摘要
The synthesis and biodistribution of β-amyloid plaques imaging agent [131I]-2- (4′-dimethylaminophenyl)- 6-iodoimidazo[1,2-α] pyridine ([131I]IMPY) were reported. The chemical structure of the labeling precursor 2-(4′-dimethylaminophenyl)-6-(tributylstannyl)imidazo[1,2-α] pyridine and all its intermediates were verified by IR,HNMR and MS. The radioiodinated compound was prepared using iododestannylation reaction by hydrogen per-oxide. Final radiochemical purity was above 95% determined by TLC. The in vivo biodistribution of [131I]IMPY in normal mice showed excellent brain uptake and washout, indicating this thioflavin-T based small molecular probe has potential for in vivo imaging amyloid deposits.
The synthesis and biodistribution of β-amyloid plaques imaging agent [^131I]-2- （4′-dimethylaminophenyl）-6-iodoimidazo[1,2-α] pyridine （[^131I]IMPY） were reported. The chemical structure of the labeling precursor 2-（4′-dimethylaminophenyl）-6- （tributylstannyl） imidazo[1, 2-α] pyridine and all its intermediates were verified by IR,HNMR and MS. The radioiodinated compound was prepared using iododestannylation reaction by hydrogen peroxide. Final radiochemical purity was above 95% determined by TLC. The in vivo biodistribution of [^131I]IMPY in normal mice showed excellent brain uptake and washout, indicating this thioflavin-T based small molecular probe has potential for in vivo imaging amyloid deposits.
基金
Jointly supported by a grant from National Natural Science Foundation (30470496), a grant from "135" Medicinal Momentous Pro-ject of Jiangsu Province (RC2002068), a grant from Department of Personnel of Jiangsu Province and a grant from Natural Science Foundation of Jiangsu Province (BK2004423).
