Synthesis of both ¹⁴C‐ and ³H‐ labelled trospectomycin and the assessment of their utility in biological studies

Abstract

SUMMARYThree radiolabelled forms of trospectomycin (6'-n-propylspectinomycin sulphate hydrate) have been synthesised, namely [8'-''C]-, [6',7'-3H]-, and [5',6',7'-3H]-trospectomycin. Although all three forms of the drug are metabolically stable and therefore suitable for use in animal studies the I4C compound is produced in poor yield as is the [6',7'-3H]trospectomycin. On the other hand, the [5',6',7'-3H]-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.