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A New Series of Tc-99m-Labeled Hepatobiliary Tracers: N'-Acyl- and N'-Sulfonyl Ethylenediamine-N,N-Diacetic Acids

Kyushu Cancer Center Research Institute and Kyushu University, Fukuoka, Japan

Correspondence: For reprints contact: Yoshiharu Karube, Kyushu Cancer Center Research Institute, Notame, Minamiku, Fukuoka, 815, Japan.

ABSTRACT

Various Tc-99m-labeled N'-substituted derivatives of ethylenediamine-N,N-diacetic acid (EDDA) are evaluated as hepatobiliary imaging agents. N'-substituted aromatic acyl and aromatic sulfonyl derivatives of EDDA, labeled with Tc-99m, were administered to rabbits and golden hamsters, and the distribution indicated clearance by the hepatobiliary system. N'-aromatic sulfonyl EDDAs were labeled with Tc-99m by the SnCl₂ method with more than 99% yield. Clearance of Tc-99m-p-toluenesulfonyl EDDA from the blood and the liver was as rapid as that of Tc-99m N-(2,6-diethylphenylcarbamoylmethyl)iminodiacetic acid (Tc-99m diethyl IDA). Substitution of a bulky group at the aromatic ring in Tc-99m benzene-sulfonyl EDDA lowered urinary excretion. It is concluded that the sulfonyl EDDAs provide a fruitful source for Tc-99m-labeled hepatobiliary radiopharmaceuticals.