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Re(I) Tri-Carbonyl Based Radiopharmaceuticals; Synthesis, in vitro Studies, and Protein Complexation

Binkley, Sarah L

Abstract Details

2016, Doctor of Philosophy, University of Akron, Chemistry.
99mTc is the most used radionuclide in diagnostic nuclear medicine. Technetium small molecule imaging agents are being used to image almost every tissue in the body, from heart and bones, to the difficult imaging of brain tissue. Though there are many 99mTc complexes currently in use, the search for an ideal technetium radiopharmaceutical is ongoing. Ideal imaging agents must be robust enough to withstand complex biological conditions and ensure clearance from the body, yet selective enough to reach their target tissues for successful scanning. Recent work has shown that compounds based on the fac-99mTc(I)(CO)3+ core exhibit increased stability and resistance to decomposition. The chemistry and pharmacokinetics of these complexes can be safely explored using the non-radioactive, isoelectronic Re(I)(CO)3+ species. Medically useful isotopes of rhenium, 188Re and 186Re, add to the potential applications of this chemistry. In this dissertation we describe the synthesis and metathesis of [Re(CO)3(TAME)]X (where X= Br-, Cl-, NO3-, ClO4-, and PF6-), and it’s toxicity in both primary and immortal cell culture lines. The toxicity of the parent molecule, [Re(CO)3(OH2)3]Br, in HeLa-S3 cell culture is explored. The preparation and characterization of a Re(CO)3+-lysozyme adduct is discussed. Additional studies of the efficacy of [Re(CO)3(OH2)3]Br as an X-ray contrast agent and the preparation and partial characterization of an Re(CO)3+-insulin adduct is also described herein.
Christopher Ziegler, Dr. (Advisor)
Thomas Leeper, Dr. (Committee Member)
Sailaja Paruchuri, Dr. (Committee Member)
Leah Shriver, Dr. (Committee Member)
Todd Blackledge, Dr. (Committee Member)
195 p.

Recommended Citations

Citations

  • Binkley, S. L. (2016). Re(I) Tri-Carbonyl Based Radiopharmaceuticals; Synthesis, in vitro Studies, and Protein Complexation [Doctoral dissertation, University of Akron]. OhioLINK Electronic Theses and Dissertations Center. http://rave.ohiolink.edu/etdc/view?acc_num=akron1469473412

    APA Style (7th edition)

  • Binkley, Sarah. Re(I) Tri-Carbonyl Based Radiopharmaceuticals; Synthesis, in vitro Studies, and Protein Complexation. 2016. University of Akron, Doctoral dissertation. OhioLINK Electronic Theses and Dissertations Center, http://rave.ohiolink.edu/etdc/view?acc_num=akron1469473412.

    MLA Style (8th edition)

  • Binkley, Sarah. "Re(I) Tri-Carbonyl Based Radiopharmaceuticals; Synthesis, in vitro Studies, and Protein Complexation." Doctoral dissertation, University of Akron, 2016. http://rave.ohiolink.edu/etdc/view?acc_num=akron1469473412

    Chicago Manual of Style (17th edition)