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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

 

RESEARCH ARTICLE

 

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

 

 


ABSTRACT

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.

 

 

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

 

 

* To whom correspondence should be addressed. E-mail: jwagener@necsa.co.za

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