Assessment of Benzydamine N-Oxidation Mediated by Flavin-Containing Monooxygenase in Different Regions of Rat Brain and Liver Using Microdialysis.

Kawaji, Akiko; Yamaguchi, Tomohiro; Tochino, Yoshihiro; Isobe, Masakazu; Takabatake, Eigo

doi:10.1248/bpb.22.1

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Liver Sampling1

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2003

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“…Subsequently, numerous reports have demonstrated that concurrent multiple-site microdialysis sampling is a useful tool for pharmacokinetic and drug metabolism studies in the liver [46][47][48][49][50][51][52][53][54][55][56].…”

Section: Liver Samplingmentioning

confidence: 99%

Assaying protein unbound drugs using microdialysis techniques

Tsai

2003

Journal of Chromatography B

115

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Section: Liver Samplingmentioning

confidence: 99%

Assaying protein unbound drugs using microdialysis techniques

Tsai

2003

Journal of Chromatography B

115

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Benzydamine <i>N</i>-Oxygenation as a Measure of Flavin-Containing Monooxygenase Activity

Yeung

Rettie

Cytochrome P450 Protocols

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Benzydamine is a nonsteroidal anti-inflammatory drug that undergoes flavin-containing monooxygenase (FMO)-dependent metabolism to a stable N-oxide. This metabolite can be quantified with high specificity and sensitivity by using a simple reverse-phase high-performance liquid chromatography (HPLC) assay with fluorescence detection. Studies with recombinant FMO enzymes demonstrate that FMOI and FMO3 are the primary catalysts of benzydamine N-oxygenation, with minimal contributions from cytochrome P450 enzymes. Investigations conducted with human liver microsomes confirm that FMO3, in large part, is responsible for benzydamine N-oxide formation in this tissue. These features render benzydamine a useful in vitro probe for FMO activity in a wide range of tissues and cell types. In addition, benzydamine appears to be a suitable in vivo probe for human liver FMO3. This chapter provides a detailed account of the experimental protocol for determining rates of formation of benzydamine N-oxide by FMO-containing enzyme fractions.

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Assessment of Benzydamine N-Oxidation Mediated by Flavin-Containing Monooxygenase in Different Regions of Rat Brain and Liver Using Microdialysis.

Cited by 2 publications

References 1 publication

Assaying protein unbound drugs using microdialysis techniques

Assaying protein unbound drugs using microdialysis techniques

Benzydamine <i>N</i>-Oxygenation as a Measure of Flavin-Containing Monooxygenase Activity

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