64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents.

64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents. Research Abstract Details 

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64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents. Abstract Text:

Jianjun Wang,Chang-Tong Yang,Young-Seung Kim,Subramanya G Sreerama,Qizhen Cao,Zi-Bo Li,Zhengjie He,Xiaoyuan Chen,Shuang Liu,Jianjun Wang,Chang-Tong Yang,Young-Seung Kim,Subramanya G Sreerama,Qizhen Cao,Zi-Bo Li,Zhengjie He,Xiaoyuan Chen,Shuang Liu,

This report presents synthesis and evaluation of the 64Cu-labeled triphenylphosphonium (TPP) cations as new radiotracers for imaging tumors by positron emission tomography. Biodistribution properties of 64Cu-L1, 64Cu-L2, 64Cu-L3, and 99mTc-Sestamibi were evaluated in athymic nude mice bearing U87MG human glioma xenografts. The most striking difference is that 64Cu-L1, 64Cu-L2, and 64Cu-L3 have much lower heart uptake (<0.6% ID/g) than 99mTc-Sestamibi ( approximately 18% ID/g) at >30 min p.i. Their tumor/heart ratios increase steadily from approximately 1 at 5 min p.i. to approximately 5 at 120 min p.i. The tumor/heart ratio of 64Cu-L3 is approximately 40 times better than that of 99mTc-Sestamibi at 120 min postinjection. Results from in vitro assays show that 64Cu-L1 is able to localize in tumor mitochondria. The tumor is clearly visualized in the tumor-bearing mice administered with 64Cu-L1 as 30 min postinjection. The 64Cu-labeled TPP/TPA cations are very selective radiotracers that are able to provide the information of mitochondrial bioenergetic function in tumors by monitoring mitochondrial potential in a noninvasive fashion.

64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents. Publishing Authors By Initials

J Wang,CT Yang,YS Kim,SG Sreerama,Q Cao,ZB Li,Z He,X Chen,S Liu,J Wang,CT Yang,YS Kim,SG Sreerama,Q Cao,ZB Li,Z He,X Chen,S Liu,

For similar surgical procedures, operative: transplantation: transplantation, heterologous research abstracts see: surgical procedures, operative: transplantation: transplantation, heterologous research

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64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Journal of medicinal chemistry

VOLUME: 50

Page Numbers: 5057-69

Journal Abbreviation: J. Med. Chem.

ISSN: 0022-2623

DAY: 15

MONTH: 09

YEAR: 2007

64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9716531

64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents. Keywords Mesh Terms:

KEYWORDS: Transplantation, Heterologous

MESH TERMS: pharmacokinetics

Chemical & Substance for Abstract: 64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents. Information

Substance Name: Radiopharmaceuticals

Registry Number: 0

Grant and Affiliation Information for 64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents.

AFFILIATION: School of Health Sciences, Purdue University, West Lafayette, Indiana, USA.

Country: United States

AGENCY: United States NHLBI

GRANT: R21 HL083961-01

ACRONYM: HL

MEDLINETA: J Med Chem

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