Open AccessEvaluation of Pan-SSTRs Targeted Radioligand [64Cu]NOTA-PA1 Using Micro-PET Imaging in Xenografted Mice
Author(s) -
Fei Liu,
Xiaoyi Guo,
Teli Liu,
Xiaoxia Xu,
Nan Li,
Chiyi Xiong,
Chun Li,
Hua Zhu,
Yang Liu
Publication year - 2020
Publication title -
acs medicinal chemistry letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.065
H-Index - 66
ISSN - 1948-5875
DOI - 10.1021/acsmedchemlett.9b00544
Subject(s) - biodistribution , somatostatin receptor , radiosynthesis , in vivo , somatostatin , radioligand , chemistry , octreotide , nuclear medicine , molecular imaging , preclinical imaging , in vitro , cancer research , positron emission tomography , medicine , biochemistry , biology , microbiology and biotechnology
64 Cu-labeled new pan-somatostatin receptors (pan-SSTRs) probe PA1 was synthesized, characterized, and evaluated by in vitro and in vivo experiments. [ 64 Cu]NOTA-PA1 was obtained with high specific activity, high radiochemical purity, and good stability. Cell uptake of [ 64 Cu]NOTA-PA1 was higher than that of [ 64 Cu]DOTA-TATE in MCF-7, A549, BGC823, and HT-29 cell lines. [ 64 Cu]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 [ 64 Cu]NOTA-PA1 revealed good detection ability in MCF-7 and A549 xenografted nude mice. The radiosynthesis, quality control, and preliminary biological evaluation of [ 64 Cu]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.