(99m)Tc-labeled dibenzylideneacetone derivatives as potential SPECT probes for in vivo imaging of β-amyloid plaque

Yanping Yang; Mengchao Cui; Bing Jin; Xuedan Wang; Zijing Li; Pingrong Yu; Jianhua Jia; Hualong Fu; Hongmei Jia; Boli Liu

doi:10.1016/j.ejmech.2013.03.057

(99m)Tc-labeled dibenzylideneacetone derivatives as potential SPECT probes for in vivo imaging of β-amyloid plaque

Yanping Yang, Mengchao Cui, Bing Jin, Xuedan Wang, Zijing Li, Pingrong Yu, Jianhua Jia, Hualong Fu, Hongmei Jia, Boli Liu

Research output: Contribution to journal › Article › peer-review

Abstract

Four (99m)Tc-labeled dibenzylideneacetone derivatives and corresponding rhenium complexes were successfully synthesized and biologically evaluated as potential imaging probes for Aβ plaques using SPECT. All rhenium complexes (5a-d) showed affinity for Aβ(1-42) aggregates (Ki = 13.6-120.9 nM), and selectively stained the Aβ plaques on brain sections of transgenic mice. Biodistribution in normal mice revealed that [(99m)Tc]5a-d exhibited moderate initial uptake (0.31%-0.49% ID/g at 2 min) and reasonable brain washout at 60 min post-injection. Although additional optimizations are still needed to facilitate it's penetration through BBB, the present results indicate that [(99m)Tc]5a may be a potential SPECT probe for imaging Aβ plaques in Alzheimer's brains.

Original language	English (US)
Pages (from-to)	90-8
Number of pages	9
Journal	European Journal of Medicinal Chemistry
Volume	64
DOIs	https://doi.org/10.1016/j.ejmech.2013.03.057
State	Published - Jun 2013

Keywords

Amyloid beta-Peptides/chemistry
Animals
Butanones/chemistry
Disease Models, Animal
Fluorescent Dyes/chemical synthesis
Male
Mice
Mice, Inbred C57BL
Mice, Inbred ICR
Mice, Transgenic
Molecular Imaging
Molecular Structure
Organometallic Compounds/chemical synthesis
Peptide Fragments/chemistry
Plaque, Amyloid/chemistry
Rhenium/chemistry
Staining and Labeling
Technetium/chemistry
Tomography, Emission-Computed, Single-Photon

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10.1016/j.ejmech.2013.03.057

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@article{d240018bac6d4cc6b8ff8179eb5a226a,

title = "(99m)Tc-labeled dibenzylideneacetone derivatives as potential SPECT probes for in vivo imaging of β-amyloid plaque",

abstract = "Four (99m)Tc-labeled dibenzylideneacetone derivatives and corresponding rhenium complexes were successfully synthesized and biologically evaluated as potential imaging probes for Aβ plaques using SPECT. All rhenium complexes (5a-d) showed affinity for Aβ(1-42) aggregates (Ki = 13.6-120.9 nM), and selectively stained the Aβ plaques on brain sections of transgenic mice. Biodistribution in normal mice revealed that [(99m)Tc]5a-d exhibited moderate initial uptake (0.31%-0.49% ID/g at 2 min) and reasonable brain washout at 60 min post-injection. Although additional optimizations are still needed to facilitate it's penetration through BBB, the present results indicate that [(99m)Tc]5a may be a potential SPECT probe for imaging Aβ plaques in Alzheimer's brains.",

keywords = "Amyloid beta-Peptides/chemistry, Animals, Butanones/chemistry, Disease Models, Animal, Fluorescent Dyes/chemical synthesis, Male, Mice, Mice, Inbred C57BL, Mice, Inbred ICR, Mice, Transgenic, Molecular Imaging, Molecular Structure, Organometallic Compounds/chemical synthesis, Peptide Fragments/chemistry, Plaque, Amyloid/chemistry, Rhenium/chemistry, Staining and Labeling, Technetium/chemistry, Tomography, Emission-Computed, Single-Photon",

author = "Yanping Yang and Mengchao Cui and Bing Jin and Xuedan Wang and Zijing Li and Pingrong Yu and Jianhua Jia and Hualong Fu and Hongmei Jia and Boli Liu",

year = "2013",

month = jun,

doi = "10.1016/j.ejmech.2013.03.057",

language = "English (US)",

volume = "64",

pages = "90--8",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson SAS",

}

TY - JOUR

T1 - (99m)Tc-labeled dibenzylideneacetone derivatives as potential SPECT probes for in vivo imaging of β-amyloid plaque

AU - Yang, Yanping

AU - Cui, Mengchao

AU - Jin, Bing

AU - Wang, Xuedan

AU - Li, Zijing

AU - Yu, Pingrong

AU - Jia, Jianhua

AU - Fu, Hualong

AU - Jia, Hongmei

AU - Liu, Boli

PY - 2013/6

Y1 - 2013/6

N2 - Four (99m)Tc-labeled dibenzylideneacetone derivatives and corresponding rhenium complexes were successfully synthesized and biologically evaluated as potential imaging probes for Aβ plaques using SPECT. All rhenium complexes (5a-d) showed affinity for Aβ(1-42) aggregates (Ki = 13.6-120.9 nM), and selectively stained the Aβ plaques on brain sections of transgenic mice. Biodistribution in normal mice revealed that [(99m)Tc]5a-d exhibited moderate initial uptake (0.31%-0.49% ID/g at 2 min) and reasonable brain washout at 60 min post-injection. Although additional optimizations are still needed to facilitate it's penetration through BBB, the present results indicate that [(99m)Tc]5a may be a potential SPECT probe for imaging Aβ plaques in Alzheimer's brains.

AB - Four (99m)Tc-labeled dibenzylideneacetone derivatives and corresponding rhenium complexes were successfully synthesized and biologically evaluated as potential imaging probes for Aβ plaques using SPECT. All rhenium complexes (5a-d) showed affinity for Aβ(1-42) aggregates (Ki = 13.6-120.9 nM), and selectively stained the Aβ plaques on brain sections of transgenic mice. Biodistribution in normal mice revealed that [(99m)Tc]5a-d exhibited moderate initial uptake (0.31%-0.49% ID/g at 2 min) and reasonable brain washout at 60 min post-injection. Although additional optimizations are still needed to facilitate it's penetration through BBB, the present results indicate that [(99m)Tc]5a may be a potential SPECT probe for imaging Aβ plaques in Alzheimer's brains.

KW - Amyloid beta-Peptides/chemistry

KW - Animals

KW - Butanones/chemistry

KW - Disease Models, Animal

KW - Fluorescent Dyes/chemical synthesis

KW - Male

KW - Mice

KW - Mice, Inbred C57BL

KW - Mice, Inbred ICR

KW - Mice, Transgenic

KW - Molecular Imaging

KW - Molecular Structure

KW - Organometallic Compounds/chemical synthesis

KW - Peptide Fragments/chemistry

KW - Plaque, Amyloid/chemistry

KW - Rhenium/chemistry

KW - Staining and Labeling

KW - Technetium/chemistry

KW - Tomography, Emission-Computed, Single-Photon

U2 - 10.1016/j.ejmech.2013.03.057

DO - 10.1016/j.ejmech.2013.03.057

M3 - Article

C2 - 23644192

SN - 0223-5234

VL - 64

SP - 90

EP - 98

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

(99m)Tc-labeled dibenzylideneacetone derivatives as potential SPECT probes for in vivo imaging of β-amyloid plaque

Abstract

Keywords

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