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2-(2-(2-(4-((4-(Methylamino)phenyl)ethynyl)phenoxy)ethoxy)[ 18 F]fluoroethoxy)ethyl-4-methylbenzenamine

2-(2-(2-(4-((4-(Methylamino)phenyl)ethynyl)phenoxy)ethoxy)[ 18 F]fluoroethoxy)ethyl-4-methylbenzenamine

Kam Leung

PMID: 21834180

Abstract:

Alzheimer's disease (AD) is a form of dementia with gradual memory loss and progressive decline in mental functions over time (1, 2). It is characterized pathologically by neuronal loss, extracellular senile plaques (aggregates of β-amyloid peptides consisting of 40-42 amino acids), and intracellular neurofibrillary tangles (filaments of microtubule-binding hyperphosphorylated protein tau) in the brain, especially in the hippocampus and associative regions of the cortex (3, 4). β-Amyloid peptides and tau protein are implicated as the main causes of neuronal degeneration and cell death (5, 6).
Early diagnosis of AD is important for treatment consideration and disease management (7). Various β-amyloid imaging agents have been developed for single-photon emission computed tomography and positron emission tomography (PET) (8-13). The binding performance of different derivatives of Congo red, thioflavin, stibene, and aminonaphthalene has been studied in human post-mortem brain tissue and in transgenic mice. Of these analogs, 2-(1-(6-[(2-[18F]fluoroethyl)(methyl)amino]-2-naphthyl)ethylidene)malono nitrile ([18F]FDDNP) was studied in humans and showed more binding in the brains of patients with AD than in those of healthy people (14). However, [18F]FDDNP showed low signal/noise ratios for PET imaging because it is highly lipophilic. N-methyl-[11C]-2-(4'-methylaminophenyl)-6-hydroxybenzothiasole, a β-amyloid binding compound based on a series of neutral thioflavin-T derivatives (15), was radiolabeled with the positron-emitting radionuclide 11C ([11C]6-OH-BTA-1, [11C]PIB). [11C]6-OH-BTA-1 was found to be a promising agent for the imaging of senile plaques in the brain (16). Zhang et al. (17) reported the development of a series of fluorinated polyethylene glycol units (n = 2-5) for PET imaging of β-amyloid plaques in the brain. 2-(2-(2-(4-((4-(Methylamino)phenyl)ethynyl)phenoxy)ethoxy)[18F]fluoroethoxy)ethyl-4-methylbenzenamine ([18F]AV-138) was validated as a PET imaging agent for β-amyloid plaques in the brain (18).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP439858283	BTA-1		439858-28-3	Price

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