Aim: To study the metabolic pathway of chiral clausenamide in the rat and understand its stereoselectivity.
Methods: The urine, feces and blood of rat were gathered after the drug was administered, the known metabolites were analyzed by HPLC-DAD and one unknown metabolite was elucidated by using LC-MS analysis. Metabolic stereoselectivity was determined by comparing the metabolic results of (+)- and (-)-clausenamide.
Results: Six known metabolites were determined and one unknown metabolite was elucidated as N-demethylclausenamide. The metabolic stereoselectivity was shown distinctly.
Conclusion: Chiral clausenamide was mainly metabolized by hydroxylation in liver and the biotransformation exhibited pronounced substrate stereoselectivity.