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Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity

Spanka, Carsten and Glatthar, Ralf and Desrayaud, Sandrine and Fendt, Markus and Orain, David and Troxler, Thomas J. and Vranesic, Ivan-Toma (2010) Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity. Bioorganic & Medicinal Chemistry Letters, 20 (1). pp. 184-188. ISSN 0960-894X

Abstract

High throughput screening led to the identification of nicotinamide derivative 2 as a structurally novel mGluR5 antagonist. Optimization of the modular scaffold led to the discovery of 16m, a compound with high affinity for mGluR5 and excellent selectivity over other glutamate receptors. Compound 16m exhibits a favorable PK profile in rats, robust anxiolytic-like effects in three different animal models of fear and anxiety, as well as a good PK/PD correlation.

Item Type: Article
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Additional Information: Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Metabotropic glutamate receptor; mGluR5 antagonist; Piperidylamides
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Date Deposited: 13 Oct 2015 13:17
Last Modified: 13 Oct 2015 13:17
URI: https://oak.novartis.com/id/eprint/1141

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