Development and evaluation of [(18)F]Flotaza for Aβ plaque imaging in postmortem human Alzheimer's disease brain.
Development and evaluation of [(18)F]Flotaza for Aβ plaque imaging in postmortem human Alzheimer's disease brain.
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DOI：
10.1016/j.bmcl.2021.128164
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发表时间：
2021-08-15
影响因子：
2.7
通讯作者：
Mukherjee J
中科院分区：
文献类型：
--
作者：
Kaur H;Felix MR;Liang C;Mukherjee J
阿尔茨海默病 (AD) 中β淀粉样蛋白 (Aβ) 积累的正电子发射断层扫描 (PET) 研究已显示出临床实用性。本研究的目的是开发和评估新型氟 18 放射性示踪剂 [18F]Flotaza（2-{2-[2-[18F]氟乙氧基]乙氧基}乙氧基）-4'-N,N-二甲基氨基偶氮苯）用于 Aβ 斑块成像的有效性。亲核[18F]氟化物用于[18F]flotaza的一步放射合成。使用由前扣带回 (AC) 和胼胝体 (CC) 组成的死后人类 AD 脑组织，Flotaza 对人类 Aβ 斑块的结合亲和力 Ki = 1.68 nM，对 Tau 蛋白的结合亲和力较弱 (>10−5 M)。 [18F]Flotaza 的放射合成非常有效，放射化学产率高 (>25%)，比活性 >74 GBq/μmol。所有 AD 受试者的脑切片均采用抗 Aβ 免疫染色呈阳性。在所有 6 名受试者中，灰质 AC 与白质 CC 中的 [18F]Flotaza 比率均 >100。观察到很少的白质结合。 [18F]Flotaza 在 AC 中的结合与抗 Aβ 免疫染色密切相关。因此，[18F]Flotaza 是一种合适的氟 18 PET 放射性示踪剂，用于人类 Aβ 斑块的 PET 成像研究。
Positron emission tomographic (PET) studies of amyloid β (Aβ) accumulation in Alzheimer’s disease (AD) have shown clinical utility. The aim of this study was to develop and evaluate the effectiveness of a new fluorine-18 radiotracer [18F]Flotaza (2-{2-[2-[18F]fluoroethoxy]ethoxy}ethoxy)-4′-N,N-dimethylaminoazobenzene), for Aβ plaque imaging. Nucleophilic [18F]fluoride was used in a one-step radiosynthesis for [18F]flotaza. Using post mortem human AD brain tissues consisting of anterior cingulate (AC) and corpus callosum (CC), binding affinity of Flotaza, Ki = 1.68 nM for human Aβ plaques and weak (>10−5 M) for Tau protein. Radiosynthesis of [18F] Flotaza was very efficient in high radiochemical yields (>25%) with specific activities >74 GBq/μmol. Brain slices from all AD subjects were positively immunostained with anti-Aβ. Ratio of [18F]Flotaza in gray matter AC to white matter CC was >100 in all the 6 subjects. Very little white matter binding was seen. [18F]Flotaza binding in AC strongly correlated with anti-Aβ immunostains. [18F]Flotaza is therefore a suitable fluorine-18 PET radiotracer for PET imaging studies of human Aβ plaques.
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影响因子：
4.3
作者：
Mondal R;Campoy AT;Liang C;Mukherjee J
通讯作者：
Mukherjee J
影响因子：
2.3
作者：
Pan, Min-Liang;Mukherjee, Meenakshi T.;Mukherjee, Jogeshwar
通讯作者：
Mukherjee, Jogeshwar
影响因子：
3.1
作者：
Pichika, Rama;Easwaramoorthy, Balu;Mukherjee, Jogeshwar
通讯作者：
Mukherjee, Jogeshwar
DOI：
10.1056/nejmoa1304839
发表时间：
2014-01-23
期刊：
The New England journal of medicine
影响因子：
--
作者：
Salloway S;Sperling R;Fox NC;Blennow K;Klunk W;Raskind M;Sabbagh M;Honig LS;Porsteinsson AP;Ferris S;Reichert M;Ketter N;Nejadnik B;Guenzler V;Miloslavsky M;Wang D;Lu Y;Lull J;Tudor IC;Liu E;Grundman M;Yuen E;Black R;Brashear HR;Bapineuzumab 301 and 302 Clinical Trial Investigators
通讯作者：
Bapineuzumab 301 and 302 Clinical Trial Investigators
影响因子：
4.7
作者：
Stephenson, Karin A.;Chandra, Rajesh;Kung, Hank F.
通讯作者：
Kung, Hank F.