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Synthesis and evaluation of a radioiodinated benzothiazole derivative as a radioligand for in vivo quantitation of β‐amyloid deposits in aging and alzheimer's disease
Author(s) -
Wang Y.,
Klunk W. E.,
Huang G.F.,
Debnath M. L.,
Holt D. P.,
Mathis C. A.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580440183
Subject(s) - radioligand , chemistry , in vivo , senile plaques , amyloid (mycology) , alzheimer's disease , benzothiazole , blood–brain barrier , biomarker , monoclonal antibody , pathology , biochemistry , in vitro , antibody , neuroscience , disease , immunology , medicine , central nervous system , biology , inorganic chemistry , microbiology and biotechnology
Amyloid deposits in the form of senile plaques and fibrillary tangles have been targeted as a biomarker for the early diagnosis of Alzheimer's disease (AD) and evaluation of the efficacy of therapeutic treatments (1–3). For in vivo quantitation of amyloid deposits in AD, efforts have been made to develop radiopharmaceuticals for PET and/or SPECT imaging that readily penetrate the blood brain barrier and selectively localize in the area of beta‐amyloid deposits in AD brain. To date, these agents such as radiolabeled monoclonal antibodies (4), plaque‐related proteins (5, 6), analogues of Congo red (7–11), and membrane dyes (12) have found limited use due to either marginal brain uptake or high non‐specific binding.