期刊
MOLECULAR IMAGING AND BIOLOGY
卷 18, 期 3, 页码 334-343出版社
SPRINGER
DOI: 10.1007/s11307-015-0906-9
关键词
Gallium-68; PIB; Automated radiosynthesis; PET; Alzheimer's disease; Cerebral amyloidopathies; Radiometabolism; Autoradiography
资金
- French National Agency for Research
- LABEX IRON (Innovative Radiopharmaceuticals in Oncology and Neurology) [ANR-11-LABX-0018-01]
- Commissariat a l'Energie Atomique et aux Energies Alternatives (CEA)
- region Basse Normandie
- Centre National de la Recherche Scientifique (CNRS)
- Fundacao para a Ciencia e Tecnologia, Portugal [SFRH/BD/46370/2008]
- French-Portuguese PESSOA project
- Fundação para a Ciência e a Tecnologia [SFRH/BD/46370/2008] Funding Source: FCT
The aim of this work is to develop an efficient and fully automated radiosynthesis of three derivatives of the Pittsburgh compound B labeled with gallium-68 for the detection of amyloid plaques. The radiolabeling of the precursors and purification of the radiolabeled agents by high pressure liquid chromatography has been studied prior to their in vitro and in vivo evaluations. The complete process led, in 50 min, to pure Ga-68 products in a 12-38 % yield and with appreciable specific radioactivity (SRA, 85-168 GBq/mu mol) which enabled us to demonstrate a considerable in vivo stability of the products. Unfortunately, this result was associated with a poor blood-brain barrier (BBB) permeability and a limited uptake of our compounds by amyloid deposits was observed by in vitro autoradiography. Although we have not yet identified a compound able to significantly mark cerebral amyloidosis, this present investigation will likely contribute to the development of more successful Ga-68 radiotracers.
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