Document Report Card

ID: ALA2331410

Journal: ACS Med Chem Lett

Title: Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.

Authors: Letavic MA, Lord B, Bischoff F, Hawryluk NA, Pieters S, Rech JC, Sales Z, Velter AI, Ao H, Bonaventure P, Contreras V, Jiang X, Morton KL, Scott B, Wang Q, Wickenden AD, Carruthers NI, Bhattacharya A.

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.

CiteXplore: 24900687

DOI: 10.1021/ml400040v