| 产品描述： | Gabapentin hydrochloride is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca2+ influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain |
| 靶点： |
Calcium Channel;CalciumChannel;GABAReceptor |
| 体外研究： |
Gabapentin (0-300 μM) hydrochloride produces a concentration-dependent inhibition of the K+-induced [Ca2+]i increase in synaptosomes (IC50=14 μM; maximal inhibition by 36%). Gabapentin (100 μM) hydrochloride decreases the K+-evoked release of endogenous aspartate and glutamate in neocortical slices by 16 and 18%, respectively. Gabapentin (0-1000 μM) hydrochloride reduces the K+-evoked [3H]-noradrenaline release in neocortical slices (IC50=48 μM; maximal inhibition of 46%) but not from synaptosomes |
| 体内研究： |
Gabapentin (5 and 10 mg/kg; i.p.; once; male BALB/c mice) hydrochloride has improving effects on spatial and emotional cognitive performance of naive mice in Morris water maze (MWM), passive avoidance (PA) and modified elevated plus maze (mEPM) tasks. Gabapentin (1-100 mg/kg; i.p.; once; male mice) hydrochloride has analgesic effect and reduces writhing in a dose-dependent manner. Animal Model: Male BALB/c mice (35-45 g) Dosage: 5 and 10 mg/kg Administration: Intraperitoneal injection; once Result: Increased the time spent in target quadrant and decreased the distance to platform in MWM test. Decreased the transfer latency on second day in mEPM test. Prolonged retention latency in PA test. Animal Model: Male mice (26-30 g) Dosage: 1, 5, 10, 50 and 100 mg/kg Administration: Intraperitoneal injection; once Result: Produced 45-70% inhibition of writhing. |
| 参考文献： |
1. Fink K, et, al. Inhibition of neuronal Ca(2+) influx by gabapentin and subsequent reduction of neurotransmitter release from rat neocortical slices. Br J Pharmacol. 2000 Jun;130(4):900-6. 2. Celikyurt IK, et, al. Gabapentin, A GABA analogue, enhances cognitive performance in mice. Neurosci Lett. 2011 Apr 1;492(2):124-8. 3. Meymandi MS, et, al. Gabapentin action and interaction on the antinociceptive effect of morphine on visceral pain in mice. Eur J Anaesthesiol. 2008 Feb;25(2):129-34. |
| 溶解性： |
Soluble in H2O |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
4.815 ml |
24.073 ml |
48.146 ml |
| 5 mM |
0.963 ml |
4.815 ml |
9.629 ml |
| 10 mM |
0.481 ml |
2.407 ml |
4.815 ml |
| 50 mM |
0.096 ml |
0.481 ml |
0.963 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京