title: Metabolic fate of loxistatin in rat.
abstract: 1. The urinary and plasma metabolites of 14C-loxistatin, a new thiol protease inhibitor, were studied after oral administration to rats. 2. The major metabolites in urine were identified as loxistatin acid (M-1), a pharmacologically active form, and its hydroxy metabolites (M-4a and M-4b). These metabolites were also shown to be the major metabolites in plasma. 3. The inhibitory activity of the synthetic metabolite, M-4b, on papain was almost the same as that of loxistatin acid.
authors.affiliation: Research Center, Taisho Pharmaceutical Co., Ltd, Saitama, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Fukushima
authors.forename: M
authors.initials: M
authors.lastname: Arai
authors.forename: M
authors.initials: M
authors.lastname: Tamai
authors.forename: C
authors.initials: C
authors.lastname: Yokoo
authors.forename: M
authors.initials: M
authors.lastname: Murata
authors.forename: T
authors.initials: T
authors.lastname: Suwa
authors.forename: T
authors.initials: T
authors.lastname: Satoh
mesh_terms: D000284:Administration, Oral; D000818:Animals; D015853:Cysteine Proteinase Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D007930:Leucine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D010206:Papain / Q000037:antagonists & inhibitors; D011355:Prodrugs / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D015853:Cysteine Proteinase Inhibitors; D011355:Prodrugs; D010206:Papain; D007930:Leucine; C108192:aloxistatin