Details

Autor(en) / Beteiligte

• Letavic, Michael A
• Lord, Brian
• Bischoff, Francois
• Hawryluk, Natalie A
• Pieters, Serge
• Rech, Jason C
• Sales, Zachary
• Velter, Adriana I
• Ao, Hong
• Bonaventure, Pascal
• Contreras, Victor
• Jiang, Xiaohui
• Morton, Kirsten L
• Scott, Brian
• Wang, Qi
• Wickenden, Alan D
• Carruthers, Nicholas I
• Bhattacharya, Anindya

Titel

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

Ist Teil von

• ACS medicinal chemistry letters, 2013-04, Vol.4 (4), p.419-422

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2013

Quelle

Elektronische Zeitschriftenbibliothek (Open access)

Beschreibungen/Notizen

• 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.