| Autor: |
Brian Lord, Jason C. Rech, Brian Scott, Kirsten L. Morton, Nicholas I. Carruthers, Victor Contreras, Natalie A. Hawryluk, Qi Wang, Xiaohui Jiang, Francois Paul Bischoff, Michael A. Letavic, Alan D. Wickenden, Pascal Bonaventure, Hong Ao, Serge Maria Aloysius Pieters, Zachary S. Sales, Anindya Bhattacharya, Adriana Ingrid Velter |
| Rok vydání: |
2013 |
| Předmět: |
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| Zdroj: |
ACS Medicinal Chemistry Letters. 4:419-422 |
| ISSN: |
1948-5875 |
| DOI: |
10.1021/ml400040v |
| Popis: |
The synthesis and preclinical characterization of two novel, brain penetrating P2X7 compounds will be described. Both compounds are shown to be high potency P2X7 antagonists in human, rat, and mouse cell lines and both were shown to have high brain concentrations and robust receptor occupancy in rat. Compound 7 is of particular interest as a probe compound for the preclinical assessment of P2X7 blockade in animal models of neuro-inflammation. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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