Article(id=1236334170478276692, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236334167978472434, articleNumber=null, orderNo=null, doi=null, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=null, receivedDateStr=null, revisedDate=null, revisedDateStr=null, acceptedDate=1666627200000, acceptedDateStr=2022-10-25, onlineDate=1772694636220, onlineDateStr=2026-03-05, pubDate=1689350400000, pubDateStr=2023-07-15, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1772694636220, onlineIssueDateStr=2026-03-05, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1772694636220, creator=13701087609, updateTime=1772694636220, updator=13701087609, issue=Issue{id=1236334167978472434, tenantId=1146029695717560320, journalId=1235980733773295621, year='2023', volume='32', issue='13', pageStart='1281', pageEnd='1384', issueExtLink='null', onlineDate='null', pubDate='null', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=0, articleOrder=1, issueType=-1, specialIssue=null, createTime=1772694635624, creator=13701087609, updateTime=1772696111905, updator=13701087609, preIssue=null, nextIssue=null, ext={EN=IssueExt(id=1236340360004292707, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236334167978472434, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1236340360004292708, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236334167978472434, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null}, startPage=1351, endPage=1357, ext={EN=ArticleExt(id=1236334170805432431, articleId=1236334170478276692, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Research progress of the mechanism, metabolism and distribution of vigabatrin, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=

The antiepileptic drug vigabatrin (VGB) is a selective and irreversible inhibitor of γ-aminobutyric acid transaminase, which can inhibit the abnormal electrical activity in brain via increasing the concentration of inhibitory neurotransmitter γ-aminobutyric acid (GABA). The clinical indications of VGB include infantile spasms and refractory partial seizure epilepsy, acting as a single treatment or an adjuvant treatment, respectively. Visual field loss is the main adverse reaction of VGB that limits its clinical application. Increasing evidence has demonstrated that, apart from acting on the GABA ergic system, VGB exerts an antiepileptic effect via regulating the metabolic changes of tissue endogenous substances including β-alanine, aspartic acid, ornithine, as well as the function of mechanistic target of rapamycin (mTOR) signalling pathway. In this article, we mainly review the progress of the studies focusing on mechanism, metabolism, and distribution of VGB, which will be helpful to understand the pharmacodynamics and toxic and side effects of VGB in depth.

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抗癫痫药物氨己烯酸(vigabatrin, VGB)是一种选择性、不可逆的γ-氨基丁酸转氨酶抑制剂,可通过增加中枢神经系统抑制性神经递质γ-氨基丁酸的浓度抑制大脑神经元异常放电。VGB的临床适应证为婴儿痉挛症的单一治疗、难治性部分发作性癫痫的辅助治疗,导致视野损失是限制其临床使用的主要不良反应。研究表明,除调节γ-氨基丁酸能神经功能之外,VGB还可通过调节β-丙氨酸、天冬氨酸和鸟氨酸等组织内源性物质的代谢变化及雷帕霉素机械靶蛋白(mTOR)信号通路的功能等途径发挥其抗癫痫作用。本文主要就VGB的作用机制及其体内代谢分布研究进展进行综述,旨在为深入了解VGB的药效和毒副作用机制提供依据。

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葛金芳,女,博士,教授,博士生导师,主要从事神经药理学研究。E-mail:
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郑强,男,硕士研究生,主要从事神经药理学研究。E-mail:

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氨己烯酸的作用机制及代谢分布研究进展
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郑强 1, 2, 3 , 樊敏 1, 2, 3 , 葛金芳 1, 2, 3
中国新药杂志 | 综述 2023,32(13): 1351-1357
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中国新药杂志 | 综述 2023, 32(13): 1351-1357
氨己烯酸的作用机制及代谢分布研究进展
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郑强1, 2, 3 , 樊敏1, 2, 3, 葛金芳1, 2, 3
作者信息
  • 1安徽医科大学药学院,合肥 230032
  • 2重大自身免疫性疾病安徽省重点实验室,合肥 230032
  • 3炎症免疫性疾病安徽省实验室,合肥 230032
  • 郑强,男,硕士研究生,主要从事神经药理学研究。E-mail:

通讯作者:

葛金芳,女,博士,教授,博士生导师,主要从事神经药理学研究。E-mail:
Research progress of the mechanism, metabolism and distribution of vigabatrin
Qiang ZHENG1, 2, 3 , Min FAN1, 2, 3, Jin-fang GE1, 2, 3
Affiliations
  • 1School of Pharmacy, Anhui Medical University, Hefei 230032, China
  • 2Anhui Province Key Laboratory of Major Autoimmune Diseases, Anhui Institute of Innovative Drugs, Hefei 230032, China
  • 3Anhui Key Laboratory of Anti-inflammatory and Immune Medicine, Ministry of Education, Anhui Medical University, Hefei 230032, China
出版时间: 2023-07-15
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抗癫痫药物氨己烯酸(vigabatrin, VGB)是一种选择性、不可逆的γ-氨基丁酸转氨酶抑制剂,可通过增加中枢神经系统抑制性神经递质γ-氨基丁酸的浓度抑制大脑神经元异常放电。VGB的临床适应证为婴儿痉挛症的单一治疗、难治性部分发作性癫痫的辅助治疗,导致视野损失是限制其临床使用的主要不良反应。研究表明,除调节γ-氨基丁酸能神经功能之外,VGB还可通过调节β-丙氨酸、天冬氨酸和鸟氨酸等组织内源性物质的代谢变化及雷帕霉素机械靶蛋白(mTOR)信号通路的功能等途径发挥其抗癫痫作用。本文主要就VGB的作用机制及其体内代谢分布研究进展进行综述,旨在为深入了解VGB的药效和毒副作用机制提供依据。

氨己烯酸  /  γ-氨基丁酸  /  婴儿痉挛症  /  分布  /  代谢

The antiepileptic drug vigabatrin (VGB) is a selective and irreversible inhibitor of γ-aminobutyric acid transaminase, which can inhibit the abnormal electrical activity in brain via increasing the concentration of inhibitory neurotransmitter γ-aminobutyric acid (GABA). The clinical indications of VGB include infantile spasms and refractory partial seizure epilepsy, acting as a single treatment or an adjuvant treatment, respectively. Visual field loss is the main adverse reaction of VGB that limits its clinical application. Increasing evidence has demonstrated that, apart from acting on the GABA ergic system, VGB exerts an antiepileptic effect via regulating the metabolic changes of tissue endogenous substances including β-alanine, aspartic acid, ornithine, as well as the function of mechanistic target of rapamycin (mTOR) signalling pathway. In this article, we mainly review the progress of the studies focusing on mechanism, metabolism, and distribution of VGB, which will be helpful to understand the pharmacodynamics and toxic and side effects of VGB in depth.

vigabatrin  /  γ-aminobutyric acid  /  infantile spasms  /  distribution  /  metabolism
郑强, 樊敏, 葛金芳. 氨己烯酸的作用机制及代谢分布研究进展. 中国新药杂志, 2023 , 32 (13) : 1351 -1357 .
Qiang ZHENG, Min FAN, Jin-fang GE. Research progress of the mechanism, metabolism and distribution of vigabatrin[J]. Chinese Journal of New Drugs, 2023 , 32 (13) : 1351 -1357 .
  • 安徽高校协同创新项目(GXXT-2020-062)
  • 安徽医科大学“三全育人”综合改革试点项目(2021xsqyr03)
2023年第32卷第13期
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  • 首发时间:2026-03-05
  • 出版时间:2023-07-15
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  • 录用日期:2022-10-25
基金
安徽高校协同创新项目(GXXT-2020-062)
安徽医科大学“三全育人”综合改革试点项目(2021xsqyr03)
作者信息
    1安徽医科大学药学院,合肥 230032
    2重大自身免疫性疾病安徽省重点实验室,合肥 230032
    3炎症免疫性疾病安徽省实验室,合肥 230032

通讯作者:

葛金芳,女,博士,教授,博士生导师,主要从事神经药理学研究。E-mail:
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2种不同金属材料的力学参数

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total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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