Radiopharmaceuticals. 16. Halogenated dopamine analogs. Synthesis and radiolabeling of 6-iododopamine and tissue distribution studies in animals

Abstract

A simple halogenated derivative of dopamine, 6-iododopamine (1), was synthesized using 2 different methods. These synthetic sequences were applied to the radiolabeling of 1 with "C, 131I and 123I. The tissue distribution of 1 in mice, dogs and rats was determined. The ratio of radioactivity (%/g) in the adrenal medulla-kidney in dogs increases from 3.45 at 2 h postinjection of 33.3 at 24 h postinjection. Thyroid uptakes in mice, dogs and rats show that in vivo deiodination of 1 is not significant.