Development and evaluation of compounds for imaging of β-amyloid plaque by means of positron emission tomography

被引：52

作者：

Henriksen, Gjermund ^{[1
]}

Yousefi, Behrooz H. ^{[1
]}

Drzezga, Alexander ^{[1
]}

Wester, Hans-Juergen ^{[1
]}

机构：

[1] Tech Univ Munich, Dept Nucl Med, Klinikum Rechts Isar, D-81675 Munich, Germany

来源：

EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING | 2008年 / 35卷 / Suppl 1期

关键词：

Alzheimer's disease; Amyloid plaque; Nuclear imaging; PET; SPECT;

D O I：

10.1007/s00259-007-0705-x

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

Purpose The proof of concept for in vivo targeting of beta-amyloid plaques (A beta) in patients with Alzheimer's disease (AD) by means of nuclear imaging methods has been shown in recent clinical studies. Methods For positron emission tomography (PET), the five compounds [C-11]PIB, 3'[F-18]FPIB, [F-18]FDDNP, [C-11]SB-13 and [F-18]F-SB-13 have been developed by a formal charge neutralisation of agents used for staining of AD brain post mortem. Results In AD-patients, these compounds have been shown to possess a selective uptake in the brain regions known to have a high A beta-load. Progress towards tracers with proportionality between tracer uptake and quantity of A beta-load, of use for longitudinal studies of AD patients, is addressed in the current development of A beta-tracers. Conclusion Despite the extensive information on the structure-affinity relationship of several A beta-binding compounds, data on the regional brain binding kinetics-beyond uptake in healthy rodents-have been obtained only for a few compounds. Recent results indicate that PET-imaging of A beta-deposits in transgenic rodent models of AD is feasible which may be valuable for a more relevant preclinical evaluation of A beta-tracers.

引用

页码：S75 / S81

页数：7

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