Abstract：
:Amyloid-beta (Abeta) plaques are a pathological hallmark of Alzheimer's disease and a current target for positron emission tomography (PET) imaging agents. Whilst [(11)C]-PiB is currently the most widely used PET ligand in clinic, a novel family of benzoxazole compounds have shown promise as Abeta imaging agents; particularly BF227. We characterised the in vitro binding of [(18)F]-BF227 toward alpha-synuclein to address its selectivity for Abeta pathology, to establish whether [(18)F]-BF227 binds to alpha-synuclein/Lewy bodies, in addition to Abeta plaques. In vitro [(18)F]-BF227 saturation studies were conducted with 200 nM alpha-synuclein or Abeta(1-42) fibrils or 100 microg of Alzheimer's disease, pure dementia with Lewy bodies or control brain homogenates. Non-specific binding was established with PiB (1 microM). In vitro binding studies indicated that [(18)F]-BF227 binds with high affinity to two binding sites on Abeta(1-42) fibrils (K(D1) = 1.31 and K(D2) = 80 nM, respectively) and to one class of binding sites on alpha-synuclein fibrils (K(D) = 9.63 nM). [(18)F]-BF227 bound to Abeta-containing Alzheimer's disease brain (K(D) = 25 +/- 0.5 nM), but failed to bind to Abeta-free dementia with Lewy bodies or age-matched control homogenates. Moreover, BF227 labelled both Abeta plaques and Lewy bodies in immunohistochemical/fluorescence analysis of human Alzheimer's disease and Parkinson's disease brain sections, respectively. This study suggests that [(18)F]-BF227 is not Abeta-selective. Evaluation of BF227 as a potential biomarker for Parkinson's disease is warranted.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Fodero-Tavoletti MT,Mulligan RS,Okamura N,Furumoto S,Rowe CC,Kudo Y,Masters CL,Cappai R,Yanai K,Villemagne VLdoi
10.1016/j.ejphar.2009.06.042subject
Has Abstractpub_date
2009-09-01 00:00:00pages
54-8issue
1-3eissn
0014-2999issn
1879-0712pii
S0014-2999(09)00575-5journal_volume
617pub_type
杂志文章abstract：:The study concerned the effect of arachidonic acid metabolites on the inflammatory reaction in granulation tissue of open wounds in rats. Metabolites or inhibitors were applied in a wound chamber attached to circular, open, full-thickness skin wounds 5 days post-wounding. The adjacent wound served as control. Blood fl...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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abstract：:[3H]Spiroperidol binding was used to assay dopaminergic receptors in synaptosomal membranes isolated from basal ganglia of cat brain. In addition to the usual filtration, a special centrifugation technique was developed which has some advantages for ligands with high non-specific binding. The specific binding to contr...
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journal_title：European journal of pharmacology
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