Display Settings:

Format

Send to:

Choose Destination
See comment in PubMed Commons below

6-(2-[18F]Fluoroethoxy)-2-[2-(4-methylaminophenyl)ethenyl]benzoxazole .

Authors

Cheng KT.

Source

Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2006 Oct 03 [updated 2008 Jan 28].

Excerpt

6-(2-[18F]Fluoroethoxy)-2-[2-(4-methylaminophenyl)ethenyl]benzoxazole ([18F]BF-168) is a radioligand that was developed for positron emission tomography (PET) imaging of amyloid-β (Aβ) plaques in the central nervous system (CNS) for detection of Alzheimer’s disease (AD) (1). 18F is a positron emitter with a physical t½ of 109.7 min. Aβ peptide was sequenced from the meningeal blood vessels of AD patients and individuals with Downs syndrome (2). Aβ peptides contain 40−42 amino acid residues and are metabolic products of Aβ precursor protein (APP) from cleavage by β and γ secretases (3). Aβ is also identified as the primary component of the neuritic plaques of AD patient brain tissue (4). Cloning of the gene that encodes the APP and its localization to chromosome 21 led to the hypothesis that Aβ accumulation is the primary event in AD pathogenesis (2, 5). This hypothesis proposes that neuronal death in AD is related to toxic effect of Aβ on the adjacent cell bodies or cell processes (6). AD is a progressive, neurogenerative disorder of the CNS that is characterized by a common set of clinical and pathological features (3). In addition to Aβ, the microtubule-associated protein tau (זּ) is also found in the cell body and axons of neurons as neurofibrillary tangles. The search for a cure or effective treatment of AD requires in vivo detection and quantification of Aβ in the brain for efficacy evaluation of AD therapy (3). Various amyloid-imaging probes have been developed based on PET, single-photon emission computed tomography, and optical imaging. These compounds generally have high binding affinity for amyloid fibrils and adequate permeability of the blood-brain barrier (1). There is evidence that suggests substantial deposition of diffuse plaques may be the initial pathological change in AD that precedes cognitive deterioration (7). Thus, imaging agents that can detect diffuse amyloid plaques may be useful for early detection of AD. Okamura et al. (1) synthesized a series of styrylbenzoxazole derivatives that target amyloid plaques, including diffuse plaques. They found that BF-168 recognized both neuritic and diffuse plaques in vivo. [18F]BF-168 appeared to be a promising candidate for PET imaging of AD.

PMID:
20641407
[PubMed]
Free Books & DocumentsFree full text
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons
    Write to the Help Desk