| Effects of Diazepam,Phenobarbital,Propranolol,and Cimetidine on Diazepam Oxidizing Isoenzymes in Rat Liver Microsomes |
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| 作者姓名： | 匡唐永 楼雅卿 赵立安 |
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| 作者单位： | 北京医科大学药理系药物代谢研究室 |
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| 摘 要： | 研究地西泮、苯巴比妥、普萘洛尔和西咪替丁对地西泮氧化代谢的影响及其药酶蛋白的初步分析，应用ＨＰＬＣ，ＳＤＳ聚丙烯酰胺凝胶电泳和薄层扫描测定地西泮及其代谢物，并对大鼠肝微粒体和酶蛋白进行分离和含量测定。结果表明地西泮、普萘洛尔和西咪替丁使肝微粒体中Ｐ４５０含量明显降低。地西泮和普萘洛尔明显抑制地西泮Ｃ３羟化活性，大剂量普萘洛尔尚能抑制地西泮Ｎ脱甲基。苯巴比妥明显诱导Ｐ４５０生成，增强地西泮Ｎ脱甲基和Ｃ３羟化酶活性及分子量为５１，０００和５９，０００的电泳蛋白带，而地西泮、普萘洛尔则呈抑制作用。并发现，地西泮Ｎ脱甲基酶活性和分子量为５９，０００蛋白含量呈线性相关（Ｐ＜０．０５），而Ｃ３羟化酶活性则与５１，０００蛋白含量呈线性相关（Ｐ＜０．０１）。因此地西泮Ｃ３羟化代谢可能与５１，０００的Ｐ４５０酶蛋白有关，而Ｎ脱甲基代谢则可能与５９，０００的Ｐ４５０酶蛋白有关。
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| 关 键 词： | 地西泮 去甲西泮 替马西泮 药酶诱导剂 药酶抑制剂 N-脱甲基化酶 C_3-羟化活性酶 细胞色素P-450 大鼠肝微粒体 |
Effects of Diazepam, Phenobarbital, Propranolol, and Ci metidine on Diazepam Oxidizing Isoenzymes in Rat Liver Microsomes |
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| Tang Yong Kuang,Ya Qing LouCorrespondence to Prof. Ya Qing Lou. and Li An Zhao Group of Drug Metabolism and Pharmacokinetics.Effects of Diazepam,Phenobarbital,Propranolol,and Cimetidine on Diazepam Oxidizing Isoenzymes in Rat Liver Microsomes[J].Journal of Chinese Pharmaceutical Sciences,1997(2). |
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| Authors: | Tang Yong Kuang Ya Qing LouCorrespondence to Prof Ya Qing Lou and Li An Zhao Group of Drug Metabolism and Pharmacokinetics |
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| Institution: | Tang Yong Kuang,Ya Qing LouCorrespondence to Prof. Ya Qing Lou. and Li An Zhao Group of Drug Metabolism and Pharmacokinetics,Department of Pharmacology,Beijing Medical University,Beijing 100083 Received October 14,1996, Accepted February 20 |
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| Abstract: | |
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| Keywords: | Diazepam Nordiazepam Temazepam Demethylase Hydroxylase Cyto chrome P 450 Liver microsomes |
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