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Preparation of a Chemically Characterized ^99mTc-Penicillamine Complex

Faculty of Pharmaceutical Sciences and School of Medicine, Kyoto University, Kyoto, Japan

Correspondence: For reprints contact: A. Yokoyama, Faculty of Pharmaceutical Sciences, Kyoto University, Shimoadachi-cho, Yoshida, Sakyo-ku, Kyoto, Japan 606.

ABSTRACT

In the reaction labeling penicillamine with ^99mTc, several different chemical states of ^99mTc were observed to occur with slight changes in the labeling conditions, such as the concentrations of penicillamine, ^99mTcO₄^-, stannous chloride, and hydrogen ion. We have studied the effects of these conditions on the formation of the monomer complex that we call Complex I, in which ^99mTc is coordinated with the penicillamine as ^99mTcO^+s. Our approach is based on the thesis that Complex I formation competes with ^99mTcO⁺² hydrolysis, which leads to other ^99mTc complexes. On this basis, the specific labeling conditions for Complex I formation have been established. Highly reproducible in vivo behavior in mice and rats was obtained with this chemically controlled Complex I.