VOPROSY MEDITSINSKOI KHIMII (ISSN 0042-8809)

Distribution of nitrazepam and its metabolites in the subcellular fractions of several white rat organs

   
Bogatskii A.V., Golovenko N.Ia., Karaseva T.L.
PubMed Id: 857409
Year: 1977  Volume: 23  Issue: 1  Pages: 92-96
After intraperitoneal administration into rats at a dose of 100 mg per kg of body weight nitrazepame (mogadone, eunoktine) was enzymatically reduced with the subsequent acetylation. Derivatives of nitrazepame were found in cellular fragments and nuclei, in mitochondrial, microsomal and soluble fractions of liver, lungs, heart and brain tissues. Reduction of the substrate was shown to occur in soluble and microsomal fractions of liver tissue and acetylation--in mitochondria of lungs and liver tissue. Nitrazepame metabolites were quite uniformly distributed over cell organelles of heart and brain tissues; this suggests that they originate in the organs from other tissues, where the processes of reduction and acetylation take place. Nitrazepame and its derivatives penetrated into brain very effectively; this phenomenon is considered as an essential one for their pharmocological activity.
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Bogatskii, A. V., Golovenko, N. Ia., Karaseva, T. L. (1977). Distribution of nitrazepam and its metabolites in the subcellular fractions of several white rat organs. Voprosy Meditsinskoi Khimii, 23(1), 92-96.
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