16 alpha-Iodo-testosterone: chemical synthesis and evaluation as a potential radiopharmaceutical.

Abstract

The chemical synthesis and characterization, including 1H NMR, of 16 alpha-iodo-androstenedione and 16 alpha-iodo-testosterone are described. Each has been synthesized with 125I and tested in rats in vivo for accumulation in androgen dependent tissues over a 24 hr time course. Neither compound was accumulated in prostate against the blood gradient of normal or 24 hr castrate animals. The metabolism, subcellular distribution and binding of 16 alpha-[125I]iodo-testosterone to protein in prostate has also been examined. By comparison with data obtained after the administration of [3H]testosterone we conclude that the failure of this iodinated androgen to accumulate in androgen dependent tissues arises because of its low binding affinity for receptor protein.

Cite this paper

@article{Symes198516AC, title={16 alpha-Iodo-testosterone: chemical synthesis and evaluation as a potential radiopharmaceutical.}, author={E K Symes and Walter F Coulson and R Duncan Farrant and E. J. G. Milroy}, journal={Biochemical pharmacology}, year={1985}, volume={34 17}, pages={3173-8} }