(R)-[18F]NEBIFQUINIDE: A promising new PET tracer for TSPO imaging

被引：15

作者：

Berroteran-Infante, Neydher ^{[1
,2
]}

Kalina, Thomas ^{[3
]}

Fetty, Lukas ^{[1
]}

Janisch, Victoria ^{[1
]}

Velasco, Ramona ^{[3
]}

Vraka, Chrysoula ^{[1
]}

Hacker, Marcus ^{[1
]}

Haug, Alexander R. ^{[1
]}

Pallitsch, Katharina ^{[3
]}

Wadsak, Wolfgang ^{[1
,2
,4
]}

Mitterhauser, Markus ^{[1
,5
]}

机构：

[1] Med Univ Vienna, Div Nucl Med, Dept Biomed Imaging & Image Guided Therapy, Wahringer Gurtel 18-20, A-1090 Vienna, Austria

[2] Univ Vienna, Fac Chem, Inst Inorgan Chem, Wahringer Str 42, A-1090 Vienna, Austria

[3] Univ Vienna, Fac Chem, Inst Organ Chem, Wahringer Str 38, A-1090 Vienna, Austria

[4] CBmed, Ctr Biomarker Res, Stiftingtalstr 5, A-8010 Graz, Austria

[5] Ludwig Boltzmann Inst Appl Diagnost, Wahringer Gurtel 18-20, A-1090 Vienna, Austria

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2019年 / 176卷

关键词：

Fluorine-18; Imaging agents; Preclinical evaluation; Radiopharmaceuticals; TSPO; 18-KDA TRANSLOCATOR PROTEIN; IN-VIVO; 18; KDA; BENZODIAZEPINE-RECEPTORS; AFFINITY BINDING; POLYMORPHISM; BRAIN; RADIOLIGAND; SENSITIVITY; LIGAND;

D O I：

10.1016/j.ejmech.2019.05.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Positron emission tomography (PET) imaging of the 18 kDa translocator protein (TSPO), has a high diagnostic potential in neurodegenerative disorders and cancer. However, TSPO is considered a challenge for molecular imaging due to the poor availability of suitable radiotracers with adequate pharmacokinetic properties. Here, we describe the development of a radiofluorinated pyridinyl isoquinoline analogue of the established TSPO PET tracer (R)-[C-11]PK11195 with improved binding properties in all known human TSPO phenotypes. We conducted a complete preclinical evaluation using in vitro, in vivo and ex vivo methods to assess the performance of this novel radiotracer and observed high specific binding of the radiotracer to TSPO, as well as high metabolic stability. Therefore, we propose this radiolabeled compound for further evaluation in animal models as well as in clinical trials. (C) 2019 Elsevier Masson SAS. All rights reserved.

引用

页码：410 / 418

页数：9

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