L-Demethyl Phencynonate Hydrochloride

Levophencynonate is an anticholinergic agent which can prevent acute motion sickness with an efficacy similar to scopolamine.It will take effect by competitive binding to central muscarinic acetylcholine receptors.Previously, there was only one investigation about metabolites of phencynonate in rats and ten metabolites have been found.A HPLC/Triple TOF MS method was established and successfully applied to investigate the in vivo metabolites of levophencynonate after a 2 mg levophencynonate hydrochloride tablet was administered to healthy volunteers.A total of 13 metabolites were found in human specimens, including six from plasma and all of 13 from urine.The metabolites consisted of phase I and phase II products, including demethylation (M1), demethylation/oxidation (M2, M3, M4, and M5), demethylation/methylene to ketone (M6, M7), oxidation (M8, M9), desaturation (M10), demethylation/desaturation (M11), di-oxidation (M12), and oxidation/glucuronidation (M13) metabolites.Products of demethylation (M1), demethylation/desaturation (M11), and oxidation/glucuronidation (M13) were the main metabolites with higher intensity than the others.These findings would provide an important basis for the clin. application and further study of levophencynonate.In addition to the feasibility of the HPLC/Triple TOF MS approach for rapid and reliable characterization of metabolites, the identifications of precise structures of these metabolites need to be confirmed by other techniques, such as ¹H and ¹³C NMR, and in order to elucidate a more detailed metabolic profile of levophencynonate.