Imaging of central nAChReceptors with 2-[¹⁸F]F-A85380: optimized synthesis and in vitro evaluation in Alzheimer's disease

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• 作者：Schmaljohann ; J. ; Minnerop ; M. ; Karwath ; P. ; Gü ; ndisch ; D. ; Falkai ; P. ; Guhlke ; S. ; Wü ; llner ; U.
• 关键词：Nicotinic acetylcholine receptor ; Fluorine-18 ; 2-¹⁸F-A85380 ; Alzheimer's disease ; PET
• 刊名：Applied Radiation and Isotopes
• 出版年：2004
• 期刊代码：6_09698043
• 类别：ce
• 出版时间：December, 2004
• 卷：61
• 期：6
• 页码：1235-1240
• 文件大小：358 K

摘要

In vivo labeling of the nicotinic acetylcholine receptors (nAChR) could be a useful tool for early diagnosis of neurodegenerative disorders. 2-[¹⁸F]F-A85380 (2-[¹⁸F]Fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine), a ligand with high affinity to the β2 subunit of the nAChRs, has been shown to label neurons in the nAChR-rich thalamus, cortex and striatum in baboons. We report an optimized synthesis resulting in an uncorrected yield of 58%in 45min (precursor 2), enabling efficient production intended for clinical use. Incubation of normal rat brain sections with 2-[¹⁸F]F-A85380 with subsequent autoradiographic analyses showed the expected distribution in nAChR areas. In human brain sections of Alzheimer's disease (AD) a decrease of 2-[¹⁸F]F-A85380 uptake to 36%of the control group was measured in the thalamus and also in the occipital cortex. These findings suggest that 2-[¹⁸F]F-A85380 is a promising PET-ligand in the diagnosis of AD.