title: Metabolite characterization of a novel sedative drug, remimazolam in human plasma and urine using ultra high-performance liquid chromatography coupled with synapt high-definition mass spectrometry.
abstract: Remimazolam is a new chemical entity belonging to the benzodiazepine class of sedative drugs, which shows faster-acting onset and recovery than currently available short-acting sedatives. In the present study, ultra high performance liquid chromatography with synapt high-definition mass spectrometry method combined with MassLynx software was established to characterize metabolites of remimazolam in human plasma and urine. In total, 5 human metabolites were detected, including 3 phase I and 2 phase II metabolites. There was no novel human metabolite detected compared to that in rat. Hydrolysis, glucuronidation and oxidation were the major metabolic reactions. To our knowledge, this is the first report of the human metabolic profile of remimazolam.
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Nanchang University, Nanchang 330006, China. Electronic address: zyyiva@163.com.
authors.forename: Ying
authors.initials: Y
authors.lastname: Zhou
authors.affiliation: Clinical Pharmacology Research Center, Peking Union Medical College Hospital, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, 100730 China.
authors.forename: Pei
authors.initials: P
authors.lastname: Hu
authors.affiliation: Clinical Pharmacology Research Center, Peking Union Medical College Hospital, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, 100730 China. Electronic address: ppbank.9@163.com.
authors.forename: Ji
authors.initials: J
authors.lastname: Jiang
mesh_terms: D000818:Animals; D001569:Benzodiazepines / Q000097:blood* / Q000652:urine*; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D004311:Double-Blind Method; D006801:Humans; D006993:Hypnotics and Sedatives / Q000097:blood* / Q000652:urine*; D051381:Rats; D012984:Software; D053719:Tandem Mass Spectrometry / Q000379:methods
chemical_list: D006993:Hypnotics and Sedatives; D001569:Benzodiazepines; C522201:remimazolam
keywords: Mass defect filter; Metabolites; Remimazolam; UPLC/SYNAPT-HDMS