Nicardipine and nifedipine inhibit fatty acid desaturases in rat liver microsomes. 1996

H Kawashima, and K Akimoto, and S Jareonkitmongkol, and N Shirasaka, and S Shimizu
Department of Agricultural Chemistry, Faculty of Agriculture, Kyoto University, Japan.

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.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D008862 Microsomes, Liver Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough. Liver Microsomes,Liver Microsome,Microsome, Liver
D009090 Mucorales An order of zygomycetous fungi, usually saprophytic, causing damage to food in storage, but which may cause respiratory infection or MUCORMYCOSIS in persons suffering from other debilitating diseases. Mucoraceae,Thamnidiaceae
D009529 Nicardipine A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. Antagonil,Cardene,Cardene I.V.,Cardene SR,Dagan,Flusemide,Lecibral,Lincil,Loxen,Lucenfal,Nicardipine Hydrochloride,Nicardipine LA,Nicardipino Ratiopharm,Nicardipino Seid,Perdipine,Ridene,Vasonase,Y-93,Hydrochloride, Nicardipine,LA, Nicardipine,Y 93,Y93
D009543 Nifedipine A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. Adalat,BAY-a-1040,Bay-1040,Cordipin,Cordipine,Corinfar,Fenigidin,Korinfar,Nifangin,Nifedipine Monohydrochloride,Nifedipine-GTIS,Procardia,Procardia XL,Vascard,BAY a 1040,BAYa1040,Bay 1040,Bay1040,Monohydrochloride, Nifedipine,Nifedipine GTIS
D002121 Calcium Channel Blockers A class of drugs that act by selective inhibition of calcium influx through cellular membranes. Calcium Antagonists, Exogenous,Calcium Blockaders, Exogenous,Calcium Channel Antagonist,Calcium Channel Blocker,Calcium Channel Blocking Drug,Calcium Inhibitors, Exogenous,Channel Blockers, Calcium,Exogenous Calcium Blockader,Exogenous Calcium Inhibitor,Calcium Channel Antagonists,Calcium Channel Blocking Drugs,Exogenous Calcium Antagonists,Exogenous Calcium Blockaders,Exogenous Calcium Inhibitors,Antagonist, Calcium Channel,Antagonists, Calcium Channel,Antagonists, Exogenous Calcium,Blockader, Exogenous Calcium,Blocker, Calcium Channel,Blockers, Calcium Channel,Calcium Blockader, Exogenous,Calcium Inhibitor, Exogenous,Channel Antagonist, Calcium,Channel Blocker, Calcium,Inhibitor, Exogenous Calcium
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D000090943 Delta-5 Fatty Acid Desaturase A fatty acid desaturase that is a rate-limiting enzyme for the conversion from dihomo-gamma-linolenic acid and EICOSATETRAENOATE (ETA) in the synthesis of ARACHIDONIC ACID and EICOSAPENTAENOATE (EPA). It is also involved in the biosynthesis of unsaturated fatty acids from the polyunsaturated fatty acids (PUFA), LINOLEIC ACID (LA), and ALPHA LINOLENIC ACID (ALA) precursors and plays an important role in the metabolism of inflammatory lipids including PROSTAGLANDIN E2. Delta 5 Desaturase,Delta-5-FADase,Fatty Acid Delta-5-Desaturase,5 Desaturase, Delta,Acid Delta-5-Desaturase, Fatty,Delta 5 FADase,Delta-5-Desaturase, Fatty Acid,Desaturase, Delta 5,Fatty Acid Delta 5 Desaturase
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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