Iodothyronine, radioiodination

In rats equilibrated with radioiodine-labelled T4 or T3 roughly half of the radioactivity appears as I- in the urine and the other half as free iodothyronines in the feces [12]. Treatment of the rats with 6-propyl-2-thiouracil (PTU) results in a marked decrease in urinary radioactivity and a reciprocal increase in fecal clearance [12]. Also, in humans, PTU has been shown to inhibit peripheral iodothyronine deiodination besides its well-known effect on thyroid hormone biosynthesis [13]. Compared with the rat, deiodination is an even more important pathway for the clearance of thyroid hormone in man as evidenced by the greater proportion undergoing urinary clearance [2]. Furthermore, estimation of iodothyronine turnover kinetics in humans has demonstrated that a major fraction of T4 disposal is accounted for by plasma production rates of T3 and rT3 [2,3],... 

PIO. Pind, K., Paper chromatographic determination of thyroid hormone (3,5,3 -tri-iodothyronine) in serum without radioiodine. Acta Endocrinol. (Copenhagen) 26, 263-272 (1957). 

Although radioiodinated antibodies have acceptable stability for in vitro applications, their in vivo stability is less ideal These tracers can act as substrates for the iodotransferase enzymes which are normally responsible for metabo lism of the thyroid hormones thyroxine and tri-iodothyronine which bear structural similarities. Although not present in the vascular circulation, these enzymes are widely distributed in many tissues and their action results in the intracellular release of the radionuclide which then either diffuses or is actively transported out of the cell and subsequently excreted in the urine. In order to try and increase the in vivo stability of antibodies labelled with radioiodine, alternative synthetic strategies have been pursued which result in molecules which are not substrates for the iodotransferases (11. 12). AU of these techniques are more complicated than the electrophilic substitution methods described above and require some synthetic chemistry in order to prepare the precursors which are not commercially available. 

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