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Synthesis of iodine‐125 labelled analogues of metyrapone and metyrapol
Author(s) -
Hays Sheryl J.,
Mangner Thomas J.
Publication year - 1983
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580201209
Subject(s) - chemistry , metyrapone , iodine , biodistribution , radiochemistry , enzyme , specific activity , organic chemistry , biochemistry , endocrinology , in vitro , medicine
Metyrapone (1) and metyrapol (2) are potent and reversible inhibitors of the 11β‐hydroxylase enzyme system of the adrenal cortex. Iodine‐125‐labelled derivatives of 1 and 2 were required for biodistribution studies. Utilizing a new exchange procedure these radioiodinated analogues were synthesized with radiochemical yields ranging from 24‐100% and specific activities as high as 1.72 Ci/mmol.