Synthesis and biodistribution of novel dansyl derivative 11C-DSB

Abstract

A novel 11C-labeled dansyl 1, 2-diphenylethene derivative for positron emission tomography (PET) imaging of β-amyloid (Aβ) plaques and apoptosis in the brain of Alzheimer’s disease (AD) was designed and synthesized. The 11C-labeled tracer, (E)-5-(dimethylamino)-N-(4-(4-11C-methoxystyryl)phenyl)-naphthalene-1-sulfonamide (11C-DSB), was synthesized. The decay-corrected radiochemistry yield was 20 ± 5% (n = 5) from 11C–CO2 within 20 min and the specific activity of 1.6 GBq/µmol. Moreover, in vivo biodistribution and preliminary PET imaging of normal mice were performed to show that 11C-DSB had moderate brain penetration and washout. But11C-DSB has high log P value, showing that its structure needs to be further improved to increase its water solubility. The results provide the basis for further research on PET and fluorescence dual-modality imaging of AD models.