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

✍ Scribed by D. A. Constable; L. G. Dring; J. R. Jones

• Publisher: John Wiley and Sons
• Year: 1990
• Tongue: French
• Weight: 293 KB
• Volume: 28
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.2580280705

✦ Synopsis

Abstract

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.