Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , Name: 1,2-Bis(2-aminoethoxy)ethane, 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, molecular formula is C6H16N2O2, belongs to benzisoxazole compound. In a document, author is Lee, SY, introduce the new discover.
Is subnanomolar binding affinity required for the in vivo imaging of acetylcholinesterase? Studies on F-18-labeled G379
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-l-oxoindan-2-fluoro-2-yl)methyl]piperidine (G379, 1), an AChE inhibitor with a subnanomolar IC50 (0.56 nM), was prepared as a F-18-labeled radioligand ([F-18]1) and evaluated in mice. Metabolism studies of [F-18]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 AT-benzylpiperidine lactam benzisoxazole (IC50 < 1 nM) and other radiolabeled benzylpiperidme derivatives (IC50 > 1 nM) suggested that a subnanornolar IC50 may not be the only important factor in determining the suitability of a radioligand for in Vivo Studies of AChE. (c) 2006 Elsevier Inc. All rights reserved.
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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics