor agonism. Based on a strategy o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3be083bfd1f1913c58b08bfe93cb732d
https://pubmed.ncbi.nlm.nih.gov/22677319

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Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential

Autor: Christoffer Bundgaard, Niels Plath, Krestian Larsen, Anette Graven Sams, Benny Bang-Andersen, Gitte Mikkelsen, Morten Hentzer, Claus Tornby Christoffersen

Publikováno v: Journal of medicinal chemistry. 53(17)

The discovery and structure-activity relationship (SAR) of a series of allosteric muscarinic M(1) receptor agonists are described. Compound 17 (Lu AE51090) was identified as a representative compound from the series, based on its high selectivity as

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96fa99c262a7e8f40d80e669722718a9
https://pubmed.ncbi.nlm.nih.gov/20684563

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Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists

Autor: Lise T. Brennum, Mogens Larsen, Tenna Juul Schrøder, Lars Torup, Benny Bang-Andersen, Anette Graven Sams, Gitte Mikkelsen

Publikováno v: Bioorganicmedicinal chemistry letters. 20(17)

Herein we describe the discovery of a series of novel adenosine A2A receptor antagonists. A successful hit-to-lead optimization of an HTS hit led to replacement of a metabolically labile ester moiety with a heteroaromatic group. A compound from the s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db639a52355c4eb2525753a63220f6bf
https://pubmed.ncbi.nlm.nih.gov/20659802

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