[18F]GE-180: A novel fluorine-18 labelled PET tracer for imaging Translocator protein 18 kDa (TSPO)

被引：99
|
作者：
Wadsworth, Harry [1 ]
Jones, Paul A. [1 ]
Chau, Wai-Fung [1 ]
Durrant, Clare [1 ]
Fouladi, Naghmeh [1 ]
Passmore, Joanna [1 ]
O'Shea, Dennis [1 ]
Wynn, Duncan [1 ]
Morisson-Iveson, Veronique [1 ]
Ewan, Amanda [1 ]
Thaning, Mikkel [2 ]
Mantzilas, Dimitrios [2 ]
Gausemel, Ingvil [2 ]
Khan, Imtiaz [1 ]
Black, Andrew [1 ]
Avory, Michelle [1 ]
Trigg, William [1 ]
机构：
[1] GE Healthcare, Grove Ctr, Amersham HP9 7LL, Bucks, England
[2] GE Healthcare AS, N-0401 Oslo, Norway
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 03期
关键词：
TSPO; PBR; PET; Neuroinflammation; Radiosynthesis; PERIPHERAL BENZODIAZEPINE-RECEPTORS; LIGANDS; BRAIN; CHROMATOGRAPHY; BINDING;
D O I：
10.1016/j.bmcl.2011.12.084
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of tricyclic compounds have been synthesised and evaluated in vitro for affinity against Translocator protein 18 kDa (TSPO) and for preferred imaging properties. The most promising of the compounds were radiolabelled and evaluated in vivo to determine biodistribution and specificity for high expressing TSPO regions. Metabolite profiling in brain and plasma was also investigated. Evaluation in an autoradiography model of neuroinflammation was also carried out for the best compound, 12a ([F-18]GE-180). (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1308 / 1313
页数：6
相关论文
共 50 条
  • [41] (R)-[18F]NEBIFQUINIDE: A promising new PET tracer for TSPO imaging
    Berroteran-Infante, Neydher
    Kalina, Thomas
    Fetty, Lukas
    Janisch, Victoria
    Velasco, Ramona
    Vraka, Chrysoula
    Hacker, Marcus
    Haug, Alexander R.
    Pallitsch, Katharina
    Wadsak, Wolfgang
    Mitterhauser, Markus
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019, 176 : 410 - 418
  • [42] An improved, regioselective synthesis of the radiolabelling precursor for the translocator protein targeting positron emission tomography imaging radiotracer [18F]GE-180
    Morisson-Iveson, Veronique
    Wadsworth, Harry
    Passmore, Joanna
    Ewan, Amanda
    Nilsen, Sondre
    Thaning, Mikkel
    Trigg, William
    [J]. TETRAHEDRON LETTERS, 2014, 55 (37) : 5141 - 5143
  • [43] Longitudinal [18F]GE-180 PET Imaging Facilitates In Vivo Monitoring of TSPO Expression in the GL261 Glioblastoma Mouse Model
    Holzgreve, Adrien
    Potter, Dennis
    Brendel, Matthias
    Orth, Michael
    Weidner, Lorraine
    Gold, Lukas
    Kirchner, Maximilian A.
    Bartos, Laura M.
    Unterrainer, Lena M.
    Unterrainer, Marcus
    Steiger, Katja
    von Baumgarten, Louisa
    Niyazi, Maximilian
    Belka, Claus
    Bartenstein, Peter
    Riemenschneider, Markus J.
    Lauber, Kirsten
    Albert, Nathalie L.
    [J]. BIOMEDICINES, 2022, 10 (04)
  • [44] Quantification of the new TSPO ligand [18F]GE-180 in patients with multiple sclerosis - initial results
    Vomacka, Lena
    Albert, Nathalie
    Lindner, Simon
    Unterrainer, Marcus
    Mahler, Christoph
    Brendel, Matthias
    Ermoschkin, Larissa
    Gosewisch, Astrid
    Brunegraf, Anika
    Kmpfel, Tania
    Kerschensteiner, Martin
    Bartenstein, Peter
    Boening, Guido
    [J]. JOURNAL OF NUCLEAR MEDICINE, 2017, 58
  • [45] First quantification results for the new TSPO radioligand [18F]GE-180 in patients with multiple sclerosis
    Vomacka, L.
    Albert, N. L.
    Lindner, S.
    Unterrainer, M.
    Mahler, C.
    Brendel, M.
    Ermoschkin, L.
    Gosewisch, A.
    Brunegraf, A.
    Buckley, C.
    Trigg, W.
    Kuempfel, T.
    Rupprecht, R.
    Kerschensteiner, M.
    Bartenstein, P.
    Boening, G.
    [J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2017, 44 : S420 - S421
  • [46] TSPO PET with [18F]GE-180 sensitively detects focal neuroinflammation in patients with relapsing-remitting multiple sclerosis
    Unterrainer, Marcus
    Mahler, C.
    Vomacka, L.
    Lindner, S.
    Havla, J.
    Brendel, M.
    Boening, G.
    Ertl-Wagner, B.
    Kuempfel, T.
    Milenkovic, V. M.
    Rupprecht, R.
    Kerschensteiner, M.
    Bartenstein, P.
    Albert, Nathalie L.
    [J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2018, 45 (08) : 1423 - 1431
  • [47] Synthesis of 6-[18F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET
    Damont, Annelaure
    Boisgard, Raphael
    Kuhnast, Bertrand
    Lemee, Frederic
    Raggiri, Guillaume
    Scarf, Alana M.
    Da Pozzo, Eleonora
    Selleri, Silvia
    Martini, Claudia
    Tavitian, Bertrand
    Kassiou, Michael
    Dolle, Frederic
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (16) : 4819 - 4822
  • [48] Evolving understanding of translocator protein 18 kDa (TSPO)
    Li, Fei
    Liu, Jian
    Garavito, R. Michael
    Ferguson-Miller, Shelagh
    [J]. PHARMACOLOGICAL RESEARCH, 2015, 99 : 404 - 409
  • [49] Initial Evaluation of [18F]GE-180 PET Imaging in Relapsing-Remitting Multiple Sclerosis Patients
    Sridharan, S.
    Buckley, C.
    Trigg, W.
    Trigg, W.
    Heurling, K.
    Sherwin, P.
    Brooks, D.
    Crouch, J.
    Crouch, J.
    Lawler, M.
    Hinz, R.
    Paulseth, R.
    Amodeo, S.
    Gulenchyn, K.
    [J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2015, 42 : S276 - S277
  • [50] A novel 18F-labelled high affinity agent for PET imaging of the translocator protein
    Blair, Adele
    Zmuda, Filip
    Malviya, Gaurav
    Tavares, Adriana A. S.
    Tamagnan, Gilles D.
    Chalmers, Anthony J.
    Dewar, Deborah
    Pimlott, Sally L.
    Sutherland, Andrew
    [J]. CHEMICAL SCIENCE, 2015, 6 (08) : 4772 - 4777
12345