Evaluation of 99mTc-labeled iminodiacetic acid derivatives of substituted 2-aminopyrroles as hepatobiliary imaging agents in rats II.
The synthesis and biodistribution properties of 99mTc-labeled 5-substituted N-(3-cyano-4-methyl-2-pyrrylcarbamoylmethyl)iminodiacetic acids and a similar series of N1-methyl analogs are described. These compounds were compared with 99mTc-labeled N-(2,6-dimethylphenylcarbamoylmethyl)iminodiacetic acid for hepatobiliary activity in the rat. The effects of structural modifications on biological activity are also reported.
Determination of stability constants and acute toxicity of potential hepatotropic gadolinium complexes
Due to their high specificity for the hepatobiliary system, iminodiacetic acid derivatives are known to form a class of hepatobiliary agents. In this paper we present new hepatotropic gadolinium complexes to be used as potential MRI contrast agents. Derivatives of N-(2-phenylamine-2-oxoethyl)iminodiacetic acid are introduced as ligands into such complexes. In this way, we hope to achieve a valuable diagnostic tool for investigating of pathological changes in the liver. Stability constants of complexes were determined by potentiometric titration in 0.1 mol L-1 NaNO3 solution at 20.0 ± 0.1OC. Stability and selectivity constants were also determined for endogenous metal ions such as Cu2+, Ca2+, and Zn2+ with the use of SUPERQUAD computer program. Acute toxicity of new gadolinium complexes was assessed in mice and histopathology examinations were carried out.
Mikiciuk-Olasik, Elzbieta,Wojewoda, Emilia,Bilichowski, Ireneusz,Witczak, Malgorzata,Karwowski, Boleslaw,Wagrowska-Danilewicz, Malgorzata,Stasikowska, Olga
p. 119 - 127
(2011/08/05)
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