Angiotensin II Receptor Blockers Inhibit the Generation of Epoxyeicosatrienoic Acid from Arachidonic Acid in Recombinant CYP 2C9, CYP 2J2 and Human Liver Microsomes
Cytochrome P450 ( CYP ) 2C9, CYP 2C8 and CYP 2J2 enzymes, which metabolize arachidonic acid (AA) to epoxyeicosatrienoic acids, have cardioprotective effects including anti‐inflammation and vasodilation. We have recently shown that some angiotensin II receptor blockers ( ARB s) may inhibit AA metabol...
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Veröffentlicht in: | Basic & clinical pharmacology & toxicology 2017-10, Vol.121 (4), p.239-245 |
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Hauptverfasser: | , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | Cytochrome P450 (
CYP
) 2C9,
CYP
2C8 and
CYP
2J2 enzymes, which metabolize arachidonic acid (AA) to epoxyeicosatrienoic acids, have cardioprotective effects including anti‐inflammation and vasodilation. We have recently shown that some angiotensin
II
receptor blockers (
ARB
s) may inhibit
AA
metabolism via
CYP
2C8. Using recombinant
CYP
2C9,
CYP
2J2 and human liver microsomes (
HLM
s), the aim was now to compare the ability of six different clinically used
ARB
s to inhibit
AA
metabolism
in vitro
. The rank order of the
ARB
s for the 50% inhibitory concentration (
IC
50
) of
AA
metabolism was losartan |
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ISSN: | 1742-7835 1742-7843 |
DOI: | 10.1111/bcpt.12789 |