Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists
ACS Medicinal Chemistry Letters2013Vol. 4(4), pp. 419–422
Citations Over TimeTop 10% of 2013 papers
Michael A. Letavic, Brian Lord, François Bischoff, Natalie A. Hawryluk, Serge Pieters, Jason C. Rech, Zachary S. Sales, Adriana I. Velter, Hong Ao, Pascal Bonaventure, Víctor Contreras, Xiaohui Jiang, Kirsten L. Morton, Brian Scott, Qi Wang, Alan D. Wickenden, Nicholas I. Carruthers, Anindya Bhattacharya
Abstract
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.
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