794479-16-6Relevant articles and documents
Novel Phenyl-Substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 Antagonists with Robust Target Engagement in Rat Brain
Chrovian, Christa C.,Soyode-Johnson, Akinola,Ao, Hong,Bacani, Genesis M.,Carruthers, Nicholas I.,Lord, Brian,Nguyen, Leslie,Rech, Jason C.,Wang, Qi,Bhattacharya, Anindya,Letavic, Michael A.
, p. 490 - 497 (2016)
Novel 5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists were optimized to allow for good blood-brain barrier permeability and high P2X7 target engagement in the brain of rats. Compound 25 (huP2X7 IC50 = 9 nM; rat P2X7 IC50