Abstract
Introduction: Hypoxia imaging agents can selectively remain in hypoxic tissue, which can directly reflect the location and degree of hypoxia.
Methods: Synthesized a novel tumor hypoxia imaging probe [99mTc]Tc(CO)3-CPA-2-NIM and evaluated its biological behavior with the purpose to assess its possibility of becoming a qualified tumor hypoxia imaging agent.
Results: Radiochemcial purity of [99mTc]Tc(CO)3-CPA-2-NIM was greater than 95% after HPLC purification. Lipophilicity coefficient of this complex was -1.74 ± 0.10 (n = 5, number of experiments), indicating it was a hydrophilic complex. In vitro cell experiments demonstrated that this complex has selectivity for hypoxia at oxygen concentrations < 10 ppm (parts per million). Biodistribution experiment in S180 tumor bearing mice showed that tumor uptake reached its highest at 2 h post-injection with mice tumor-to-muscle ratio.
Conclusions: Complex [99mTc]Tc(CO)3-CPA-2-NIM has the possibility of becoming a tumor hypoxia imaging agent.
Graphical Abstract
[http://dx.doi.org/10.1007/978-1-4939-7665-2_25] [PMID: 29330809]
[http://dx.doi.org/10.1016/j.bmcl.2003.11.017] [PMID: 14741282]
[PMID: 17706178]
[PMID: 33757460]
[http://dx.doi.org/10.1016/j.apradiso.2011.02.025] [PMID: 21420304]
[http://dx.doi.org/10.3390/cells8121487]
[http://dx.doi.org/10.3109/0284186X.2015.1067721] [PMID: 26203928]
[PMID: 8274515]
[PMID: 8274515]
[http://dx.doi.org/10.1007/BF01247374] [PMID: 8612666]
[http://dx.doi.org/10.1021/ja980745t]
[http://dx.doi.org/10.1016/j.bmc.2006.08.011] [PMID: 16949291]
[http://dx.doi.org/10.1016/j.bmcl.2014.06.051] [PMID: 25001483]
[http://dx.doi.org/10.1007/s10967-010-0455-2]
[http://dx.doi.org/10.1016/j.bmcl.2006.01.001] [PMID: 16460938]