【摘要】：尿苷二磷酸-葡萄糖醛酸轉(zhuǎn)移酶(UDP-glucuronosyltransferases,UGT)為II相代謝酶,可催化某些藥物與葡萄糖醛酸的結(jié)合反應(yīng)。腦組織UGT表達(dá)廣泛,但表達(dá)量與活性低于肝臟;腦內(nèi)UGT同樣可被誘導(dǎo)或抑制,從而影響藥物腦組織的分布和水平;并與細(xì)胞色素P450(cytochrome P450,CYP)、轉(zhuǎn)運蛋白密切配合,共同參與、影響某些藥物的腦內(nèi)代謝動力學(xué)過程;多種藥物以葡萄糖醛酸化產(chǎn)物形式跨越血腦屏障,或以原形在腦內(nèi)直接生成葡萄糖醛酸化產(chǎn)物,從而發(fā)揮各自藥理作用。本文簡述了UGT腦內(nèi)亞型、分布、誘導(dǎo)、抑制,與CYP和轉(zhuǎn)運蛋白的相互作用,舉例說明某些藥物腦內(nèi)葡萄糖醛酸化過程,旨在為靶向中樞神經(jīng)系統(tǒng)藥物的設(shè)計、應(yīng)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.
【作者單位】： 中國醫(yī)學(xué)科學(xué)院北京協(xié)和醫(yī)學(xué)院藥物研究所藥物代謝室創(chuàng)新藥物非臨床藥代/藥效北京市重點實驗室活性物質(zhì)發(fā)現(xiàn)與適藥化研究北京市重點實驗室;
【基金】：十二五新藥創(chuàng)制重大專項資助項目(2012ZX09301002-001-007,2012ZX09301002-006,2012ZX09103-101-001)
【分類號】：R96

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