药物的葡萄糖醛酸化与脑内过程
发布时间：2019-01-02 13:16
【摘要】：尿苷二磷酸-葡萄糖醛酸转移酶(UDP-glucuronosyltransferases,UGT)为II相代谢酶,可催化某些药物与葡萄糖醛酸的结合反应。脑组织UGT表达广泛,但表达量与活性低于肝脏;脑内UGT同样可被诱导或抑制,从而影响药物脑组织的分布和水平;并与细胞色素P450(cytochrome P450,CYP)、转运蛋白密切配合,共同参与、影响某些药物的脑内代谢动力学过程;多种药物以葡萄糖醛酸化产物形式跨越血脑屏障,或以原形在脑内直接生成葡萄糖醛酸化产物,从而发挥各自药理作用。本文简述了UGT脑内亚型、分布、诱导、抑制,与CYP和转运蛋白的相互作用,举例说明某些药物脑内葡萄糖醛酸化过程,旨在为靶向中枢神经系统药物的设计、应用提供研究思路。
[Abstract]:Uridine diphosphate glucuronyltransferase (UDP-glucuronosyltransferases,UGT) is a metabolic enzyme in II phase and can catalyze the binding reaction of some drugs with glucuronic acid. The expression of UGT in brain tissue is widespread, but the expression and activity are lower than that in liver, and UGT in brain can also be induced or inhibited, thus affecting the distribution and level of drug brain tissue. It also works closely with cytochrome P450 (cytochrome P450 CYP) and transporter to affect the metabolic dynamics of some drugs. Many drugs cross the blood-brain barrier in the form of glucuronide products or produce glucuronide products directly in the brain in the original form, thus exerting their respective pharmacological effects. In this paper, the subtype, distribution, induction, inhibition and interaction with CYP and transporter of UGT are briefly described. The process of glucuronation in the brain of some drugs is illustrated for the purpose of designing targeted drugs in the central nervous system (CNS). Application provides research ideas.
【作者单位】： 中国医学科学院北京协和医学院药物研究所药物代谢室创新药物非临床药代/药效北京市重点实验室活性物质发现与适药化研究北京市重点实验室;
【基金】：十二五新药创制重大专项资助项目(2012ZX09301002-001-007,2012ZX09301002-006,2012ZX09103-101-001)
【分类号】：R96
[Abstract]:Uridine diphosphate glucuronyltransferase (UDP-glucuronosyltransferases,UGT) is a metabolic enzyme in II phase and can catalyze the binding reaction of some drugs with glucuronic acid. The expression of UGT in brain tissue is widespread, but the expression and activity are lower than that in liver, and UGT in brain can also be induced or inhibited, thus affecting the distribution and level of drug brain tissue. It also works closely with cytochrome P450 (cytochrome P450 CYP) and transporter to affect the metabolic dynamics of some drugs. Many drugs cross the blood-brain barrier in the form of glucuronide products or produce glucuronide products directly in the brain in the original form, thus exerting their respective pharmacological effects. In this paper, the subtype, distribution, induction, inhibition and interaction with CYP and transporter of UGT are briefly described. The process of glucuronation in the brain of some drugs is illustrated for the purpose of designing targeted drugs in the central nervous system (CNS). Application provides research ideas.
【作者单位】： 中国医学科学院北京协和医学院药物研究所药物代谢室创新药物非临床药代/药效北京市重点实验室活性物质发现与适药化研究北京市重点实验室;
【基金】：十二五新药创制重大专项资助项目(2012ZX09301002-001-007,2012ZX09301002-006,2012ZX09103-101-001)
【分类号】：R96
【相似文献】
相关期刊论文 前10条
1 景];;葡萄糖醛酸[J];山西医学杂志;1962年03期
2 陈亚坤,李新,曾苏;N~+-葡萄糖醛酸缀合反应的物种差异[J];中国现代应用药学;2004年03期
3 ;葡萄糖醛酸，
本文编号：2398538
本文链接：https://www.wllwen.com/yixuelunwen/yiyaoxuelunwen/2398538.html
最近更新
教材专著
