Synthesis and Evaluation of 13N-Labelled Azo Compounds for β-Amyloid Imaging in Mice
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- 作者：Vijay Gaja (1)
Vanessa Gómez-Vallejo (1)
Maria Puigivila (1)
Carlos Pérez-Campa?a (1)
Abraham Martin (2)
Ana García-Osta (3)
Teresa Calvo-Fernández (4)
Mar Cuadrado-Tejedor (3)
Rafael Franco (3) (5)
Jordi Llop (1) - 关键词：Positron emission tomography ; Tg2576 ; Alzheimer's disease ; Nitrogen ; 13 ; β ; Amyloid ; Animal biomarker
- 刊名：Molecular Imaging and Biology
- 出版年：2014
- 出版时间：August 2014
- 年：2014
- 卷：16
- 期：4
- 页码：538-549
- 全文大小：4,534 KB
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Vanessa Gómez-Vallejo (1)
Maria Puigivila (1)
Carlos Pérez-Campa?a (1)
Abraham Martin (2)
Ana García-Osta (3)
Teresa Calvo-Fernández (4)
Mar Cuadrado-Tejedor (3)
Rafael Franco (3) (5)
Jordi Llop (1)
1. Radiochemistry Department, Molecular Imaging Unit, CIC biomaGUNE, San Sebastian, Spain
2. Molecular Imaging Unit, CIC biomaGUNE, San Sebastian, Spain
3. Division of Neuroscience, CIMA, University of Navarra, Pamplona, Spain
4. Animal Facility, Molecular Imaging Unit, CIC biomaGUNE, San Sebastian, Spain
5. Department of Biochemistry and Molecular Biology, University of Barcelona, Barcelona, Spain - ISSN：1860-2002
文摘
Purpose The aim of the present study was to develop short half-lived tools for in vitro and in vivo β-amyloid imaging in mice, for which no suitable PET tracers are available. Procedures Five 13N-labelled azo compounds (1-strong class="a-plus-plus">5) were synthesized using a three-step process using cyclotron-produced [13N]NO3 ?/sup>. Biodistribution studies were performed using positron emission tomography–computed tomography (PET–CT) on 20-month-old healthy, wild-type (WT) mice. In vivo and in vitro binding assays were performed using PET-CT and autoradiography, respectively, on 20-month-old healthy (WT) mice and transgenic (Tg2576) Alzheimer's disease model mice. Results 13N-labelled azo compounds were prepared with decay corrected radiochemical yields in the range 27?±- % to 39?±- %. Biodistribution studies showed good blood–brain barrier penetration for compounds 1 and 3-; good clearance data were also obtained for compounds 1- and 5. Compounds 2, 3 and 5 (but not 1) showed a significant uptake in β-amyloid-rich structures when assayed in in vitro autoradiographic studies. PET studies showed significant uptake of compounds 2 and 3 in the cortex of transgenic animals that exhibit β-amyloid deposits. Conclusions The results underscore the potential of compounds 2 and 3 as in vitro and in vivo markers for β-amyloid in animal models of Alzheimer's disease.