• 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

加巴喷丁对钾离子诱导的突触体钙内流的调节作用

Modulation of K(+)-induced synaptosomal calcium influx by gabapentin.

作者信息

Meder W P, Dooley D J

机构信息

Pfizer Global Research & Development, Department of Neuroscience Therapeutics, Ann Arbor, MI 48105, USA.

出版信息

Brain Res. 2000 Sep 1;875(1-2):157-9. doi: 10.1016/s0006-8993(00)02610-x.

DOI:10.1016/s0006-8993(00)02610-x
PMID:10967310
Abstract

Gabapentin, a drug useful in several neurological and psychiatric disorders, decreased K(+) (15 mM)-induced Ca(2+) increase in Fura-PE3-loaded rat neocortical synaptosomes (IC(50)=9.7 microM; submaximal inhibition of 28.6%). This effect may indicate a selective modulation of presynaptic Ca(2+) influx in response to depolarizing (pathological) conditions causing excessive neurotransmitter release.

摘要

加巴喷丁是一种对多种神经和精神疾病有效的药物，它可降低在负载Fura-PE3的大鼠新皮质突触体中由钾离子（15 mM）诱导的细胞内钙离子浓度升高（半数抑制浓度=9.7微摩尔；最大抑制率为28.6%）。这种效应可能表明在导致神经递质过度释放的去极化（病理）条件下，对突触前钙离子内流有选择性调节作用。

相似文献

1
Modulation of K(+)-induced synaptosomal calcium influx by gabapentin.加巴喷丁对钾离子诱导的突触体钙内流的调节作用
Brain Res. 2000 Sep 1;875(1-2):157-9. doi: 10.1016/s0006-8993(00)02610-x.
2
Inhibition of neuronal Ca(2+) influx by gabapentin and subsequent reduction of neurotransmitter release from rat neocortical slices.加巴喷丁对神经元Ca(2+)内流的抑制作用及随后大鼠新皮质切片神经递质释放的减少。
Br J Pharmacol. 2000 Jun;130(4):900-6. doi: 10.1038/sj.bjp.0703380.
3
Inhibition of neuronal Ca(2+) influx by gabapentin and pregabalin in the human neocortex.加巴喷丁和普瑞巴林对人新皮质神经元钙离子内流的抑制作用
Neuropharmacology. 2002 Feb;42(2):229-36. doi: 10.1016/s0028-3908(01)00172-1.
4
Gabapentin inhibits presynaptic Ca(2+) influx and synaptic transmission in rat hippocampus and neocortex.
Eur J Pharmacol. 2002 Aug 9;449(3):221-28. doi: 10.1016/s0014-2999(02)02044-7.
5
Effects of gabapentin and pregabalin on K+-evoked 3H-GABA and 3H-glutamate release from human neocortical synaptosomes.加巴喷丁和普瑞巴林对钾离子诱发的人新皮质突触体释放3H-γ-氨基丁酸和3H-谷氨酸的影响。
Naunyn Schmiedebergs Arch Pharmacol. 2009 Apr;379(4):361-9. doi: 10.1007/s00210-008-0370-z. Epub 2008 Nov 11.
6
Gabapentin actions on Kir3 currents and N-type Ca2+ channels via GABAB receptors in hippocampal pyramidal cells.加巴喷丁通过海马锥体细胞中的GABAB受体对Kir3电流和N型Ca2+通道的作用。
Synapse. 2003 Nov;50(2):95-109. doi: 10.1002/syn.10247.
7
Gabapentin inhibits high-threshold calcium channel currents in cultured rat dorsal root ganglion neurones.加巴喷丁可抑制培养的大鼠背根神经节神经元中的高阈值钙通道电流。
Br J Pharmacol. 2002 Jan;135(1):257-65. doi: 10.1038/sj.bjp.0704439.
8
A comparison of Ca2+ channel blocking mode between gabapentin and verapamil: implication for protection against hypoxic injury in rat cerebrocortical slices.加巴喷丁与维拉帕米钙通道阻断模式的比较：对大鼠大脑皮质切片缺氧损伤保护作用的启示
Br J Pharmacol. 2003 May;139(2):435-43. doi: 10.1038/sj.bjp.0705246.
9
Stimulus-dependent modulation of [(3)H]norepinephrine release from rat neocortical slices by gabapentin and pregabalin.加巴喷丁和普瑞巴林对大鼠新皮层切片中[³H]去甲肾上腺素释放的刺激依赖性调节
J Pharmacol Exp Ther. 2000 Dec;295(3):1086-93.
10
Inhibition of K(+)-evoked glutamate release from rat neocortical and hippocampal slices by gabapentin.加巴喷丁对大鼠新皮质和海马切片中钾离子诱发的谷氨酸释放的抑制作用。
Neurosci Lett. 2000 Feb 18;280(2):107-10. doi: 10.1016/s0304-3940(00)00769-2.

引用本文的文献

1
Gabapentin potentiates sensitivity to the interoceptive effects of alcohol and increases alcohol self-administration in rats.加巴喷丁增强大鼠对酒精内感受作用的敏感性并增加其酒精自我给药量。
Neuropharmacology. 2016 Feb;101:216-24. doi: 10.1016/j.neuropharm.2015.09.027. Epub 2015 Sep 28.
2
Nerve injury-induced calcium channel alpha-2-delta-1 protein dysregulation leads to increased pre-synaptic excitatory input into deep dorsal horn neurons and neuropathic allodynia.神经损伤诱导的钙通道α-2-δ-1蛋白失调导致突触前兴奋性输入增加至脊髓背角深层神经元，并引发神经性疼痛。
Eur J Pain. 2015 Oct;19(9):1267-76. doi: 10.1002/ejp.656. Epub 2015 Feb 17.
3
Molecular pharmacology of high voltage-activated calcium channels.
高电压激活钙通道的分子药理学
J Bioenerg Biomembr. 2003 Dec;35(6):491-505. doi: 10.1023/b:jobb.0000008022.50702.1a.
4
Gabapentin blocks L-type and P/Q-type Ca2+ channels involved in depolarization-stimulated nitric oxide synthase activity in primary cultures of neurons from mouse cerebral cortex.加巴喷丁可阻断参与小鼠大脑皮质神经元原代培养物中去极化刺激的一氧化氮合酶活性的L型和P/Q型Ca2+通道。
Pharm Res. 2003 Jun;20(6):897-9. doi: 10.1023/a:1024078704020.
5
A comparison of Ca2+ channel blocking mode between gabapentin and verapamil: implication for protection against hypoxic injury in rat cerebrocortical slices.加巴喷丁与维拉帕米钙通道阻断模式的比较：对大鼠大脑皮质切片缺氧损伤保护作用的启示
Br J Pharmacol. 2003 May;139(2):435-43. doi: 10.1038/sj.bjp.0705246.