Auto-synthesis of fluoro-18-FDDNP on Alzheimer's research

Alzheimer's disease (AD) is an epidemic neurodegenerative disorder-affecting millions of elderly adults. Senile plaques (SPs) and neurofibrillay tangles (NFTs) are hallmarks in AD. [¹⁸F]FDDNP (2-(1-{ 6-[(2-fluoroethyl)(methyl)amino]-2-naphthyl} ethylidene)malononitrile) was superior binding with SPs and NFTs. High quality [¹⁸F]FDDNP was produced by an auto synthesizer. [¹⁸F]FDDNP has a partition coefficient of 1.93±0.10 mean was it shows hydrophobic ability to penetrate the blood brain barrier (BBB). In vitro autoradiography saturated with Tg2576, showed high retention ratio for Aβ rich regions (for example in Tg2576, hippocampus and frontal cortex were 2.10±0.34 and 1.90±0.17, respectively) and human brain section, postcentral gyrus, and occipital lobe showed significant different retention ratio (1.48±0.04 and 2.3±70.13, respectively). In ex vivo study, in hippocampus and frontal cortex region, Tg2576 had better retention than control mice. (2.40±0.33 and 2.19±0.22, respectively). In this paper, we show our modified protocol for the synthesis of [¹⁸F]FDDNP and report in vitro, in vivo and ex vivo results in transgenic mice as a model for applications in Aβ radiopharmaceutical research.