Evaluation of PET Imaging Performance of the TSPO Radioligand [18F]DPA-714 in Mouse and Rat Models of Cancer and Inflammation.
Authors/Creators
- 1. Inserm U1023, Laboratoire d'Imagerie Moléculaire Expérimentale, Université Paris Sud, Orsay, France; CEA, DSV/I2BM, Service Hospitalier Frédéric Joliot, Orsay, France; Techna Institute, University Health Network, 101 College Street, Room 7-302, Toronto, Ontario, CanadaM5G 1L7 and Institute of Biomaterials and Biomedical Engineering, University of Toronto, Toronto, Ontario, Canada
- 2. Inserm U1023, Laboratoire d'Imagerie Moléculaire Expérimentale, Université Paris Sud, Orsay, France and CEA, DSV/I2BM, Service Hospitalier Frédéric Joliot, Orsay, France
- 3. CEA, DSV/I2BM, Service Hospitalier Frédéric Joliot, Orsay, France
Description
PURPOSE:
Many radioligands have been explored for imaging the 18-kDa translocator protein (TSPO), a diagnostic and therapeutic target for inflammation and cancer. Here, we investigated the TSPO radioligand [18F]DPA-714 for positron emission tomography (PET) imaging of cancer and inflammation.
PROCEDURES:
[18F]DPA-714 PET imaging was performed in 8 mouse and rat models of breast and brain cancer and 4 mouse and rat models of muscular and bowel inflammation.
RESULTS:
[18F]DPA-714 showed different uptake levels in healthy organs and malignant tissues of mice and rats. Although high and displaceable [18F]DPA-714 binding is observed ex vivo, TSPO-positive PET imaging of peripheral lesions of cancer and inflammation in mice did not show significant lesion-to-background signal ratios. Slower [18F]DPA-714 metabolism and muscle clearance in mice compared to rats may explain the elevated background signal in peripheral organs in this species.
CONCLUSION:
Although TSPO is an evolutionary conserved protein, inter- and intra-species differences call for further exploration of the pharmacological parameters of TSPO radioligands.
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Zheng_MolImagingBiol_2015-P08.pdf
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