Fluorine-18 labeling of three novel D-peptides by conjugation with N-succinimidyl-4-[F-18]fluorobenzoate and preliminary examination by postmortem whole-hemisphere human brain autoradiography

Introduction: beta-Amyloid (A beta) plaques and neurofibrillary tangles are the main characteristics of Alzheimer's disease (AD). Positron emission tomography (PET), a high-resolution, sensitive, and noninvasive imaging technique, has been widely utilized in visualizing the localization of plaques and tangles and thereby distinguishing between AD and healthy controls. A small 12-mer D-enantiomeric peptide (amino acid sequence=QSHYRHISPAQV), denoted as D1, has high binding affinity to A beta in vitro in the sub-micromolar range, and consequently, its radiolabeled analogues have a potential as radioligands for visualizing amyloid plaques in vivo by PET.