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Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists
[Image: see text] We describe the synthesis and SAR of 1,2,3-triazolopiperidines as a novel series of potent, brain penetrant P2X7 antagonists. Initial efforts yielded a series of potent human P2X7R antagonists with moderate to weak rodent potency, some CYP inhibition, poor metabolic stability, and...
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| Publicado en: | ACS Med Chem Lett |
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| Main Authors: | , , , , , , , , |
| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado: |
American Chemical
Society
2015
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| Acceso en liña: | https://ncbi.nlm.nih.gov/pmc/articles/PMC4468405/ https://ncbi.nlm.nih.gov/pubmed/26101572 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00089 |
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