Evaluation of Pan-SSTRs Targeted Radioligand [64Cu]NOTA-PA1 Using Micro-PET Imaging in Xenografted Mice

Fei Liu, Xiaoyi Guo, Teli Liu, Xiaoxia Xu, Nan Li, Chiyi Xiong, Chun Li, Hua Zhu, Zhi Yang

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

64Cu-labeled new pan-somatostatin receptors (pan-SSTRs) probe PA1 was synthesized, characterized, and evaluated by in vitro and in vivo experiments. [64Cu]NOTA-PA1 was obtained with high specific activity, high radiochemical purity, and good stability. Cell uptake of [64Cu]NOTA-PA1 was higher than that of [64Cu]DOTA-TATE in MCF-7, A549, BGC823, and HT-29 cell lines. [64Cu]NOTA-PA1 showed high binding affinity for SSTRs expressed in A549 cells. The in vivo biodistribution and micropositron emission tomography (micro-PET) imaging studies of [64Cu]NOTA-PA1 revealed good detection ability in MCF-7 and A549 xenografted nude mice. The radiosynthesis, quality control, and preliminary biological evaluation of [64Cu]NOTA-PA1 have broaden the application of radiolabeled octreotide for SSTRs imaging, which could act as a potential multisubtypes targeted radiotracer for imaging SSTRs-positive tumors.

Original languageEnglish (US)
Pages (from-to)445-450
Number of pages6
JournalACS Medicinal Chemistry Letters
Volume11
Issue number4
DOIs
StatePublished - Apr 9 2020
Externally publishedYes

Keywords

  • Somatostatin analogues
  • [Cu]NOTA-PA1
  • molecular imaging
  • positron emission tomography imaging

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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