Disposition and metabolism of (2S,3S,4R)-N′′-cyano-N-(6-amino-3,4-dihydro-3-hydroxy-2-methyl-2-dimethoxy methyl-2H-benzopyran-4-yl)-N′-benzylguanidine, a novel neuroprotective agent for ischemia-reperfusion damage, in rats

Title
Disposition and metabolism of (2S,3S,4R)-N′′-cyano-N-(6-amino-3,4-dihydro-3-hydroxy-2-methyl-2-dimethoxy methyl-2H-benzopyran-4-yl)-N′-benzylguanidine, a novel neuroprotective agent for ischemia-reperfusion damage, in rats
Author
유혜현
Keywords
KR31378; pharmacokinetics; distribution; metabolism; excretion; ( 2S,3S,4R)-N'- cyano- N(6-amino-3,4-dihydro-3-hydroxy-2; methyl-2-dimethoxy methyl-2H-benzopyran-4-yl)-N'- benzylguanidine
Issue Date
2007-05
Publisher
TAYLOR & FRANCIS LTD
Citation
XENOBIOTICA, v. 37, No. 5, Page. 534-548
Abstract
The metabolism and disposition of KR31378 (a benzopyran derivative and a novel neuroprotective agent) were investigated following single oral or intravenous administration of [C-14]- KR31378 to rats. [C-14]- KR31378 was rapidly absorbed after oral dosing with an oral bioavailability of greater than 71%. The maximum plasma concentration and area under the curve of total radioactivity in rat plasma increased proportionally to the administered dose. KR31378 was distributed over all organs and tissues except for brain, eyeball and testis, and declined by first order kinetics up to 24 h after dosing. Excretion of the radioactivity was 29.5% of the dose in the urine and 58.5% in the feces within 2 days after oral administration. Biliary excretion of the radioactivity in bile duct-cannulated rats was about 66.0% for the first 24 h. KR31378 was extensively metabolized by ring hydroxylation, O-demethylation, oxidation and reduction with subsequent N-acetylation and O-glucuronide conjugation. N-acetylated conjugates (M2, M10, M11, M12, M14, and M15) were identified as the predominant metabolites in rats.
URI
https://www.tandfonline.com/doi/full/10.1080/00498250601188790http://repository.hanyang.ac.kr/handle/20.500.11754/106507
ISSN
0049-8254; 1366-5928
DOI
10.1080/00498250601188790
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COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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