Published April 3, 2014
| Version v1
Journal article
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The First CNS-Active Carbarone: A Novel P2X7 Receptor Antagonist with Antidepressant Activity.
Creators
- 1. School of Chemistry, Sydney University, NSW 2006, Australia
- 2. Faculty of Health Science, Sydney University, NSW 2006, Australia and Brain and Mind Research Institute, 100 Mallett Street, Camperdown, NSW 2050, Australia
- 3. Discipline of Pharmacology, Sydney University, NSW 2006, Australia and Brain and Mind Research Institute, 100 Mallett Street, Camperdown, NSW 2050, Australia
- 4. Brain and Mind Research Institute, 100 Mallett Street, Camperdown, NSW 2050, Australia
- 5. School of Psychology, Sydney University, NSW 2006, Australia
- 6. School of Chemistry and Faculty of Health Science, Sydney University, NSW 2006, Australia and Brain and Mind Research Institute, 100 Mallett Street, Camperdown, NSW 2050, Australia
Description
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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