کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2154927 1090264 2006 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Is subnanomolar binding affinity required for the in vivo imaging of acetylcholinesterase? Studies on 18F-labeled G379
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی تحقیقات سرطان
پیش نمایش صفحه اول مقاله
Is subnanomolar binding affinity required for the in vivo imaging of acetylcholinesterase? Studies on 18F-labeled G379
چکیده انگلیسی

Acetylcholinesterase (AChE) is an important cholinergic marker of Alzheimer's disease (AD) and shows reduced activity in postmortem AD brain tissues. 1-(4-Fluorobenzyl)-4-[(5,6-dimethoxy-1-oxoindan-2-fluoro-2-yl)methyl]piperidine (G379, 1), an AChE inhibitor with a subnanomolar IC50 (0.56 nM), was prepared as a 18F-labeled radioligand ([18F]1) and evaluated in mice. Metabolism studies of [18F]1 showed no metabolites in the mouse brain. Tissue distribution studies demonstrated its uniform regional distribution in the mouse brain, suggesting that this radioligand is not suitable for the in vivo imaging of AChE. This result along with reports on radiolabeled N-benzylpiperidine lactam benzisoxazole (IC50<1 nM) and other radiolabeled benzylpiperidine derivatives (IC50>1 nM) suggested that a subnanomolar IC50 may not be the only important factor in determining the suitability of a radioligand for in vivo studies of AChE.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Nuclear Medicine and Biology - Volume 33, Issue 1, January 2006, Pages 91–94
نویسندگان
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