Potential tissue-imaging agents: 23-(trimethyl[117mSn]stannyl)-24-nor-5α-cholan-3β-ol

Tin-117m-labeled 23-(trimethylstannyl)-24-nor-5 alpha-cholan-3 beta-ol (2) has been prepared by reaction of trimethyl [117mSn]tin lithium with 3 beta-acetoxy-23-bromo-24-nor-5 alpha-cholane (1). Tin-117m (2) shows pronounced adrenal uptake (2.5% injected dose) in female rats 1 day after injection. F...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1983-10, Vol.26 (10), p.1535-1537
Main Authors: KNAPP, F. F. JR, CALLAHAN, A. P, AMBROSE, K. R, FERREN, L. A, BUTLER, T. A, COFFEY, J. L
Format: Article
Language:English
Subjects:
Adrenal Glands - metabolism
Alicyclic compounds, terpenoids, prostaglandins, steroids
Animals
Chemistry
Cholanes - chemical synthesis
Cholanes - metabolism
Exact sciences and technology
Female
Indicators and Reagents
Kidney - metabolism
Kinetics
Liver - metabolism
Male
Mass Spectrometry
Organic chemistry
Ovary - metabolism
Preparations and properties
Radioisotopes
Radionuclide Imaging - methods
Rats
Spectrophotometry, Infrared
Steroids
Tissue Distribution
Trialkyltin Compounds - chemical synthesis
Trimethyltin Compounds - chemical synthesis
Trimethyltin Compounds - metabolism
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Summary:Tin-117m-labeled 23-(trimethylstannyl)-24-nor-5 alpha-cholan-3 beta-ol (2) has been prepared by reaction of trimethyl [117mSn]tin lithium with 3 beta-acetoxy-23-bromo-24-nor-5 alpha-cholane (1). Tin-117m (2) shows pronounced adrenal uptake (2.5% injected dose) in female rats 1 day after injection. Furthermore, the adrenal to liver (9.1:1) and adrenal to blood (33.7:1) ratios are high after this period. The absorbed radiation dose values from [117mSn]2 to human organs have also been estimated by using rat tissue distribution and excretion data. [117mSn]2 is the first reported tissue-specific organic radiopharmaceutical labeled with this nuclide and may have potential as an adrenal imaging agent.
ISSN:0022-2623
1520-4804