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.

Evaluation of 99mTc-labeled iminodiacetic acid derivatives of substituted 2-aminopyrroles as hepatobiliary imaging agents. I.

N-(3-Cyano-4,5-dimethyl-2-pyrrylcarbamoylmethyl)iminodiacetic acid (IIa) and N-(3-cyano-4-methyl-5-benzyl-2-pyrrylcarbamoylmethyl)iminodiacetic acid (IIb) were synthesized, labeled with technetium 99m, and compared with 99mTc-labeled p-isopropylacetanilidoiminodiacetic acid (I) for hepatobiliary activity in rats. All three compounds showed similar clearance of radioactivity from the blood. Comparison of the amount of radioactivity in various organs 1 hr after injection showed no significant difference between I and IIb. Compound IIa showed significantly less radioactivity in the GI tract and a higher amount in the kidneys and bladder.