[18F]DPA-714, [18F]PBR111 and [18F]FEDAA1106-Selective radioligands for imaging TSPO 18 kDa with PET: Automated radiosynthesis on a TRACERLAb FX-FN synthesizer and quality controls

被引：57

作者：

Kuhnast, Bertrand ^{[1
]}

Damont, Annelaure ^{[1
]}

Hinnen, Francoise ^{[1
]}

Catarina, Tony ^{[1
]}

Demphel, Stephane ^{[1
]}

Le Helleix, Stephane ^{[1
]}

Coulon, Christine ^{[1
]}

Goutal, Sebastien ^{[1
]}

Gervais, Philippe ^{[1
]}

Dolle, Frederic ^{[1
]}

机构：

[1] CEA, Serv Hosp Frederic Joliot, I2BM, F-91401 Orsay, France

来源：

APPLIED RADIATION AND ISOTOPES | 2012年 / 70卷 / 03期

关键词：

Fluorine-18; TRACERlab FX-FN; TSPO; 18; kDa; F-18]DPA-714; F-18]FEDAA1106; F-18]PBR111; PERIPHERAL BENZODIAZEPINE-RECEPTOR; SELECTIVE RADIOLIGAND; LIGAND; PBR;

D O I：

10.1016/j.apradiso.2011.10.015

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Imaging of TSPO 18 kDa with PET is more and more considered as a relevant biomarker of inflammation in numerous diseases. Development of new radiotracers for TSPO 18 kDa has seen acceleration in the last years and the challenge today is to make available large amounts of such a radiotracer in compliance with GMP standards for application in humans. We present in this technical note automated productions of [F-18]DPA-714, [F-18]PBR111 and [F-18]FEDAA1106, three promising radiotracers for Tspo 18 kDa imaging, using a TRACERlab FX-FN synthesizer. This note also includes the quality control data of the validation batches for the manufacturing qualification of clinical production of [F-18]DPA-714. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：489 / 497

页数：9

共 21 条

[1] Positron emission tomography imaging of neuroinflammation [J].

Cagnin, Annachiara ;

Kassiou, Michael ;

Meikle, Steve R. ;

Banati, Richard B. .

NEUROTHERAPEUTICS, 2007, 4 (03) :443-452

[2] SYNTHESIS OF N-(C-11) METHYL, N-(METHYL-1 PROPYL), (CHLORO-2 PHENYL)-1 ISOQUINOLEINE CARBOXAMIDE-3 (PK-11195) - A NEW LIGAND FOR PERIPHERAL BENZODIAZEPINE RECEPTORS [J].

CAMSONNE, R ;

CROUZEL, C ;

COMAR, D ;

MAZIERE, M ;

PRENANT, C ;

SASTRE, J ;

MOULIN, MA ;

SYROTA, A .

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1984, 21 (10) :985-991

[3] Translocator protein 18 kDa (TSPO): Molecular sensor of brain injury and repair [J].

Chen, Ming-Kai ;

Guilarte, Tomas R. .

PHARMACOLOGY & THERAPEUTICS, 2008, 118 (01) :1-17

[4] Radiosynthesis of [18F]DPA-714, a selective radioligand for imaging the translocator protein (18 kDa) with PET [J].

Damont, Annelaure ;

Hinnen, Francoise ;

Kuhnast, Bertrand ;

Schollhorn-Peyronneau, Marie-Anne ;

James, Michelle ;

Luus, Christopher ;

Tavitian, Bertrand ;

Kassiou, Michael ;

Dolle, Frederic .

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2008, 51 (7-8) :286-292

[5] Peripheral benzodiazepine receptor and its clinical targeting [J].

Decaudin, D .

ANTI-CANCER DRUGS, 2004, 15 (08) :737-745

[6] Radiolabelled Molecules for Imaging the Translocator Protein (18 kDa) Using Positron Emission Tomography [J].

Dolle, Frederic ;

Luus, Christopher ;

Reynolds, Aaron ;

Kassiou, Michael .

CURRENT MEDICINAL CHEMISTRY, 2009, 16 (22) :2899-2923

[7] Radiosynthesis of [18F]PBR111, a selective radioligand for imaging the translocator protein (18 kDa) with PET [J].

Dolle, Frederic ;

Hinnen, Francoise ;

Damont, Annelaure ;

Kuhnast, Bertrand ;

Fookes, Christopher ;

Pham, Tien ;

Tavitian, Bertrand ;

Katsifis, Andrew .

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2008, 51 (13-14) :435-439

[8] Synthesis and biological evaluation of substituted [18F]imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography [J].

Fookes, Christopher J. R. ;

Pham, Tien Q. ;

Mattner, Filomena ;

Greguric, Ivan ;

Loc'h, Christian ;

Liu, Xiang ;

Berghofer, Paula ;

Shepherd, Rachael ;

Gregoire, Marie-Claude ;

Katsifis, Andrew .

JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (13) :3700-3712

[9] The peripheral benzodiazepine receptor: A promising therapeutic drug target [J].

Galiegue, S ;

Tinel, N ;

Casellas, P .

CURRENT MEDICINAL CHEMISTRY, 2003, 10 (16) :1563-1572

[10] DPA-714, a new translocator protein-specific ligand: Synthesis, radiofluorination, and pharmacologic characterization [J].

James, Michelle L. ;

Fulton, Roger R. ;

Vercoullie, Johnny ;

Henderson, David J. ;

Garreau, Lucette ;

Chalon, Sylvie ;

Dolle, Frederic ;

Costa, Barbara ;

Guilloteau, Denis ;

Kassiou, Michael .

JOURNAL OF NUCLEAR MEDICINE, 2008, 49 (05) :814-822

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