Biotransformation of proterguride in the perfused rat liver.

The metabolic pathway of the dopaminagonistic ergoline derivative, proterguride, was studied in vitro in a rat liver perfusion experiment. Metabolites were isolated by preparative HPLC and identified by MS and NMR analyses. In total, seven compounds could be identified. The metabolic steps involved in the biodegradation of proterguride are N-deethylation, N-oxidation, hydroxylation, and/or dehydrogenation and oxidative cleavage of the indole ring.