期刊
INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY
卷 12, 期 8, 页码 1127-1131出版社
CAMBRIDGE UNIV PRESS
DOI: 10.1017/S1461145709990204
关键词
Acetylcholinesterase inhibitor; donepezil; PET; sigma(1) receptor; [C-11]SA4503
资金
- Japan Society for the Promotion of Science. [19390301, 20390334]
- Grants-in-Aid for Scientific Research [20390334, 19390301] Funding Source: KAKEN
The acetylcholinesterase (AChE) inhibitor donepezil is also a sigma(1) receptor agonist. We examined whether donepezil binds to a, receptors in the living human brain after a single oral administration. Dynamic positron emission tomography (PET) data acquisition using the selective sigma(1) receptor ligand [C-11]SA4503 was performed to evaluate quantitatively the binding of [C-11]SA4503 to at receptors in eight healthy male volunteers. Each subject had a PET scan before and after receiving a single dose of donepezil (5 or 10 mg). The binding potential of [C-11]SA4503 was calculated. Doses of 5 mg and 10 mg donepezil bound to a, receptors in the human brain with occupancies of similar to 60% and similar to 75%, respectively, in a dose-dependent manner. This study demonstrated that donepezil binds to sigma(1) receptors in the Living human brain at therapeutic doses. Therefore, sigma(1) receptors may be implicated in the pharmacological mechanism of donepezil in the human brain.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据