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Improved radiosynthesis and preliminary in vivo evaluation of the 11C-labeled tetrazine [11C]AE-1 for pretargeted PET imaging.
Stéen, E Johanna L; Jørgensen, Jesper T; Petersen, Ida N; Nørregaard, Kamilla; Lehel, Szabolcs; Shalgunov, Vladimir; Birke, Alexander; Edem, Patricia E; L'Estrade, Elina T; Hansen, Hanne D; Villadsen, Jonas; Erlandsson, Maria; Ohlsson, Tomas; Yazdani, Abdolreza; Valliant, John F; Kristensen, Jesper L; Barz, Matthias; Knudsen, Gitte M; Kjær, Andreas; Herth, Matthias M.
Afiliação
  • Stéen EJL; Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark; Department of Clinical Physiology, Nuclear Medicine and PET, University Hospital Copenhagen, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen,
  • Jørgensen JT; Department of Clinical Physiology, Nuclear Medicine and PET, University Hospital Copenhagen, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark; Cluster for Molecular Imaging, Department of Biomedical Sciences, University of Copenhagen, Blegdamsvej 3, 2200 Copenhagen, Denmark.
  • Petersen IN; Department of Clinical Physiology, Nuclear Medicine and PET, University Hospital Copenhagen, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark; Cluster for Molecular Imaging, Department of Biomedical Sciences, University of Copenhagen, Blegdamsvej 3, 2200 Copenhagen, Denmark.
  • Nørregaard K; Department of Clinical Physiology, Nuclear Medicine and PET, University Hospital Copenhagen, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark; Cluster for Molecular Imaging, Department of Biomedical Sciences, University of Copenhagen, Blegdamsvej 3, 2200 Copenhagen, Denmark.
  • Lehel S; Department of Clinical Physiology, Nuclear Medicine and PET, University Hospital Copenhagen, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark.
  • Shalgunov V; Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
  • Birke A; Institute of Organic Chemistry, Johannes-Gutenberg University, Duesbergweg 10-14, D-55099 Mainz, Germany.
  • Edem PE; Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark; Department of Clinical Physiology, Nuclear Medicine and PET, University Hospital Copenhagen, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen,
  • L'Estrade ET; Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark; Department of Clinical Physiology, Nuclear Medicine and PET, University Hospital Copenhagen, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen,
  • Hansen HD; Neurobiology Research Unit, Rigshospitalet and University of Copenhagen, Blegdamsvej 9, 2100 Copenhagen, Denmark.
  • Villadsen J; Neurobiology Research Unit, Rigshospitalet and University of Copenhagen, Blegdamsvej 9, 2100 Copenhagen, Denmark.
  • Erlandsson M; Radiation Physics, Nuclear Medicine Physics Unit, Skånes University Hospital, Barngatan 3, 222 42 Lund, Sweden.
  • Ohlsson T; Radiation Physics, Nuclear Medicine Physics Unit, Skånes University Hospital, Barngatan 3, 222 42 Lund, Sweden.
  • Yazdani A; Department of Chemistry and Chemical Biology, McMaster University, 1280 Main Street West, Hamilton, Ontario L8S 4M1, Canada.
  • Valliant JF; Department of Chemistry and Chemical Biology, McMaster University, 1280 Main Street West, Hamilton, Ontario L8S 4M1, Canada.
  • Kristensen JL; Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
  • Barz M; Institute of Organic Chemistry, Johannes-Gutenberg University, Duesbergweg 10-14, D-55099 Mainz, Germany.
  • Knudsen GM; Neurobiology Research Unit, Rigshospitalet and University of Copenhagen, Blegdamsvej 9, 2100 Copenhagen, Denmark.
  • Kjær A; Department of Clinical Physiology, Nuclear Medicine and PET, University Hospital Copenhagen, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark; Cluster for Molecular Imaging, Department of Biomedical Sciences, University of Copenhagen, Blegdamsvej 3, 2200 Copenhagen, Denmark. Electronic addres
  • Herth MM; Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark; Department of Clinical Physiology, Nuclear Medicine and PET, University Hospital Copenhagen, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen,
Bioorg Med Chem Lett ; 29(8): 986-990, 2019 04 15.
Article em En | MEDLINE | ID: mdl-30795854
Pretargeted nuclear imaging based on the ligation between tetrazines and nano-sized targeting agents functionalized with trans-cyclooctene (TCO) has recently been shown to improve both imaging contrast and dosimetry in nuclear imaging of nanomedicines. Herein, we describe the improved radiosynthesis of a 11C-labeled tetrazine ([11C]AE-1) and its preliminary evaluation in both mice and pigs. Pretargeted imaging in mice was carried out using both a new TCO-functionalized polyglutamic acid and a previously reported TCO-functionalized bisphosphonate system as targeting agents. Unfortunately, pretargeted imaging was not successful using these targeting agents in pair with [11C]AE-1. However, brain imaging in pig indicated that the tracer crossed the blood-brain-barrier. Hence, we suggest that this tetrazine scaffold could be used as a starting point for the development of pretargeted brain imaging, which has so far been a challenging task.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tetrazóis / Radioisótopos de Carbono / Compostos Radiofarmacêuticos / Tomografia por Emissão de Pósitrons Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tetrazóis / Radioisótopos de Carbono / Compostos Radiofarmacêuticos / Tomografia por Emissão de Pósitrons Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2019 Tipo de documento: Article