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Updated: Jul 20, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
Effects of irsogladine on P450-isoform specific activities in human hepatic microsomes
Akio Nakamura1, Katsuhiko Tougou, Hiroko Kitazumi
1Research Laboratories, Nippon Shinyaku Co., Ltd., Kyoto, Japan. ak.nakamura@po.nippon-shinyaku.co.jp
Abstract:
The effects of irsogladine (CAS 84504-69-8) on P450-isoform specific activities in human hepatic microsomes were examined. Irsogladine had little effects on coumarin hydroxylation (CYP2A6), 7-benzyloxyresorufin O-debenzylation (CYP2B6), S-mephenytoin hydroxylation (CYP2C19), bufuralol hydroxylation (CYP2D6), chlorzoxazone hydroxylation (CYP2E1) and nifedipine oxidation (CYP3A4) at concentrations ranging from 10 to 50 pmol/L. However, it inhibited 7-ethoxyresorufin O-deethylation (CYP1A2) and tolbutamide hydroxylation (CYP2C9) with the Ki values of 276 and 156 micromol/L, respectively. This suggests that it is a weak inhibitor of these isoforms. Because the plasma concentrations of irsogladine in humans are much lower than these Ki values, it is unlikely that irsogladine causes drug interactions with other drugs.
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