Radioligand Development for PET Imaging of β-Amyloid (Aβ)-Current Status

Title: Radioligand Development for PET Imaging of β-Amyloid (Aβ)-Current Status

Volume: 14 Issue: 1

Author(s): Lisheng Cai, Robert B. Innis and Victor W. Pike

Affiliation:

Keywords: PET imaging, β-amyloid, radioligand, assay, Alzheimer's disease

Abstract: Two of the main pathological hallmarks of Alzheimers disease (AD) are neuritic plaques and neurofibrillary tangles. Significant evidence supports a critical and probable causative role of βamyloid (Aβ) plaque formation. Since neuroprotective treatments are typically most effective at early stages of injury, the detection and measurement of Aβ load in living brain should be performed at early and perhaps even presymptomatic stages of AD. Two primary targets of molecular imaging research with positron emission tomography (PET) are to develop surrogate markers (radioligands) for assessing disease progression and for monitoring the efficacy of developmental therapeutics. Here, we review the current status of radioligand development for PET imaging of Aβ aggregates. General structure-activity relationships have emerged, including the identification of at least three different ligand binding sites in various Aβ aggregates and recognition of the general structural requirements for ligand binding at each site. Also a few radioligands applicable to imaging Aβ plaques in living human brain with positron emission tomography (PET) have emerged, including [11C]PIB, [11C]SB- 13 and [18F]FDDNP.

Cite this article as:

Cai Lisheng, Innis B. Robert and Pike W. Victor, Radioligand Development for PET Imaging of β-Amyloid (Aβ)-Current Status, Current Medicinal Chemistry 2007; 14 (1) . https://dx.doi.org/10.2174/092986707779313471