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A Facile Radiolabeling of [18F]FDPA via Spirocyclic Iodonium Ylides: Preliminary PET Imaging Studies in Preclinical Models of Neuroinflammation
- Source :
- Journal of Medicinal Chemistry. 60(12):5222-5227
- Publication Year :
- 2017
- Publisher :
- ELSEVIER, 2017.
-
Abstract
- A suitable TSPO PET ligand may visualize and quantify neuroinflammation in a living brain. Herein we report a 18F-ligand, [18F]2 ([18F]FDPA), is radiolabeled in high yield and high specific activity based on our spirocyclic iodonium ylide (SCIDY) strategy. [18F]2 demonstrated saturable specific binding to TSPO, substantially elevated brain uptake, and slow washout of bound PET signal in the preclinical models of brain neuroinflammation (cerebral ischemia and Alzheimer's disease).
Details
- Language :
- English
- ISSN :
- 00222623
- Volume :
- 60
- Issue :
- 12
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.jairo.........c0f4915c6ce37fe85e51e025e37a27b5