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Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives : Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists

Woltering, Thomas J. and Wichmann, Jürgen and Goetschi, Erwin and Knoflach, Frédéric and Ballard, Theresa M. and Huwyler, Jörg and Gatti, Silvia. (2010) Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives : Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists. Bioorganic & medicinal chemistry letters, Vol. 20, H. 23. pp. 6969-6974.

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Official URL: http://edoc.unibas.ch/dok/A5840214

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Abstract

This study completes a series of papers devoted to the characterization of the non-competitive mGluR2/3 antagonist properties of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives with particular emphasis on derivatizations compatible with brain penetration and in vivo activity. Especially the compounds bearing a para-pyridine consistently showed in vivo activity in rat behavioral models after oral administration, for example, blockade of the mGluR2/3 agonist LY354740-induced hypoactivity and improvement of a working memory deficit induced either by LY354740 or scopolamine in the delayed match to position task (DMTP). Moreover, combination studies with a cholinesterase inhibitor show apparent synergistic effects on working memory impairment induced by scopolamine.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmazeutische Technologie (Huwyler)
UniBasel Contributors:Huwyler, Jörg
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Pergamon
ISSN:0960-894X
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:08 Jun 2012 06:56
Deposited On:08 Jun 2012 06:51

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