他拉莫三嗪
Talampanel.
作者信息
Howes John F, Bell Cynthia
机构信息
Department of New Drug Development, IVAX Research, Inc., Miami, Florida 33137, USA.
出版信息
Neurotherapeutics. 2007 Jan;4(1):126-9. doi: 10.1016/j.nurt.2006.11.001.
Abstract
Talampanel is a novel anticonvulsant that acts as an allosteric inhibitor of the AMPA receptor. Talampanel has a broad spectrum of action in animal models of epilepsy and neuroprotection. Clinical experience to date has been able to show effectiveness in reduction of seizures in patients with refractory partial seizures.
摘要
他拉莫三嗪是一种新型抗惊厥药，作为α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体的变构抑制剂发挥作用。他拉莫三嗪在癫痫和神经保护动物模型中具有广泛的作用谱。迄今为止的临床经验已证明其对减少难治性部分性癫痫患者的癫痫发作有效。
相似文献
1
Talampanel.他拉莫三嗪
Neurotherapeutics. 2007 Jan;4(1):126-9. doi: 10.1016/j.nurt.2006.11.001.
2
Protective effect of the antiepileptic drug candidate talampanel against AMPA-induced striatal neurotoxicity in neonatal rats.抗癫痫候选药物他仑帕奈对新生大鼠AMPA诱导的纹状体神经毒性的保护作用。
Brain Res Bull. 2002 Oct 15;59(1):35-40. doi: 10.1016/s0361-9230(02)00835-3.
3
Talampanel suppresses the acute and chronic effects of seizures in a rodent neonatal seizure model.他拉莫三嗪在啮齿动物新生儿癫痫模型中可抑制癫痫发作的急性和慢性影响。
Epilepsia. 2009 Apr;50(4):694-701. doi: 10.1111/j.1528-1167.2008.01947.x. Epub 2009 Feb 12.
4
Pre- and post-exposure talampanel (GYKI 53773) against kainic acid seizures in neonatal rats.暴露前和暴露后使用他拉莫林（GYKI 53773）预防新生大鼠的海藻酸诱发癫痫。
Pharmacol Rep. 2016 Feb;68(1):190-5. doi: 10.1016/j.pharep.2015.08.011. Epub 2015 Sep 1.
5
Talampanel, a new antiepileptic drug: single- and multiple-dose pharmacokinetics and initial 1-week experience in patients with chronic intractable epilepsy.他拉莫三嗪，一种新型抗癫痫药物：慢性顽固性癫痫患者的单剂量和多剂量药代动力学及最初1周的用药经验
Epilepsia. 2003 Jan;44(1):46-53. doi: 10.1046/j.1528-1157.2003.128902.x.
6
AMPA receptor inhibitors for the treatment of epilepsy: the role of perampanel.AMPA 受体抑制剂治疗癫痫：仑帕奈的作用。
Expert Rev Neurother. 2013 Jun;13(6):647-55. doi: 10.1586/ern.13.46.
7
Talampanel a non-competitive AMPA-antagonist attenuates caspase-3 dependent apoptosis in mouse brain after transient focal cerebral ischemia.他仑帕奈，一种非竞争性AMPA拮抗剂，可减轻短暂性局灶性脑缺血后小鼠脑中依赖半胱天冬酶-3的细胞凋亡。
Brain Res Bull. 2006 Jul 31;70(3):260-2. doi: 10.1016/j.brainresbull.2006.02.024. Epub 2006 Mar 31.
8
Pharmacotherapy of epilepsy: newly approved and developmental agents.癫痫的药物治疗：新批准和正在研发的药物。
CNS Drugs. 2011 Feb;25(2):89-107. doi: 10.2165/11584860-000000000-00000.
9
Phase 2 trial of talampanel, a glutamate receptor inhibitor, for adults with recurrent malignant gliomas.替拉奈班的 2 期临床试验，谷氨酸受体抑制剂，用于复发性恶性脑胶质瘤的成人患者。
Cancer. 2010 Apr 1;116(7):1776-82. doi: 10.1002/cncr.24957.
10
Mechanism of inhibition of the GluA2 AMPA receptor channel opening by talampanel and its enantiomer: the stereochemistry of the 4-methyl group on the diazepine ring of 2,3-benzodiazepine derivatives.噻加宾及对映体抑制 GluA2 AMPA 受体通道开放的作用机制：2,3-苯并二氮䓬衍生物的二氮杂环庚烷环上 4-甲基的立体化学。
ACS Chem Neurosci. 2013 Apr 17;4(4):635-44. doi: 10.1021/cn3002398. Epub 2013 Feb 12.
引用本文的文献
1
Disrupted glutamate homeostasis as a target for glioma therapy.谷氨酸代谢失衡作为胶质瘤治疗的靶点。
Pharmacol Rep. 2024 Dec;76(6):1305-1317. doi: 10.1007/s43440-024-00644-y. Epub 2024 Sep 11.
2
Deciphering the Biophysical Properties of Ion Channel Gating Pores by Coumarin-Benzodiazepine Hybrid Derivatives: Selective AMPA Receptor Antagonists.通过香豆素-苯二氮杂䓬杂合体衍生物解析离子通道门控孔的生物物理特性：选择性 AMPA 受体拮抗剂。
Mol Neurobiol. 2024 Jul;61(7):4565-4576. doi: 10.1007/s12035-023-03871-1. Epub 2023 Dec 18.
3
Antitumor Potential of Antiepileptic Drugs in Human Glioblastoma: Pharmacological Targets and Clinical Benefits.抗癫痫药物在人胶质母细胞瘤中的抗肿瘤潜力：药理学靶点与临床益处
Biomedicines. 2023 Feb 16;11(2):582. doi: 10.3390/biomedicines11020582.
4
Anti-tumor effects of perampanel in malignant glioma cells.吡仑帕奈对恶性胶质瘤细胞的抗肿瘤作用。
Oncol Lett. 2022 Oct 7;24(6):421. doi: 10.3892/ol.2022.13541. eCollection 2022 Dec.
5
Synergistic Effect of Perampanel and Temozolomide in Human Glioma Cell Lines.吡仑帕奈与替莫唑胺对人胶质瘤细胞系的协同作用
J Pers Med. 2021 May 10;11(5):390. doi: 10.3390/jpm11050390.
6
Radiosensitizers in the temozolomide era for newly diagnosed glioblastoma.替莫唑胺时代用于新诊断胶质母细胞瘤的放射增敏剂
Neurooncol Pract. 2020 Jun;7(3):268-276. doi: 10.1093/nop/npz057. Epub 2019 Nov 30.
7
The AMPA receptor antagonist perampanel robustly rescues amyotrophic lateral sclerosis (ALS) pathology in sporadic ALS model mice.AMPA 受体拮抗剂吡仑帕奈能显著改善散发性 ALS 模型小鼠的肌萎缩侧索硬化症（ALS）病理。
Sci Rep. 2016 Jun 28;6:28649. doi: 10.1038/srep28649.
8
Mechanism-based design of 2,3-benzodiazepine inhibitors for AMPA receptors.基于机制的AMPA受体2,3-苯并二氮杂䓬抑制剂设计
Acta Pharm Sin B. 2015 Nov;5(6):500-5. doi: 10.1016/j.apsb.2015.07.007. Epub 2015 Sep 26.
9
Treatment of status epilepticus with ketamine, are we there yet?氯胺酮治疗癫痫持续状态，我们做到了吗？
CNS Neurosci Ther. 2013 Jun;19(6):411-27. doi: 10.1111/cns.12096. Epub 2013 Apr 20.
10
Mechanism of inhibition of the GluA2 AMPA receptor channel opening by talampanel and its enantiomer: the stereochemistry of the 4-methyl group on the diazepine ring of 2,3-benzodiazepine derivatives.噻加宾及对映体抑制 GluA2 AMPA 受体通道开放的作用机制：2,3-苯并二氮䓬衍生物的二氮杂环庚烷环上 4-甲基的立体化学。
ACS Chem Neurosci. 2013 Apr 17;4(4):635-44. doi: 10.1021/cn3002398. Epub 2013 Feb 12.
本文引用的文献
1
2
Talampanel improves the functional deficit after transient focal cerebral ischemia in rats. A 30-day follow up study.他拉莫三嗪可改善大鼠短暂性局灶性脑缺血后的功能缺损。一项为期30天的随访研究。
Brain Res Bull. 2006 Jan 15;68(4):269-76. doi: 10.1016/j.brainresbull.2005.08.018. Epub 2005 Sep 19.
3
Unified pharmacogenetics-based parent-metabolite pharmacokinetic model incorporating acetylation polymorphism for talampanel in humans.基于统一药物遗传学的母体-代谢物药代动力学模型，纳入了人类中他拉莫泮的乙酰化多态性。
J Pharmacokinet Pharmacodyn. 2005 Aug;32(3-4):377-400. doi: 10.1007/s10928-005-0001-y.
4
The AMPA-antagonist talampanel is neuroprotective in rodent models of focal cerebral ischemia.AMPA拮抗剂他仑帕奈在局灶性脑缺血的啮齿动物模型中具有神经保护作用。
Brain Res Bull. 2005 Jul 15;66(1):43-9. doi: 10.1016/j.brainresbull.2005.03.012. Epub 2005 Apr 21.
5
Effect of two noncompetitive AMPA receptor antagonists GYKI 52466 and GYKI 53405 on vigilance, behavior and spike-wave discharges in a genetic rat model of absence epilepsy.两种非竞争性AMPA受体拮抗剂GYKI 52466和GYKI 53405对失神癫痫基因大鼠模型警觉性、行为及棘波放电的影响
Brain Res. 2004 May 22;1008(2):236-44. doi: 10.1016/j.brainres.2004.01.087.
6
Immunohistochemical analysis of protein expression after middle cerebral artery occlusion in mice.小鼠大脑中动脉闭塞后蛋白质表达的免疫组织化学分析。
Acta Neuropathol. 2004 Feb;107(2):127-36. doi: 10.1007/s00401-003-0789-8. Epub 2003 Nov 26.
7
Effect of zonisamide on molecular regulation of glutamate and GABA transporter proteins during epileptogenesis in rats with hippocampal seizures.唑尼沙胺对海马癫痫大鼠癫痫发生过程中谷氨酸和γ-氨基丁酸转运蛋白分子调控的影响。
Brain Res Mol Brain Res. 2003 Aug 19;116(1-2):1-6. doi: 10.1016/s0169-328x(03)00183-9.
8
9
Talampanel, a new antiepileptic drug: single- and multiple-dose pharmacokinetics and initial 1-week experience in patients with chronic intractable epilepsy.他拉莫三嗪，一种新型抗癫痫药物：慢性顽固性癫痫患者的单剂量和多剂量药代动力学及最初1周的用药经验
Epilepsia. 2003 Jan;44(1):46-53. doi: 10.1046/j.1528-1157.2003.128902.x.
10
A crossover, add-on trial of talampanel in patients with refractory partial seizures.托吡酯对难治性部分性癫痫患者的交叉附加试验。
Neurology. 2002 Jun 11;58(11):1680-2. doi: 10.1212/wnl.58.11.1680.
Zotero 插件