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SPECT Imaging Agents for Detecting Cerebral β-Amyloid Plaques.

Ono M, Saji H - Int J Mol Imaging (2011)

Bottom Line: The development of radiotracers for use in vivo to image β-amyloid (Aβ) plaques in cases of Alzheimer's disease (AD) is an important, active area of research.The presence of Aβ aggregates in the brain is generally accepted as a hallmark of AD.This paper reviews the current situation in the development of agents for SPECT-based imaging of Aβ plaques in Alzheimer's brains.

View Article: PubMed Central - PubMed

Affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.

ABSTRACT
The development of radiotracers for use in vivo to image β-amyloid (Aβ) plaques in cases of Alzheimer's disease (AD) is an important, active area of research. The presence of Aβ aggregates in the brain is generally accepted as a hallmark of AD. Since the only definitive diagnosis of AD is by postmortem staining of affected brain tissue, the development of techniques which enable one to image Aβ plaques in vivo has been strongly desired. Furthermore, the quantitative evaluation of Aβ plaques in the brain could facilitate evaluation of the efficacy of antiamyloid therapies currently under development. This paper reviews the current situation in the development of agents for SPECT-based imaging of Aβ plaques in Alzheimer's brains.

No MeSH data available.


Related in: MedlinePlus

Chemical structure of SPECT imaging agents derived from Congo Red.
© Copyright Policy - open-access
Related In: Results  -  Collection


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fig3: Chemical structure of SPECT imaging agents derived from Congo Red.

Mentions: Many radioiodinated imaging agents derived from Congo Red or thioflavin-T have been developed. Compounds 1 [29], 2 [29], 3 [40], 4 [23], 5 [24], and 6 [25] (Figure 3) are thought to be derived from Congo Red. Although 1, 2, and 3 showed unfavorable pharmacokinetics in vivo such as low uptake into the brain and a slow washout, the radioactivity pharmacokinetics of 5 and 6 was much improved. Because thioflavin-T has a lower molecular weight than Congo Red, implying greater blood-brain penetration, a number of groups have worked to develop probes for SPECT derived from thioflavin-T including 7 (IMPY) [26–28], 8 (TZDM) [29], 9 (IBOX) [30], 10 (benzofuran derivatives) [31], and 11 (phenylindole derivatives) (Figure 4) [32].


SPECT Imaging Agents for Detecting Cerebral β-Amyloid Plaques.

Ono M, Saji H - Int J Mol Imaging (2011)

Chemical structure of SPECT imaging agents derived from Congo Red.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3094870&req=5

fig3: Chemical structure of SPECT imaging agents derived from Congo Red.
Mentions: Many radioiodinated imaging agents derived from Congo Red or thioflavin-T have been developed. Compounds 1 [29], 2 [29], 3 [40], 4 [23], 5 [24], and 6 [25] (Figure 3) are thought to be derived from Congo Red. Although 1, 2, and 3 showed unfavorable pharmacokinetics in vivo such as low uptake into the brain and a slow washout, the radioactivity pharmacokinetics of 5 and 6 was much improved. Because thioflavin-T has a lower molecular weight than Congo Red, implying greater blood-brain penetration, a number of groups have worked to develop probes for SPECT derived from thioflavin-T including 7 (IMPY) [26–28], 8 (TZDM) [29], 9 (IBOX) [30], 10 (benzofuran derivatives) [31], and 11 (phenylindole derivatives) (Figure 4) [32].

Bottom Line: The development of radiotracers for use in vivo to image β-amyloid (Aβ) plaques in cases of Alzheimer's disease (AD) is an important, active area of research.The presence of Aβ aggregates in the brain is generally accepted as a hallmark of AD.This paper reviews the current situation in the development of agents for SPECT-based imaging of Aβ plaques in Alzheimer's brains.

View Article: PubMed Central - PubMed

Affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.

ABSTRACT
The development of radiotracers for use in vivo to image β-amyloid (Aβ) plaques in cases of Alzheimer's disease (AD) is an important, active area of research. The presence of Aβ aggregates in the brain is generally accepted as a hallmark of AD. Since the only definitive diagnosis of AD is by postmortem staining of affected brain tissue, the development of techniques which enable one to image Aβ plaques in vivo has been strongly desired. Furthermore, the quantitative evaluation of Aβ plaques in the brain could facilitate evaluation of the efficacy of antiamyloid therapies currently under development. This paper reviews the current situation in the development of agents for SPECT-based imaging of Aβ plaques in Alzheimer's brains.

No MeSH data available.


Related in: MedlinePlus