A Facile Radiolabeling of [ 18 F]FDPA via Spirocyclic Iodonium Ylides: Preliminary PET Imaging Studies in Preclinical Models of Neuroinflammation.

Autor: Wang L; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Harvard Medical School , Boston, Massachusetts 02114, United States., Cheng R; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Harvard Medical School , Boston, Massachusetts 02114, United States.; School of Pharmaceutical Science and Technology, Tianjin University , 92 Weijin Road, Nankai District, Tianjin, China., Fujinaga M; Department of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555, Japan., Yang J; Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital & Harvard Medical School , Boston, Massachusetts 02129, United States., Zhang Y; Department of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555, Japan., Hatori A; Department of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555, Japan., Kumata K; Department of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555, Japan., Yang J; Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital & Harvard Medical School , Boston, Massachusetts 02129, United States., Vasdev N; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Harvard Medical School , Boston, Massachusetts 02114, United States., Du Y; School of Pharmaceutical Science and Technology, Tianjin University , 92 Weijin Road, Nankai District, Tianjin, China., Ran C; Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital & Harvard Medical School , Boston, Massachusetts 02129, United States., Zhang MR; Department of Radiopharmaceutics Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555, Japan., Liang SH; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Harvard Medical School , Boston, Massachusetts 02114, United States.
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2017 Jun 22; Vol. 60 (12), pp. 5222-5227. Date of Electronic Publication: 2017 Jun 05.
DOI: 10.1021/acs.jmedchem.7b00432
Abstrakt: A suitable TSPO PET ligand may visualize and quantify neuroinflammation in a living brain. Herein we report a 18 F-ligand, [ 18 F]2 ([ 18 F]FDPA), is radiolabeled in high yield and high specific activity based on our spirocyclic iodonium ylide (SCIDY) strategy. [ 18 F]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).
Databáze: MEDLINE