A dual fluorinated and iodinated radiotracer for PET and SPECT imaging of β-amyloid plaques in the brain

…, T Fuchigami, M Haratake, M Nakayama, H Saji

Index: Watanabe, Hiroyuki; Ono, Masahiro; Kimura, Hiroyuki; Kagawa, Shinya; Nishii, Ryuichi; Fuchigami, Takeshi; Haratake, Mamoru; Nakayama, Morio; Saji, Hideo Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 21 p. 6519 - 6522

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Citation Number: 20

Abstract

We report a fluorinated and iodinated radiotracer as a probe for PET/SPECT to detect of β- amyloid (Aβ) plaques in the brain of patients with Alzheimer's disease (AD). We successfully designed and synthesized the fluorinated and iodinated aurone derivative (3) and its radiolabels ([125I] 3 and [18F] 3). In binding experiments in vitro, 3 showed high affinity for Aβ aggregates (Ki= 6.81 nM). In brain sections of AD model mice, 3 intensely stained Aβ ...