The first CNS-active carborane: A novel P2X7 receptor antagonist with antidepressant activity.

Shane M Wilkinson,Hendra Gunosewoyo,Melissa L Barron,Aurelie Boucher,Michelle McDonnell,Peter Turner,Daniel E Morrison,Maxwell R Bennett,Iain S McGregor,Louis M Rendina,Michael Kassiou

ACS chemical neuroscience（2014）

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摘要

Relative to other polycyclic frameworks (1-3), a carborane cage (4 and Cs·5) exerts a significant biological effect as an inhibitor of the purinergic P2X7 receptor (P2X7R) which allows one to target depression in vivo and thus demonstrate, for the first time, that a carborane has the capacity to modify CNS activity.

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关键词

depression,central nervous system

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