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Synthesis of both 14 C‐ and 3 H‐ labelled trospectomycin and the assessment of their utility in biological studies
Author(s) -
Constable D. A.,
Dring L. G.,
Jones J. R.
Publication year - 1990
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.2580280705
Subject(s) - chemistry , urine , yield (engineering) , radiochemistry , carbon 14 , chemical synthesis , stereochemistry , chromatography , biochemistry , in vitro , materials science , metallurgy , physics , quantum mechanics
Three radiolabelled forms of trospectomycin (6′‐n‐propylspectinomycin sulphate hydrate) have been synthesised, namely [8′‐ 14 C]‐, [6′,7′‐ 3 H]‐, and [5′,6′,7′‐ 3 H]‐trospectomycin. Although all three forms of the drug are metabolically stable and therefore suitable for use in animal studies the 14 C compound is produced in poor yield as is the [6′,7′‐ 3 H]trospectomycin. On the other hand, the [5′,6′,7′‐ 3 H]‐form is produced in good yield and appears to be the labelled form of choice. Following subcutaneous administration of any of the labelled forms to rats, more than 50% of the dose was excreted in the urine as unchanged drug during the first 6h after dosing. Approximately 80% and 10% of the dose appeared in the urine and faeces respectively after 6 days.