Bogatskiĭ A V, Golovenko N Ia, Karaseva T L
Vopr Med Khim. 1977 Jan-Feb(1):92-6.
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.
以每千克体重100毫克的剂量对大鼠进行腹腔注射后，硝西泮（莫加东、优诺克汀）会发生酶促还原，随后进行乙酰化。在细胞碎片和细胞核中，以及肝脏、肺、心脏和脑组织的线粒体、微粒体和可溶性部分中发现了硝西泮的衍生物。底物的还原发生在肝脏组织的可溶性和微粒体部分，乙酰化发生在肺和肝脏组织的线粒体中。硝西泮代谢物在心脏和脑组织的细胞器中分布相当均匀；这表明它们起源于其他组织中的器官，在那里发生还原和乙酰化过程。硝西泮及其衍生物能非常有效地穿透大脑；这种现象被认为对它们的药理活性至关重要。
