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South African Journal of Chemistry

On-line version ISSN 1996-840X
Print version ISSN 0379-4350

S.Afr.j.chem. (Online) vol.61  Durban  2008




Modelling of the blood plasma species of biguanide derivatives exhibiting potential as diagnostic radiopharmaceuticals



Judith M. WagenerI, * ; Midred K. DithebeI; Daniel MoganoII; Ignacy CukrowskiII; Jan Rijn ZeevaartIII

IRadiochemistry, NECSA, P.O. Box 582, Pretoria 0001, South Africa
IIDepartment of Chemistry, University of Pretoria, Pretoria 0002, South Africa
IIICARST, North West University, Mafikeng Campus, Private Bag X2046, Mmabatho 2735, South Africa




99mTc-DMSA (DMSA=dimercaptosuccinic acid), the gold standard for static renal imaging, has a long uptake time, which is a limiting factor in diagnostic procedures and also leads to a relatively high radiation dose to patients. The ligands dimethyl biguanide (DMBG), biuret (BIU), 2-imino-4-thiobiuret (ITB) and carboxy-biguanide (CBIG) have nitrogen donor atoms, which are able to complex transition elements. The formation constants needed in order to establish a blood plasma model for these ligands were determined by potentiometry and the results are reported herein. Based on blood plasma modelling, it was shown that the ligands had selectivity for 99mTc over blood plasma metal ions at physiological pH and it was therefore hypothesized that the Tc-ligand complex would survive in blood plasma. Furthermore, no or few side effects related to the mobilization of blood plasma metal ions by these ligands are expected, once the radiopharmaceutical has been administered. It is also expected that these ligands should clear rapidly from the blood plasma.

Keywords: Biguanides, kidney agents, stability formation constants, blood plasma speciation, CBIG, DMBG, BIU, ITB



Full text available only in pdf format.




1 P. Ray, Chem. Rev., 1962, 62, 313-359.         [ Links ]

2 Physics, techniques and procedures: Radionuclide renal imaging. General Electric Company 1997-2007, GE Healthcare. Accessed 2 August 2004.         [ Links ]

3 General practice notebook- a UK medical reference on the World Wide Web, Static renal scintigraphy, Oxbridge Solution Ltd., 2007. Accessed 2 August 2004.         [ Links ]

4 M. Neves, I. Dormehl, E. Kilian, W. Louw, K. Lalaoui and J.J. Pedroso de Lima, Nucl. Med. Biol., 2000, 27, 593-597.         [ Links ]

5 M. Neves, L. Gano, M. Joào Ribeiro, A.C. Santos, A. Marchi, C. Sawas-Dimopolou and J.J. Pedroso de Lima, Nucl. Med. Biol., 1999, 26, 79-83.         [ Links ]

6 A. Marchi, M. Neves, L. Marvelli, M. Cattabriga, R. Rossi, V. Bertolasi andV Ferretti, Technetium, Rhenium and Other Metals in Chemistry and Nuclear Medicine ( M. Nicolini and U. Mazzi, eds.), vol. 5,5th edn., SG Editoriali, Padova, Italy, 1999, pp. 271-275.         [ Links ]

7 M. Neves and R. Fautso, Nucl. Med. Biol., 1999, 26, 85-89.         [ Links ]

8 A. Marchi, L. Marvelli, M. Cattabriga, R. Rossi, M. Neves, V. Bertolasi and V. Ferretti, J. Chem. Soc, Dalton Trans., 1999, 1937-1943.         [ Links ]

9 S.D. Larsen, M.A. Connell, M.M. Cudahy, B.R. Evans, P.D. May, M.D. Meglasson, T.J. O'Sullivan, H.J. Schostarez, J.C. Sih, F.C. Stevens, S.P Tanis, C.M. Tegley, J.A. Tucker, VA. Vaillancourt, T.J. Vidmar, W. Watt and J.H. Yu, J. Med. Chem., 2001, 44, 1217-1230.         [ Links ]

10 J. R. Zeevaart, N.V. Jarvis and W.K.A. Louw, J. Inorg. Biochem., 2001, 83, 57-65.         [ Links ]

11 J. R. Zeevaart, W.K.A. Louw, Z.I. Kolar, J.M. Wagener, N.V. Jarvis and R.A.M.J. Claessens, J. Radioanal. Nucl. Chem., 2003, 257, 83-91.         [ Links ]

12 J. R. Zeevaart, D.R. Jansen, M.F. Botelho, A. Abrunhosa, C. Gomes, L. Metello, Z.I. Kolar, G.C. Krijger, W.K.A. Louw and I.C. Dormehl, J. Inorg. Biochem., 2004, 98, 1523-1530.         [ Links ]

13 P.M. May, K. Murray and D.R. Williams, Talanta, 1985, 32, 483-89.         [ Links ]

14 P.M. May, P.W. Linder and D.R. Williams, J. Chem. Soc., Dalton Trans., 1977, 588-95.         [ Links ]

15 A.E. Martell and R.M. Smith (eds), NIST Standard Reference Database 46, Version 8.0, Gaithersburg MD 20899, USA, 2003.         [ Links ]

16 J. R. Zeevaart and S. Olsen, Appl. Radiat. Iso, 2006, 64, 812-814.         [ Links ]

17 J. R. Zeevaart, W.K.A. Louw, E. Kilian and I. Cukrowski 99mTc labelled biguanide derivatives: chemical speciation modelling thereof and evaluation in vervets, submitted to J. Inorg. Biochem.         [ Links ]

18 R.M. Sanyal, P.C. Srivastava and B.K. Banerjee, J. Inorg. Nucl. Chem., 1975, 37, 343-347.         [ Links ]

19 R.D. Hancock and A.E. Martell, Chem. Rev., 1989, 89, 1875-1914.         [ Links ]

20 R.C. Mehrotra, Comprehensive Coordination Chemistry (G. Wilkinson, ed.), vol. 2, Pergamon Press, Elmsford, NY, USA, 1987, pp. 269-291.         [ Links ]

21 M. Goodgame and I. Hussian, Inorg. Chim. Acta, 1989, 160, 183-188.         [ Links ]

22 R.K. Ray and G.B. Kaufman, Inorg. Chim. Acta, 1990, 173, 207-214.         [ Links ]

23 R.K. Ray and G.B. Kaufman, Inorg. Chim. Acta, 1990, 174, 257-262.         [ Links ]

24 A.E. Martell and R.M. Smith, Critical Stability Constants, vol. 3, Plenum Press, New York, USA, 1977.         [ Links ]

25 A.E. Martell and R.M. Smith, Critical Stability Constants, vol. 1, Plenum Press, New York, USA, 1974.         [ Links ]



Received 5 November 2007
Revised 15 April 2008
Accepted 30 April 2008



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