Abstract:
:To develop agents for radionuclide imaging Aβ plaques in vivo, we prepared three fluorine-substituted analogs of arylbenzothiazole class; compound 2 has a high affinity for Aβ (K(i)=5.5nM) and the specific binding to Aβ in fluorescent staining. In preparation for the synthesis of these arylbenzothiazole analogs in radiolabeled form as an Aβ plaques-specific positron emission tomography (PET) imaging probe, we investigated synthetic route suitable for its labeling with the short-lived PET radionuclide fluorine-18 (t(1/2)=110min) and diaryliodonium tosylate precursors (12, 13a-e and 14). 2-Aryl-6-[(18)F]fluorobenzothiazoles ([(18)F]1-3) were synthesized in efficiently short reaction times (40-60min) with high radiochemical yields (19-40%), purities (>95%) and specific activities (85-118GBq/μmol). Tissue distribution studies showed that high radioactivity of [(18)F]2 accumulated in the brain with rapid clearance in healthy mice. Radioactive metabolites were analyzed in brain samples of mice and corresponded to 81% of parent remained by 30min after a tail-vein injection. These results suggest that [(18)F]2 is a promising probe for evaluation of Aβ plaques imaging in brain using PET.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Lee BC,Kim JS,Kim BS,Son JY,Hong SK,Park HS,Moon BS,Jung JH,Jeong JM,Kim SEdoi
10.1016/j.bmc.2011.03.029subject
Has Abstractpub_date
2011-05-01 00:00:00pages
2980-90issue
9eissn
0968-0896issn
1464-3391pii
S0968-0896(11)00210-0journal_volume
19pub_type
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