Nicardipine and Nifedipine Inhibit Fatty Acid Desaturases in Rat Liver Microsomes
Author(s) -
Hiroshi Kawashima,
Kengo Akimoto,
Saeree Jareonkitmongkol,
Norifumi Shirasaka,
Sakayu Shimizu
Publication year - 1996
Publication title -
bioscience biotechnology and biochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.509
H-Index - 116
eISSN - 1347-6947
pISSN - 0916-8451
DOI - 10.1271/bbb.60.1672
Subject(s) - nicardipine , nifedipine , cinnarizine , verapamil , microsome , pharmacology , chemistry , diltiazem , flunarizine , biochemistry , biology , calcium , in vitro , organic chemistry
Nicardipine and nifedipine, Ca channel blockers, inhibited rat liver microsomal desaturases, though verapamil, methoxyverapamil, cinnarizine, flunarizine, and diltiazem did not. However, nicardipine and nefidipine apparently did not inhibit the fungal desaturation in Mortierella alpina 1S-4. Nicardipine inhibited rat liver microsomal delta 5 desaturase specifically (50% inhibitory concentration. 170 microM), and nifedipine inhibited delta 6 desaturase specifically (78 microM). The inhibition by nicardipine and nifedipine is uncompetitive, the Ki values for delta 5 and delta 6 desaturases being 62 and 44 microM, respectively.
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