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Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead

This Letter describes the synthesis and SAR of two mGluR4 positive allosteric modulator leads, 6 and 7. VU001171 (6) represents the most potent (EC(50) = 650 nM), efficacious (141% Glu Max) and largest fold shift (36-fold) of any mGluR4 PAM reported to date. However, this work highlights the challen...

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書誌詳細
主要な著者: Williams, Richard, Niswender, Colleen M., Luo, Qingwei, Le, Uyen, Conn, P. Jeffrey, Lindsley, Craig W.
フォーマット: Artigo
言語:Inglês
出版事項: 2008
主題:
オンライン・アクセス:https://ncbi.nlm.nih.gov/pmc/articles/PMC3787871/
https://ncbi.nlm.nih.gov/pubmed/19097893
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2008.11.104
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