Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu(3) Selective and CNS Penetrant Negative Allosteric Modulator (NAM)

A multi-dimensional, iterative parallel synthesis effort identified a series of highly selective mGlu3 NAMs with sub-micromolar potency and good CNS penetration. Of these, ML337 resulted (mGlu(3) IC(50) = 593 nM, mGlu(2) IC(50) >30 μM) with B:P ratios of 0.92 (mouse) to 0.3 (rat). DMPK profiling...

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Xehetasun bibliografikoak
Egile Nagusiak: Wenthur, Cody J., Morrison, Ryan, Felts, Andrew S., Smith, Katrina A., Engers, Julie L., Byers, Frank W., Daniels, J. Scott, Emmitte, Kyle A., Conn, P. Jeffrey, Lindsley, Craig W.
Formatua: Artigo
Hizkuntza:Inglês
Argitaratua: 2013
Gaiak:
Article
Sarrera elektronikoa:https://ncbi.nlm.nih.gov/pmc/articles/PMC3769689/
https://ncbi.nlm.nih.gov/pubmed/23718281
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm400439t
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