scholarly journals Novel 99mTc labelled complexes with 2-nitroimidazole isocyanide: design, synthesis and evaluation as potential tumor hypoxia imaging agents

MedChemComm ◽  
2018 ◽  
Vol 9 (6) ◽  
pp. 988-994 ◽  
Author(s):  
Qing Ruan ◽  
Xuran Zhang ◽  
Xiao Lin ◽  
Xiaojiang Duan ◽  
Junbo Zhang
Keyword(s):  
Tumor Hypoxia ◽  
Imaging Agents ◽  
Hypoxia Imaging ◽  
Design Synthesis ◽  
Direct Labelling ◽  
Labelling Method

99mTc-2c can be prepared by a direct labelling method without the need for heating and would be a promising probe for hypoxia imaging.

scholarly journals Design, Synthesis and Labeling of Tripeptide Derivatives with 99mTc as Hypoxia Imaging Agents

2019 ◽  
Vol 22 (3) ◽  
pp. 160-173
Author(s):  
Mohammad Hassan Houshdar Tehrnai ◽  
Mahtab Mohammadpoor ◽  
Soraya Shahhosseini ◽  
◽  
◽  
...  
Keyword(s):  
Imaging Agents ◽  
Hypoxia Imaging ◽  
Design Synthesis

Ferritin-Conjugated Antibody for the Demonstration of Isoantigens on the Surface of Murine Cells

1968 ◽  
Vol 26 ◽  
pp. 48-49
Author(s):  
T. Aoki ◽  
J. Izard ◽  
U. Hämmerling ◽  
E. de Harven ◽  
L. J. Old
Keyword(s):  
Cell Surface ◽  
Gamma Globulin ◽  
Leukemia Cells ◽  
Labelling Technique ◽  
Direct Labelling ◽  
Labelling Method

Although a variety of viral and cellular antigens have been demonstrated by ferritin-labeled antibody, this technique has not been used to locate isoantigens on the surface of nucleated cells. The recognition of several systems of isoantigens on the surface of thymocytes, lymphocytes and leukemia cells of the mouse and the ease with which these cells can be obtained in free suspension led us to consider the ferritin-labelling method to determine the amount and location of these isoantigens on the cell surface. Because of the problems involved in the direct labelling of mouse gamma globulin by ferritin, we have chosen an indirect labelling technique (i.e. ferritin-conjugated rabbit anti mouse γG)to detect localization of mouse isoantibody.

scholarly journals Significant impact of different oxygen breathing conditions on noninvasive in vivo tumor-hypoxia imaging using [18F]-fluoro-azomycinarabino-furanoside ([18F]FAZA)

2011 ◽  
Vol 6 (1) ◽  
pp. 165 ◽  
Author(s):  
Florian C Maier ◽  
Manfred Kneilling ◽  
Gerald Reischl ◽  
Funda Cay ◽  
Daniel Bukala ◽  
...  
Keyword(s):  
Tumor Hypoxia ◽  
Hypoxia Imaging ◽  
Oxygen Breathing

scholarly journals 2-Nitroimidazole-Furanoside Derivatives for Hypoxia Imaging—Investigation of Nucleoside Transporter Interaction, 18F-Labeling and Preclinical PET Imaging

2019 ◽  
Vol 12 (1) ◽  
pp. 31
Author(s):  
Florian Maier ◽  
Anna Schweifer ◽  
Vijaya Damaraju ◽  
Carol Cass ◽  
Gregory Bowden ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Tumor Hypoxia ◽  
Radiochemical Yield ◽  
Nucleoside Transporters ◽  
Nucleoside Transporter ◽  
Hypoxia Imaging ◽  
Molar Activity ◽  
Slow Kinetics ◽  
Sugar Derivatives

The benefits of PET imaging of tumor hypoxia in patient management has been demonstrated in many examples and with various tracers over the last years. Although, the optimal hypoxia imaging agent has yet to be found, 2-nitroimidazole (azomycin) sugar derivatives—mimicking nucleosides—have proven their potential with [18F]FAZA ([18F]fluoro-azomycin-α-arabinoside) as a prominent representative in clinical use. Still, for all of these tracers, cellular uptake by passive diffusion is postulated with the disadvantage of slow kinetics and low tumor-to-background ratios. We recently evaluated [18F]fluoro-azomycin-β-deoxyriboside (β-[18F]FAZDR), with a structure more similar to nucleosides than [18F]FAZA and possible interaction with nucleoside transporters. For a deeper insight, we comparatively studied the interaction of FAZA, β-FAZA, α-FAZDR and β-FAZDR with nucleoside transporters (SLC29A1/2 and SLC28A1/2/3) in vitro, showing variable interactions of the compounds. The highest interactions being for β-FAZDR (IC50 124 ± 33 µM for SLC28A3), but also for FAZA with the non-nucleosidic α-configuration, the interactions were remarkable (290 ± 44 µM {SLC28A1}; 640 ± 10 µM {SLC28A2}). An improved synthesis was developed for β-FAZA. For a PET study in tumor-bearing mice, α-[18F]FAZDR was synthesized (radiochemical yield: 15.9 ± 9.0% (n = 3), max. 10.3 GBq, molar activity > 50 GBq/µmol) and compared to β-[18F]FAZDR and [18F]FMISO, the hypoxia imaging gold standard. We observed highest tumor-to-muscle ratios (TMR) for β-[18F]FAZDR already at 1 h p.i. (2.52 ± 0.94, n = 4) in comparison to [18F]FMISO (1.37 ± 0.11, n = 5) and α-[18F]FAZDR (1.93 ± 0.39, n = 4), with possible mediation by the involvement of nucleoside transporters. After 3 h p.i., TMR were not significantly different for all 3 tracers (2.5–3.0). Highest clearance from tumor tissue was observed for β-[18F]FAZDR (56.6 ± 6.8%, 2 h p.i.), followed by α-[18F]FAZDR (34.2 ± 7.5%) and [18F]FMISO (11.8 ± 6.5%). In conclusion, both isomers of [18F]FAZDR showed their potential as PET hypoxia tracers. Differences in uptake behavior may be attributed to a potential variable involvement of transport mechanisms.

89Zr-incorporated iron oxide nanocluster by chelator-free simple direct-labelling method for PET diagnosis

2019 ◽  
Vol 72-73 ◽  
pp. S63
Author(s):  
P. Choi ◽  
J. Lee ◽  
C. Vyas ◽  
Y. Gong ◽  
E. Lee ◽  
...  
Keyword(s):  
Iron Oxide ◽  
Direct Labelling ◽  
Labelling Method

Design strategy of optical probes for tumor hypoxia imaging

2020 ◽  
Vol 63 (12) ◽  
pp. 1786-1797 ◽  
Author(s):  
Fengfeng Xue ◽  
Jufeng Chen ◽  
Hangrong Chen
Keyword(s):  
Tumor Hypoxia ◽  
Design Strategy ◽  
Hypoxia Imaging ◽  
Optical Probes

Synthesis and biodistribution of novel 99mTc labeled 4-nitroimidazole dithiocarbamate complexes as potential agents to target tumor hypoxia

MedChemComm ◽  
2015 ◽  
Vol 6 (6) ◽  
pp. 1143-1148 ◽  
Author(s):  
Zhenxiang Li ◽  
Junbo Zhang ◽  
Zhonghui Jin ◽  
Weifang Zhang ◽  
Yanyan Zhang
Keyword(s):  
Tumor Hypoxia ◽  
Imaging Agent ◽  
Hypoxia Imaging

99mTcO-N4IPDTC was prepared from a kit without the need for purification and would be a promising hypoxia imaging agent.

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