首个具有中枢神经系统活性的碳硼烷：一种具有抗抑郁活性的新型P2X7受体拮抗剂。
The first CNS-active carborane: A novel P2X7 receptor antagonist with antidepressant activity.
作者信息
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
机构信息
School of Chemistry, ‡Faculty of Health Science, §Discipline of Pharmacology, and ∥School of Psychology, Sydney University , NSW 2006, Australia.
出版信息
ACS Chem Neurosci. 2014 May 21;5(5):335-9. doi: 10.1021/cn500054n. Epub 2014 Apr 3.
Abstract
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.
摘要
相对于其他多环骨架（1-3），碳硼烷笼（4和Cs·5）作为嘌呤能P2X7受体（P2X7R）的抑制剂发挥显著的生物学效应，这使得其能够在体内靶向治疗抑郁症，从而首次证明碳硼烷具有调节中枢神经系统活性的能力。
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