Transgenic mice brain imaging studies of Alzheimer's disease

Lipophilicity is one of the major brain radiopharmaceutical design criteria. Alzheimer disease PET imaging agents based on lipophilicity modification are [18F]RO6958948 [1] and [18F] Florbetapir, design by replacing with a Nitrogen element either in the aromatic ring of [18F]Flortaucipir or [18F]Florbetaben. The structure of [18F]FEONM is designed to provide higher lipophilicity than [18F]FDDNP. Structure modification on a certain bioactive molecule in order to increase its lipophilicity will be also possibly increasing the percentage of penetrating blood brain barrier. Increasing the blood brain barrier crossing ratio, the specificity of this active biomolecule targeting effect might be decreased. Therefore, we design an ethyl oxide modified naphthol based Alzheimer disease positron emission tomography imaging agent [18F]FEONM, in order to compare the uptake effect of Tau tangle and Beta amyloid. PET radiopharmaceiticals for brain imaging are based on very short half-life radionuclides, most of them will be decayed in one day. One of the longest half-life organic radionuclides is fluorine-18, therefore critical step to producing PET radiopharmaceuticals online is radiofluorination reaction. The highest radiofluorination reaction yield can be made from carboxy glass reactor [2]. In carboxy glass reactor, the function of gap area (FG) [3] curve of radiofluorination yield can be approached with Gauss distribution, Gauss or Welch apodization function. After determine the radiofluorination rate constant, the length of microfluidic plug flow reactor can be designed.

Author(s): Chen Jenn-Tzong

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