Journal article Open Access

The First CNS-Active Carbarone: A Novel P2X7 Receptor Antagonist with Antidepressant Activity.

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

Relative to other polycyclic frameworks (13), 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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