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抑制剂/激动剂
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蛋白质酪氨酸激酶 膜转运蛋白
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/ Levetiracetam/左乙拉西坦

Levetiracetam/左乙拉西坦 {[allProObj[0].p_purity_real_show]}

货号：A185961 同义名： UCB L059; SIB-S1

Levetiracetam是一种抗癫痫药，具有抗高痛觉过敏作用，能够结合突触小泡蛋白 SV2A（pIC50 = 5.7），推测通过改变小泡外排过程发挥作用。

Levetiracetam/左乙拉西坦 化学结构 CAS号：102767-28-2
Levetiracetam/左乙拉西坦 化学结构
CAS号：102767-28-2
Levetiracetam/左乙拉西坦 3D分子结构
CAS号：102767-28-2
Levetiracetam/左乙拉西坦 化学结构 CAS号：102767-28-2
Levetiracetam/左乙拉西坦 3D分子结构 CAS号：102767-28-2
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Levetiracetam/左乙拉西坦 纯度/质量文件 产品仅供科研

货号：A185961 标准纯度： {[allProObj[0].p_purity_real_show]}
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Levetiracetam/左乙拉西坦 生物活性

靶点

  • Calcium Channel
描述 Levetiracetam is an anticonvulsant with antihyperalgesic efficacy in inflammatory pain. It binds the synaptic vesicle protein SV2A (pIC50 = 5.7), presumably altering vesicle exocytosis.

Levetiracetam/左乙拉西坦 细胞实验

Cell Line
Concentration Treated Time Description References
Spinal cord neurons 100 μM 25 seconds At 100 μM, LEV had no effect on the amplitude or desensitization time constant of glycine-induced currents. Br J Pharmacol. 2002 Jul;136(5):659-72.
Hippocampal neurons 100 μM 25 seconds At 100 μM, LEV significantly reduced the peak amplitude of GABA-induced currents (78.2% of control) but had a lesser effect on the desensitization of GABA currents (134.2% of control). Br J Pharmacol. 2002 Jul;136(5):659-72.
Cerebellar granule neurons 100 μM 25 seconds At 100 μM, LEV marginally but significantly affected the peak amplitude of the current induced by 50 μM GABA and slowed the decay phase (desensitization). Br J Pharmacol. 2002 Jul;136(5):659-72.

Levetiracetam/左乙拉西坦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Alzheimer's disease model mice Subcutaneous injection 75 mg/kg/d Continuous for 28 days LEV effectively reduced abnormal spike activity in hAPP mice, reversed hippocampal remodeling, behavioral abnormalities, synaptic dysfunction, and deficits in learning and memory. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):E2895-903
Mice Sound-induced clonic convulsions model Intraperitoneal injection 17 mg/kg Single dose, 30 minutes before testing LEV significantly suppressed sound-induced clonic convulsions. This protective effect was significantly abolished by co-administration of the β-carboline FG 7142 (10 mg/kg), while the benzodiazepine receptor antagonist flumazenil (5 mg/kg) had no effect. Br J Pharmacol. 2002 Jul;136(5):659-72.
ICR mice Not specified Intraperitoneal injection 1, 3, 10, 30, 100 and 300 mg kg-1 Twice daily for 5 days Investigated the effects of Levetiracetam on glutamine synthetase activity in mouse brain, showing no significant effect after single or repeated administration. Br J Pharmacol. 1999 Apr;126(7):1634-8
Mice Sepsis model (CLP) Intraperitoneal injection 300 mg/kg Every 12 hours for 48 hours Prevention of post-sepsis anxiety and PTSD-like fear expression Brain. 2022 May 24;145(4):1391-1409
Mice STXBP1-encephalopathy model Intraperitoneal injection 50 mg/kg Once daily for 5 days To evaluate the effect of the antiepileptic drug levetiracetam on epileptic-like activity and EEG abnormalities in STXBP1-encephalopathy model mice. Results showed that levetiracetam significantly reduced spike-wave discharges. Brain. 2018 May 1;141(5):1350-1374
Mice IL18KO/APP/PS1 mouse model Oral 1.8 mg/mL Daily for 8 weeks Levetiracetam almost completely prevented death in IL18KO/APP/PS1 mice Proc Natl Acad Sci U S A. 2018 Sep 4;115(36):9002-9007
Transgenic APP mice (line J20) Alzheimer's disease model Intraperitoneal injection and subcutaneous micro-osmotic pump 75 mg/kg 3 times per day for 2 weeks; or continuously for 4 weeks via micro-osmotic pumps To evaluate the effects of Levetiracetam on neurogenesis and spatial discrimination, showing that treatment restored neurogenesis dynamics and improved spatial discrimination Cell Rep. 2019 Jun 25;27(13):3741-3751.e4

Levetiracetam/左乙拉西坦 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01392768 Epilepsy Part... 展开 >>ial Seizures 收起 << Phase 3 Completed - -
NCT00413296 Post-Traumatic Stress Disorder Phase 2 Phase 3 Completed - United States, North Carolina ... 展开 >> Duke University Medical Center Durham, North Carolina, United States, 27705 收起 <<
NCT00826865 Seizures Not Applicable Completed - United States, Arizona ... 展开 >> MDS Pharma Services Phoenix, Arizona, United States, 85044 收起 <<

Levetiracetam/左乙拉西坦 参考文献

[1]Rigo JM, Hans G, et al. The anti-epileptic drug levetiracetam reverses the inhibition by negative allosteric modulators of neuronal GABA- and glycine-gated currents. Br J Pharmacol. 2002 Jul;136(5):659-72.

[2]Lukyanetz EA, Shkryl VM, Kostyuk PG. Selective blockade of N-type calcium channels by levetiracetam. Epilepsia. 2002 Jan;43(1):9-18.

Levetiracetam/左乙拉西坦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.88mL

1.18mL

0.59mL

29.38mL

5.88mL

2.94mL

58.75mL

11.75mL

5.88mL

Levetiracetam/左乙拉西坦 技术信息

CAS号102767-28-2
分子式C8H14N2O2
分子量 170.21
SMILES Code CC[C@H](N1CCCC1=O)C(N)=O
MDL No. MFCD03265610
别名 UCB L059; SIB-S1; Levetiracetam, Keppra, Etiracetam, UCB 6474
运输蓝冰
InChI Key HPHUVLMMVZITSG-LURJTMIESA-N
Pubchem ID 5284583
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 90 mg/mL(528.76 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 85 mg/mL(499.39 mM)

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Levetiracetam | UCB L059;SIB-S1;Levetiracetam, Keppra, Etiracetam, UCB 6474 | Other Compounds | SV2 | GAK | AmBeed-信号通路专用抑制剂 | Levetiracetam/左乙拉西坦 纯度/质量文件 | Levetiracetam/左乙拉西坦 生物活性 | Levetiracetam/左乙拉西坦 临床数据 | Levetiracetam/左乙拉西坦 参考文献 | Levetiracetam/左乙拉西坦 实验方案 | Levetiracetam/左乙拉西坦 技术信息

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