• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

γ-乙炔基γ-氨基丁酸的抗癫痫活性:一种γ-氨基丁酸转氨酶的催化不可逆抑制剂。

Antiseizure activity of gamma-acetylenic gamma-aminobutyric acid: a catalytic irreversible inhibitor of gamma-aminobutyric acid transaminase.

作者信息

Schechter P J, Tranier Y, Jung M J, Sjoerdsma A

出版信息

J Pharmacol Exp Ther. 1977 Jun;201(3):606-12.

PMID:864598
Abstract

gamma-Acetylenic gamma-aminobutyric acid (gamma-acetylenic GABA) produces several-fold sustained elevations of brain GABA concentrations when administered intraperitoneally to mice. It protects mice against seizures induced by audiogenic stimuli, electroshock, thiosemicarbazide, isoniazid and strychnine. The duration and degree of audiogenic seizure protection appears to correlate with elevations in whole brain GABA levels. gamma-Acetylenic GABA does not protect against seizures induced by pentylenetetrazol or picrotoxin even at doses that increase brain GABA concentrations approximately 6-fold. This differential antiseizure activity suggests that the GABA system may play a role in some, but not all experimentally produced seizures.

摘要

γ-乙炔基γ-氨基丁酸(γ-乙炔基GABA)腹腔注射给小鼠时,可使脑内GABA浓度持续升高数倍。它能保护小鼠免受听源性刺激、电休克、氨基硫脲、异烟肼和士的宁诱发的癫痫发作。听源性癫痫发作保护的持续时间和程度似乎与全脑GABA水平的升高相关。即使在能使脑内GABA浓度增加约6倍的剂量下,γ-乙炔基GABA也不能保护小鼠免受戊四氮或印防己毒素诱发的癫痫发作。这种不同的抗癫痫活性表明,GABA系统可能在某些但并非所有实验性癫痫发作中起作用。

相似文献

1
Antiseizure activity of gamma-acetylenic gamma-aminobutyric acid: a catalytic irreversible inhibitor of gamma-aminobutyric acid transaminase.γ-乙炔基γ-氨基丁酸的抗癫痫活性:一种γ-氨基丁酸转氨酶的催化不可逆抑制剂。
J Pharmacol Exp Ther. 1977 Jun;201(3):606-12.
2
Audiogenic seizure protection by elevated brain GABA concentration in mice: effects of gamma-acetylenic gaba and gamma-vinyl GABA, two irreversible GABA-T inhibitors.小鼠脑内γ-氨基丁酸(GABA)浓度升高对听源性癫痫的保护作用:两种不可逆性GABA转氨酶(GABA-T)抑制剂——γ-乙炔基氨基丁酸和γ-乙烯基氨基丁酸的作用
Eur J Pharmacol. 1977 Oct 15;45(4):319-28. doi: 10.1016/0014-2999(77)90270-9.
3
[The mechanism of the anticonvulsive action of diazepam].[地西泮抗惊厥作用的机制]
Biull Eksp Biol Med. 1975 Mar;79(3):50-3.
4
[On the mechanism of action of valproid acid].[关于丙戊酸的作用机制]
Arzneimittelforschung. 1977;27(5):1081-2.
5
Differential sensitivity of ethanol withdrawal signs in the rat to gamma-aminobutyric acid (GABA)mimetics: blockade of audiogenic seizures but not forelimb tremors.大鼠乙醇戒断症状对γ-氨基丁酸(GABA)模拟物的差异敏感性:对听源性惊厥有阻断作用,但对前肢震颤无阻断作用。
J Pharmacol Exp Ther. 1983 Sep;226(3):720-5.
6
Behavioral effects of vigabatrin correlated with whole brain gamma-aminobutyric acid metabolism in audiogenic sensitive rats.氨己烯酸对听源性敏感大鼠的行为学影响与全脑γ-氨基丁酸代谢的相关性
Arzneimittelforschung. 1998 Jul;48(7):713-6.
7
Effect of gamma-vinyl GABA on bicuculline-induced seizures.
Neuropharmacology. 1981 Apr;20(4):351-5. doi: 10.1016/0028-3908(81)90008-3.
8
Catalytic inhibitors of GABA-transaminase as anticonvulsants in baboons with photosensitive epilepsy [proceedings].γ-氨基丁酸转氨酶催化抑制剂作为光敏性癫痫狒狒的抗惊厥药物[会议论文集]
Br J Pharmacol. 1978 Jun;63(2):390P.
9
Hypersynchronisation and sedation produced by GABA-transaminase inhibitors and picrotoxin: does GABA participate in sleep control?γ-氨基丁酸转氨酶抑制剂和印防己毒素引起的过度同步化与镇静作用:γ-氨基丁酸是否参与睡眠调控?
Waking Sleeping. 1979 Jul;3(3):245-54.
10
Changes in primary afferent depolarization after administration of gamma-acetylenic gamma aminobutyric acid (GAG), a gamma-aminobutyric acid (GABA) transaminase inhibitor.γ-乙炔基γ-氨基丁酸(GAG,一种γ-氨基丁酸(GABA)转氨酶抑制剂)给药后初级传入去极化的变化。
J Pharmacol Exp Ther. 1979 Nov;211(2):326-30.

引用本文的文献

1
Design and Mechanism of GABA Aminotransferase Inactivators. Treatments for Epilepsies and Addictions.GABA 转氨酶失活剂的设计与机制。癫痫和成瘾的治疗方法。
Chem Rev. 2018 Apr 11;118(7):4037-4070. doi: 10.1021/acs.chemrev.8b00009. Epub 2018 Mar 23.
2
Molecular targets for antiepileptic drug development.抗癫痫药物研发的分子靶点
Neurotherapeutics. 2007 Jan;4(1):18-61. doi: 10.1016/j.nurt.2006.11.010.
3
Investigation of the antifibrillatory activity of some anticonvulsant gamma-aminobutyric acid-transaminase inhibitors in the rabbit isolated heart: comparison with phenytoin and mexiletine.
某些抗惊厥γ-氨基丁酸转氨酶抑制剂对兔离体心脏抗纤颤活性的研究:与苯妥英和美西律的比较。
Br J Pharmacol. 1980;71(2):635-9. doi: 10.1111/j.1476-5381.1980.tb10984.x.
4
A comparative study of the pharmacology of inhibitors of GABA-metabolism.γ-氨基丁酸代谢抑制剂的药理学比较研究
Naunyn Schmiedebergs Arch Pharmacol. 1980;315(2):119-28. doi: 10.1007/BF00499254.
5
Oxolinic acid and diazepam: their reciprocal antagonism in rodents.恶喹酸和地西泮:它们在啮齿动物中的相互拮抗作用。
Psychopharmacology (Berl). 1980 Jan;67(1):91-5. doi: 10.1007/BF00427601.
6
GABAergic modulation of ethanol-induced motor impairment.乙醇诱导的运动障碍的γ-氨基丁酸能调节
J Pharmacol Exp Ther. 1982 Dec;223(3):750-6.
7
Cellular compartments of GABA in brain and their relationship to anticonvulsant activity.大脑中γ-氨基丁酸的细胞区室及其与抗惊厥活性的关系。
Mol Cell Biochem. 1981 Sep 25;39:305-29. doi: 10.1007/BF00232582.
8
Decreased susceptibility to seizures induced by bicuculline after transient bilateral clamping of the carotid arteries in rats.大鼠双侧颈总动脉短暂夹闭后对荷包牡丹碱诱发癫痫的易感性降低。
J Neural Transm Gen Sect. 1991;83(1-2):127-37. doi: 10.1007/BF01244459.
9
Actions of gamma-acetylenic GABA on single central neurones in rat [proceedings].γ-乙炔基 GABA 对大鼠单个中枢神经元的作用[会议论文集]
Br J Pharmacol. 1978 Nov;64(3):383P-384P.
10
Effect of elevated brain GABA concentrations on the actions of bicuculline and picrotoxin in mice.脑内γ-氨基丁酸浓度升高对小鼠荷包牡丹碱和印防己毒素作用的影响。
Psychopharmacology (Berl). 1977 Oct 20;54(2):145-8. doi: 10.1007/BF00426770.