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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...
Αποθηκεύτηκε σε:
| Κύριοι συγγραφείς: | , , , , , , , , , |
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| Μορφή: | Artigo |
| Γλώσσα: | Inglês |
| Έκδοση: |
2013
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| Θέματα: | |
| Διαθέσιμο Online: | 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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