Reduction of nitrazepam by rat liver mitochondria

Blume, H.

Arzneimittel-Forschung 30(9): 1566-1571

1980


ISSN/ISBN: 0004-4172
PMID: 7193026
Document Number: 160610
Highly purified rat liver mitochondria are able to reduce nitro groups of organic compounds to primary amines. This reductase-activity is bound to mitochondrial inner membrane or its matrix. It has no plain substrate specificity whereas it will attack the various substrates at widely different rates [nitrazepam (Mogadan) 1.7 times faster than 4-nitrobenzoic acid]. The activity was markedly inhibited under aerobic conditions. The rate of nitrazepam reduction by rat liver mitochondria was about 1/3--1/4 the rate by microsomal fraction, provided that both preparations contained the same protein amounts. NADH was required as a cofactor, but the nitroreduction was also stimulated by some Krebs cycle intermediates, especially by alpha-ketoglutarate. The reaction was markedly inhibited by organic solvents, even by little volumes. DMSO and DMF are cancelling every activity.

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