Abstract:
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 [(18)F]DPA-714 for positron emission tomography (PET) imaging of cancer and inflammation. PROCEDURES:[(18)F]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:[(18)F]DPA-714 showed different uptake levels in healthy organs and malignant tissues of mice and rats. Although high and displaceable [(18)F]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 [(18)F]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.
journal_name
Mol Imaging Bioljournal_title
Molecular imaging and biologyauthors
Zheng J,Winkeler A,Peyronneau MA,Dollé F,Boisgard Rdoi
10.1007/s11307-015-0877-xsubject
Has Abstractpub_date
2016-02-01 00:00:00pages
127-34issue
1eissn
1536-1632issn
1860-2002pii
10.1007/s11307-015-0877-xjournal_volume
18pub_type
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