Abstract

The goal of the proposed work is the development of new and improved radiopharmaceuticals labeled with generator-produced metal radionuclides (Ga-68, Cu-62, Tc-99m) for use in diagnostic nuclear medicine. Major emphasis will be placed on the preparatoin of tracers for non-invasive evaluation or regional cerebral and myocardial blood flow. New compounds of these elements, possessing properties believed important in achieving the desired in vivo behavior, will be synthesized and characterized at macroscopic concentrations (10-3 -10-1M) using conventional chemical techniques. Radiolabeled compounds of these nuclides will then be prepared and characterized, with chromatographic techniques being employed to correlate chemistry at the no- carrier-added level with that defined at macroscopic concentrations. The potential of these radiolabeled compounds to serve as useful radiopharmaceuticals will be evaluated by biodistribution studies in rats. Compounds showing adequate uptake in organs of interest will be investigated in greater detail in larger animals (dogs). Suitability for organ imaging will be determined and comparisons with accepted tracers then employed to assess the physiological significance of the images obtained.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Cancer Institute (NCI)
Type
Research Project (R01)
Project #
7R01CA046909-02
Application #
3190416
Study Section
Diagnostic Radiology Study Section (RNM)
Project Start
1987-08-01
Project End
1990-05-31
Budget Start
1987-08-01
Budget End
1988-05-31
Support Year
2
Fiscal Year
1987
Total Cost
Indirect Cost

  Institution

Name
Purdue University
Department
Type
Schools of Pharmacy
DUNS #
072051394
City
West Lafayette
State
IN
Country
United States
Zip Code
47907

  Publications

Hsiao, Yui-May; Mathias, Carla J; Wey, Shiaw-Pyng et al. (2009) Synthesis and biodistribution of lipophilic and monocationic gallium radiopharmaceuticals derived from N,N'-bis(3-aminopropyl)-N,N'-dimethylethylenediamine: potential agents for PET myocardial imaging with 68Ga. Nucl Med Biol 36:39-45
Mathias, C J; Wang, S; Lee, R J et al. (1996) Tumor-selective radiopharmaceutical targeting via receptor-mediated endocytosis of gallium-67-deferoxamine-folate. J Nucl Med 37:1003-8
Yuan, H; Antholine, W E; Subczynski, W K et al. (1996) Release of CuPTSM from human serum albumin after addition of fatty acids. J Inorg Biochem 61:251-9
Mathias, C J; Bergmann, S R; Green, M A (1995) Species-dependent binding of copper(II) bis(thiosemicarbazone) radiopharmaceuticals to serum albumin. J Nucl Med 36:1451-5
John, E K; Bott, A J; Green, M A (1994) Preparation and biodistribution of copper-67 complexes with tetradentate Schiff-base ligands. J Pharm Sci 83:587-90
Tsang, B W; Mathias, C J; Fanwick, P E et al. (1994) Structure-distribution relationships for metal-labeled myocardial imaging agents: comparison of a series of cationic gallium (III) complexes with hexadentate bis(salicylaldimine) ligands. J Med Chem 37:4400-6
Mathias, C J; Green, M A; Morrison, W B et al. (1994) Evaluation of Cu-PTSM as a tracer of tumor perfusion: comparison with labeled microspheres in spontaneous canine neoplasms. Nucl Med Biol 21:83-7
Coggin, D K; Mathias, C J; Green, M A (1994) Investigation of [67Ga]dimethylgallium(III) acetylacetonate as a potential radiopharmaceutical. Nucl Med Biol 21:283-5
Green, M A; Mathias, C J; Neumann, W L et al. (1993) Potential gallium-68 tracers for imaging the heart with PET: evaluation of four gallium complexes with functionalized tripodal tris(salicylaldimine) ligands. J Nucl Med 34:228-33
Mathias, C J; Bergmann, S R; Green, M A (1993) Development and validation of a solvent extraction technique for determination of Cu-PTSM in blood. Nucl Med Biol 20:343-9

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