Nicardipine and nifedipine inhibit fatty acid desaturases in rat liver microsomes.
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.
Kawashima
H
H
Department of Agricultural Chemistry, Faculty of Agriculture, Kyoto University, Japan.
Akimoto
K
K
Jareonkitmongkol
S
S
Shirasaka
N
N
Shimizu
S
S
D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology*; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D000090943:Delta-5 Fatty Acid Desaturase; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D044943:Fatty Acid Desaturases / Q000037:antagonists & inhibitors*; D007700:Kinetics; D016014:Linear Models; D050602:Linoleoyl-CoA Desaturase; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D009090:Mucorales / Q000187:drug effects / Q000201:enzymology; D009529:Nicardipine / Q000494:pharmacology*; D009543:Nifedipine / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar
D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D000090943:Delta-5 Fatty Acid Desaturase; D004791:Enzyme Inhibitors; D009529:Nicardipine; D044943:Fatty Acid Desaturases; D050602:Linoleoyl-CoA Desaturase; D009543:Nifedipine