Journal of Radioanalytical and Nuclear Chemistry

, Volume 275, Issue 2, pp 379–385 | Cite as

99mTc-glucoheptonate-guanine: Synthesis, biodistribution and imaging in animals

  • P. Unak
  • S. Teksoz
  • F. Z. Biber Muftuler
  • E. I. Medine
  • C. Acar
  • Y. Yurekli
Article

Abstract

The aim of the current study was to design a nucleotide-based radiopharmaceutical which could be labeled with 99mTc and to investigate its radiopharmaceutical efficiency and stability. GHA (glucoheptonate) was used as bifunctional chelate. GHA was labeled with 99mTc by SnCl2 reduction method first, and then G (guanine) was conjugated with 99mTc-GHA at 90 °C. In order to determine its radiopharmaceutical stability, thin layer radio chromatography (TLRC) and electrophoresis were employed. In addition, the results were confirmed using high performance liquid radio chromatography (HPLRC). Scintigraphic imaging was performed on rats with mammary tumors, while tissue distribution was determined on Albino Wistar rats. Labeling yield was found to be over 95% and the labeled complex maintained its stability during the study period. The lipophilicity of the 99mTc-GHG was measured and the partition coefficient (logP) of the labeled compound calculated. The results demonstrated that the uptake of 99mTc-GHG (99mTc-glucoheptonate-guanine) reached its maximum at 3 hours p.i. in stomach and intestines. Main way of excretion was renal. Hepatobiliary excretion was also observed. In conclusion, 99mTc-GHG may be useful as a nucleotide-based radiopharmaceutical for in vivo applications.

Keywords

Guanine Mammary Tumor DMBA Gamma Camera Image Hepatobiliary Excretion 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

  1. 1.
    M. K. Dewanjee, M. Kapadvanjwala, A. Krishan, A. N. Serafini, A. K. Ghafouripour, E. L. Oates, D. M. Lopez, G. N. Sfakianakis, J. Clin. Immun., 16 (1993) 276.Google Scholar
  2. 2.
    M. K. Dewanjee, Diagnostatic Oncology, 3 (1993) 189.Google Scholar
  3. 3.
    D. J. Hnatowich Jr., P. Winnard, F. Virzi, M. Fogarasi, T. Sano, C. L. Smith, C. R. Cantor, M. Rusckowski, J. Nucl. Med., 36 (1995) 2306.Google Scholar
  4. 4.
    V. N. Karamychev, I. G. Panyutin, M. K. Kim, N. Le, C. H. Paik, J. A. Carrasquillo, M. W. Reed, R. D. Neumann, J. Nucl. Med., 41 (2000) 1093.Google Scholar
  5. 5.
    B. Gutfilen, E. Rodrigues, R. Soraggi, L. H. B. Da Fonseca, Nucl. Med. Com., 22 (2001) 1133.CrossRefGoogle Scholar
  6. 6.
    U. Muhlhausen, R. Schirrmacher, M. Piel, B. Lecher, M. Briegert, A. Piee-Staffa, B. Kaina, F. Rosch, J. Med. Chem., 49 (2006) 263.CrossRefGoogle Scholar
  7. 7.
    B. Gutfilen, B. L. A. Ribeiro, M. F. Mattos, C. R. Dasilva, M. Bernardo, Arquivos de Biologia e Tecnologia, 39 (1996) 69.Google Scholar
  8. 8.
    V. N. Karamychev, M. W. Reed, R. D. Neumann, I. G. Panyutin, Acta Oncol., 39 (2000) 687.CrossRefGoogle Scholar
  9. 9.
    D. J. Yang, K. Ozaki, C. S. Oh, A. Azhdarinia, T. Yang, M. Ito, A. Greenwe, J. Bryant, S. Kohanim, V. K. Wong, E. E. Kim, Pharm. Res., 22 (2005) 1472.CrossRefGoogle Scholar
  10. 10.
    S. Pervez, A. Mushtaq, M. Arif, Z. H. Chohan, J. Radioanal. Nucl. Chem., 256 (2003) 293.CrossRefGoogle Scholar
  11. 11.
    Y. Peña, M. A. Coca, A. Perera, J. F. Batista, M. L. Bush, E. L. Sa'nchez, Clin. Nucl. Med., 30 (2005) 126.CrossRefGoogle Scholar
  12. 12.
    S. Barai, G. P. Bandopadhayaya, P. K. Julka, S. S. Kale, R. Kumar, A. Malhotra, A. K. Haloi, A. Seith, K. K. Naik, H. Dhanapathi, J. Clin. Neurosci., 12 (2005) 36.CrossRefGoogle Scholar
  13. 13.
    F. Z. Biber, P. Unak, T. Ertay, E. İ. Medine, F. Zihnioglu, C. Tasci, H. Durak, Appl. Radiation Isotopes, 64 (2006) 778.CrossRefGoogle Scholar
  14. 14.
    T. Ertay, P. Unak, C. Tasci, F. Z. Biber, F. Zihnioglu, H. Durak, J. Radioanal. Nucl. Chem., 265 (2005) 475.CrossRefGoogle Scholar
  15. 15.
    T. Ertay, P. Unak, C. Tasci, F. Z. Biber, F. Zihnioglu, E. İ. Medine, H. Durak, J. Radioanal. Nucl. Chem., 269 (2006) 21.CrossRefGoogle Scholar
  16. 16.
    E. S. Delpassand, D. G. Yang, S. Wallace, A. Cherif, S. M. Quadri, G. Price, A. Goubert, T. Inoue, D. A. Podoloff, J. Pharm. Sci., 85 (1996) 553.CrossRefGoogle Scholar
  17. 17.
    R. Mannhold, H. Waterbeemd, J. Computer-Aided Molecular Design, 15 (2001) 337.CrossRefGoogle Scholar
  18. 18.
    T. Ertay, P. Unak, F. Z. Biber, C. Tasci, F. Zihnioglu, H. Durak, Appl. Radiation Isotopes, 65 (2007) 170.CrossRefGoogle Scholar
  19. 19.
    T. Ertay, P. Unak, C. Tasci, F. Zihnioglu, H. Durak, Appl. Radiation Isotopes, 62 (2005) 883.CrossRefGoogle Scholar
  20. 20.
    H. Mäcke, Schweizerische Medizinische Wochenschrift, 9 (1991) 299.Google Scholar
  21. 21.
    M. Jong, W. H. Bakker, B. F. Bernard, R. Valkema, D. J. J. Kwekkeboom, C. Reubi, A. Srinivasan, M. Schmidt, E. P. Krenning, J. Nucl. Med., 40 (1999) 2081.Google Scholar
  22. 22.
    W. H. Strauss, A. Nunn, K. Linder, J. Nucl. Cardiol., 2 (1995) 437.CrossRefGoogle Scholar
  23. 23.
    D. E. Ponde, C. S. Dence, D. P. Schuster, M. J. Welch, Nucl. Med. Biol., 31 (2004) 133.CrossRefGoogle Scholar
  24. 24.
    D. A. Mankoff, A. F. Shields, J. M. Link, M. M. Graham, M. Muzi, L. M. Peterson, J. Nucl. Med., 40 (1999) 614.Google Scholar

Copyright information

© Springer Science+Business Media, LLC. 2008

Authors and Affiliations

  • P. Unak
    • 1
  • S. Teksoz
    • 1
  • F. Z. Biber Muftuler
    • 1
  • E. I. Medine
    • 1
  • C. Acar
    • 1
  • Y. Yurekli
    • 2
  1. 1.Department of Nuclear Applications, Institute of Nuclear SciencesEge UniversityBornova IzmirTurkey
  2. 2.Department of Nuclear Medicine, School of MedicineAdnan Menderes UniversityAydinTurkey

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