Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Application of LC-NMR for Characterization of Rat Urinary Metabolites of Zonampanel Monohydrate (YM872)
Kin-ya SohdaTsuyoshi MinematsuTadashi HashimotoKen-ichi SuzumuraMasashi FunatsuKatsuhiro SuzukiHarumitsu ImaiTakashi UsuiHidetaka Kamimura
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2004 Volume 52 Issue 11 Pages 1322-1325


Zonampanel monohydrate (YM872) has a potent and selective antagonistic effect on the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor. Metabolic fingerprinting in rat urine after a single intravenous administration of 14C-labeled YM872 (14C-YM872) revealed the presence of two metabolites, R1 and R2. The two metabolites were semi-purified by preparative HPLC from rat urine after a single intravenous administration of non-labeled YM872, and their structures were elucidated by various instrumental analyses involving LC-NMR. The results showed that R1 and R2 have a hydroxyamino group and an amino group at the C-7 position of the quinoxalinedione skeleton, respectively. Therefore, the proposed metabolic pathway of YM872 in rats involves the reduction of the nitro group to a hydroxyamino group and then subsequent reduction to an amino group.

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© 2004 The Pharmaceutical Society of Japan
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