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Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile

[Image: see text] 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 15iin vivo in the fear-potentiate...

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Detalhes bibliográficos
Main Authors: Carcache, David, Vranesic, Ivo, Blanz, Joachim, Desrayaud, Sandrine, Fendt, Markus, Glatthar, Ralf
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2010
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4018045/
https://ncbi.nlm.nih.gov/pubmed/24900255
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml100215b
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