Gabapentin

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Chemical Structure| 60142-96-3 同义名 : CI-945
CAS号 : 60142-96-3
货号 : A262003
分子式 : C9H17NO2
纯度 : 98%
分子量 : 171.23
MDL号 : MFCD00865286
存储条件:

Pure form Keep in dark place,Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 1 mg/mL(5.84 mM),配合低频超声助溶,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: 50 mg/mL(291.99 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Gabapentin (GBP) is an analog of GABA, it does not bind to GABAA or GABAB receptors, but it can increase GABA and can decrease glutamate concentrations. One imaging study has reported that gabapentin (1200 and 2400 mg) significantly (and rapidly) increased measurable concentrations of brain gamma-aminobutryric acid (GABA)[3]. In vivo, once daily treatment with the anti-epileptic and neuropathic pain medication, gabapentin, at low dosage (50 mg/kg) mitigates experimentally induced autonomic dysreflexia (AD) soon after injections, likely by impeding glutamatergic signaling. In addition distinct mechanisms of action for acute GBP to mitigate induced AD whereas chronic GBP increases non-induced AD frequencies[4].
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
NCT00967707 Post-traumatic Neuropathic Pai... 展开 >>n 收起 << Phase 2 Completed - Sweden ... 展开 >> Multidisciplinary Pain Centre, Uppsala University Hospital Uppsala, Sweden, 75185 收起 <<
NCT01177514 Pain After Photorefractive Ker... 展开 >>atectomy 收起 << Phase 4 Completed - Mexico ... 展开 >> Codet Vision Institute Tijuana, Baja California, Mexico, 22320 收起 <<
NCT00934193 Post-thoracotomy Pain Phase 3 Withdrawn - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.84mL

1.17mL

0.58mL

29.20mL

5.84mL

2.92mL

58.40mL

11.68mL

5.84mL

参考文献

[1]Sills GJ. The mechanisms of action of gabapentin and pregabalin. Curr Opin Pharmacol. 2006 Feb;6(1):108-13.

[2]Fink K, Dooley DJ, et al. Inhibition of neuronal Ca(2+) influx by gabapentin and pregabalin in the human neocortex. Neuropharmacology. 2002 Feb;42(2):229-36.

[3]Smith RV, Havens JR, Walsh SL. Gabapentin misuse, abuse and diversion: a systematic review. Addiction. 2016;111(7):1160-1174.

[4]Eldahan KC, Williams HC, Cox DH, Gollihue JL, Patel SP, Rabchevsky AG. Paradoxical effects of continuous high dose gabapentin treatment on autonomic dysreflexia after complete spinal cord injury. Exp Neurol. 2020;323:113083.