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Benzimidazoles as potent and orally active mGlu5 receptor antagonists with an improved PK profile

Carcache, David and Vranesic, Ivan-Toma and Blanz, Joachim and Desrayaud, Sandrine and Fendt, Markus and Glatthar, Ralf (2011) Benzimidazoles as potent and orally active mGlu5 receptor antagonists with an improved PK profile. ACS Medicinal Chemistry Letters, 2 (1). pp. 58-62. ISSN 1948-5875

Abstract

A focused chemical optimization effort of compound 1 based on metabolite elucidation is described, resulting in 15i, a highly potent and selective mGlu5 receptor antagonist with an improved pharmacokinetic profile compared to 1. Characterization of 15i in vivo in the fear-potentiated startle (FPS) paradigm revealed a robust reduction of conditioned fear behavior. This effect nicely correlates with the rat brain pharmacokinetics.

Item Type: Article
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Additional Information: archiving not formally supported by this publisher
Keywords: mGlu5; benzimidazoles; pharmacokinetics
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Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16
URI: https://oak.novartis.com/id/eprint/3352

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