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Synthesis and biodistribution of [~(131)I]IMPY

Lu Chun

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Abstract

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.

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What this paper is about

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.

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Available abstract

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.

Key concepts: Biodistribution, Chemistry, In vivo, Thioflavin, Radiochemistry, Imaging agent, Chemical synthesis, Preclinical imaging

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