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Nicardipine and Nifedipine Inhibit Fatty Acid Desaturases in Rat Liver Microsomes
Abstract:Nicardipine and nifedipine, Ca channel blockers, inhibited rat liver microsomal desaturases, though verapamil, methoxyverapamil, cinnarizine, flunarizine, and diltiazem did not. However, nicardipine and nifedipine apparently did not inhibit the fungal desaturation in Mortierella alpina 1S-4. Nicardipine inhibited rat liver microsomal Δ5 desaturase specifically (50% inhibitory concentration, 170 μm), and nifedipine inhibited Δ6 desaturase specifically (78 μm). The inhibition by nicardipine and nifedipine is uncompetitive, the Ki values for Δ5 and Δ6 desaturases being 62 and 44 μm, respectively.
Keywords:nicardipine  nifedipine  desaturase  polyunsaturated fatty acid  Ca channel blocker
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