Nuclear Medicine and Biology 2013-07-01

Synthesis and evaluation of11C-labeled naphthalene derivative as a novel non-peptidergic probe for the β-secretase (BACE1) imaging in Alzheimer's disease brain

Tomoki Kawai, Hidekazu Kawashima, Yuji Kuge, Hideo Saji

Index: Nucl. Med. Biol. 40(5) , 705-9, (2013)

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Abstract

Introduction As a first trial for in vivo imaging of β-secretase (BACE1) in Alzheimer's disease brain, we applied a novel non-peptidergic small molecule which has high affinity to the enzyme, naphthalene-1-carboxylic acid (3′-chloro-4′-fluoro-4-piperazin-1-yl-biphenyl-3-yl)amide (NCFB) into positron emission tomography (PET) probe. In the current study, N-11C-methylated compound of NCFB, [11C]Me-NCFB was synthesized and evaluated for the visualization of BACE1 in brain.