Development of dual functional SPECT/fluorescent probes for imaging cerebral β-amyloid plaques

Ono, Masahiro; Ishikawa, Manami; Kimura, Hiroyuki; Hayashi, Shun; Matsumura, Kenji; Watanabe, Hiroyuki; Shimizu, Yoichi; Cheng, Yan; Cui, Mengchao; Kawashima, Hidekazu; Saji, Hideo

doi:10.1016/j.bmcl.2010.05.027

Cited by 59 publications

(35 citation statements)

References 25 publications

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“…The high quantum yield, biocompatibility, and high lipophilicity of the BODIPY fluorophore render it attractive for the design of NIRF probes. In this regard, inspired by NIAD-4, Ono and his team 57 reported their first BODIPY-derived fluorescence/SPECT dual probe BODIPY7. It contains a conjugated thiophene-phenyl chain similar to NIAD-4.…”

Section: Nirf a β Probesmentioning

confidence: 99%

Near-infrared fluorescent probes for imaging of amyloid plaques in Alzheimer׳s disease

Tong

Lou

Wang

2015

Acta Pharmaceutica Sinica B

115

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One of the early pathological hallmarks of Alzheimer׳s disease (AD) is the deposition of amyloid-β (Aβ) plaques in the brain. There has been a tremendous interest in the development of Aβ plaques imaging probes for early diagnosis of AD in the past decades. Optical imaging, particularly near-infrared fluorescence (NIRF) imaging, has emerged as a safe, low cost, real-time, and widely available technique, providing an attractive approach for in vivo detection of Aβ plaques among many different imaging techniques. In this review, we provide a brief overview of the state-of-the-art development of NIRF Aβ probes and their in vitro and in vivo applications with special focus on design strategies and optical, binding, and brain-kinetic properties.

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Section: Nirf a β Probesmentioning

confidence: 99%

Near-infrared fluorescent probes for imaging of amyloid plaques in Alzheimer׳s disease

Tong

Lou

Wang

2015

Acta Pharmaceutica Sinica B

115

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“…We have previously reported a dual SPECT/fluorescent probe based on the BODIPY scaffold, for the imaging of Aβ plaques in vivo. 41 Despite good affinity for synthetic Aβ(1−42) aggregates and the clear labeling of Aβ plaques in sections of the mouse brain, the BODIPY-based probe was not suitable for imaging in vivo due to its poor uptake into the brain. Two other papers have reported BODIPY-based probes targeting Aβ plaques.…”

mentioning

confidence: 99%

BODIPY-Based Molecular Probe for Imaging of Cerebral β-Amyloid Plaques

Ono

Watanabe

Kimura

et al. 2012

ACS Chem. Neurosci.

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140

115

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We designed and synthesized a BODIPY-based probe (BAP-1) for the imaging of β-amyloid plaques in the brain. In binding experiments in vitro, BAP-1 showed excellent affinity for synthetic Aβ aggregates. β-Amyloid plaques in Tg2576 mouse brain were clearly visualized with BAP-1. In addition, the labeling of β-amyloid plaques was demonstrated in vivo in Tg2576 mice. These results suggest BAP-1 to be a useful fluorescent probe for the optical imaging of cerebral β-amyloid plaques in patients with Alzheimer's disease.

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“…The boron [ 125 I]-labeled dipyrro-methane (BODIPY) analogue 175 was prepared to serve as a dual functional SPECT/fluorescence probe for imaging Aβ (Scheme 14) [112]. Compound 175 was synthesized through Suzuki coupling of the starting boronic acid 176 with 1-bromo-4-iodobenzene ( 171 ).…”

Section: Reviewmentioning

confidence: 99%

Amyloid-β probes: Review of structure–activity and brain-kinetics relationships

Eckroat¹,

Mayhoub²

2013

Beilstein J. Org. Chem.

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SummaryThe number of people suffering from Alzheimer’s disease (AD) is expected to increase dramatically in the coming years, placing a huge burden on society. Current treatments for AD leave much to be desired, and numerous research efforts around the globe are focused on developing improved therapeutics. In addition, current diagnostic tools for AD rely largely on subjective cognitive assessment rather than on identification of pathophysiological changes associated with disease onset and progression. These facts have led to numerous efforts to develop chemical probes to detect pathophysiological hallmarks of AD, such as amyloid-β plaques, for diagnosis and monitoring of therapeutic efficacy. This review provides a survey of chemical probes developed to date for AD with emphasis on synthetic methodologies and structure–activity relationships with regards to affinity for target and brain kinetics. Several probes discussed herein show particularly promising results and will be of immense value moving forward in the fight against AD.

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Development of dual functional SPECT/fluorescent probes for imaging cerebral β-amyloid plaques

Cited by 59 publications

References 25 publications

Near-infrared fluorescent probes for imaging of amyloid plaques in Alzheimer׳s disease

Near-infrared fluorescent probes for imaging of amyloid plaques in Alzheimer׳s disease

BODIPY-Based Molecular Probe for Imaging of Cerebral β-Amyloid Plaques

Amyloid-β probes: Review of structure–activity and brain-kinetics relationships

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