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Molecules 2018, 23(3), 702; https://doi.org/10.3390/molecules23030702

Bridging from Brain to Tumor Imaging: (S)-(−)- and (R)-(+)-[18F]Fluspidine for Investigation of Sigma-1 Receptors in Tumor-Bearing Mice

1
Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, 04318 Leipzig, Germany
2
Department of Diagnostic Radiology, PET Center, Yale University School of Medicine, New Haven, CT 06519, USA
3
Department of Radiopharmaceutical and Chemical Biology, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, 01328 Dresden, Germany
4
Department of Neurosurgery and Biomedical Engineering, Yale University School of Medicine, New Haven, CT 06519, USA
5
Technische Universität Dresden, School of Science, Faculty of Chemistry and Food Chemistry, 01062 Dresden, Germany
This publication is dedicated to Professor Jörg Steinbach on the occasion of his 65th birthday.
These authors contributed equally.
*
Author to whom correspondence should be addressed.
Received: 27 January 2018 / Revised: 12 March 2018 / Accepted: 18 March 2018 / Published: 20 March 2018
(This article belongs to the Special Issue Current Aspects of Radiopharmaceutical Chemistry)
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Abstract

Sigma-1 receptors (Sig1R) are highly expressed in various human cancer cells and hence imaging of this target with positron emission tomography (PET) can contribute to a better understanding of tumor pathophysiology and support the development of antineoplastic drugs. Two Sig1R-specific radiolabeled enantiomers (S)-(−)- and (R)-(+)-[18F]fluspidine were investigated in several tumor cell lines including melanoma, squamous cell/epidermoid carcinoma, prostate carcinoma, and glioblastoma. Dynamic PET scans were performed in mice to investigate the suitability of both radiotracers for tumor imaging. The Sig1R expression in the respective tumors was confirmed by Western blot. Rather low radiotracer uptake was found in heterotopically (subcutaneously) implanted tumors. Therefore, a brain tumor model (U87-MG) with orthotopic implantation was chosen to investigate the suitability of the two Sig1R radiotracers for brain tumor imaging. High tumor uptake as well as a favorable tumor-to-background ratio was found. These results suggest that Sig1R PET imaging of brain tumors with [18F]fluspidine could be possible. Further studies with this tumor model will be performed to confirm specific binding and the integrity of the blood-brain barrier (BBB). View Full-Text
Keywords: [18F]fluspidine; carcinoma; glioblastoma; melanoma; sigma-1 receptor; dedicated small animal PET/CT [18F]fluspidine; carcinoma; glioblastoma; melanoma; sigma-1 receptor; dedicated small animal PET/CT
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Kranz, M.; Bergmann, R.; Kniess, T.; Belter, B.; Neuber, C.; Cai, Z.; Deng, G.; Fischer, S.; Zhou, J.; Huang, Y.; Brust, P.; Deuther-Conrad, W.; Pietzsch, J. Bridging from Brain to Tumor Imaging: (S)-(−)- and (R)-(+)-[18F]Fluspidine for Investigation of Sigma-1 Receptors in Tumor-Bearing Mice. Molecules 2018, 23, 702.

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