Metabolism of ¹⁴C-thymoxamine in rat and man

Abstract

1. After oral administration of ¹⁴C-thymoxamine to rat and man the total ¹⁴C excreted in urine and faeces was determined.

2. Six metabolites were isolated from the excreta of man and rat by chemical extraction and identified by g.l.c.-mass spectral analyses.

3. Two other metabolites, highly polar and resistant to enzymic hydrolysis, were isolated by extraction on XAD₂ resin and h.p.l.c. analysis. These two metabolites were identified by n.m.r. and by mass spectrometry in the fast atomic bombardment mode.

4. These two major metabolites of thymoxamine in man and rat have been identified and characterised as the sulphate conjugates of desacetyl-thymoxamine and N-monodesmethyl-desacetyl-thymoxamine.