Gabapentin
(Synonyms: 加巴喷丁) 目录号 : GC12714
An approved antiepileptic drug
Cas No.:60142-96-3
Sample solution is provided at 25 µL, 10mM.
Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.IC50 Value: 140 nM (α2δ subunit of calcium channel) [1]Target: Calcium Channelin vitro: Gabapentin, baclofen and CGP 44532 all reduced the electrically stimulated release of [3H]glutamic acid (IC50=20 microM, 0.8 microM and 2 microM, respectively). Gabapentin was without effect on the release of [3H]GABA, whilst baclofen (IC50=8 microM) and CGP 44532 (IC50=1 microM) inhibited [3H]GABA release [2]. A large inhibition of calcium currents by gabapentin was observed in pyramidal neocortical cells (up to 34%). Significantly, the gabapentin-mediated inhibition of calcium currents saturated at particularly low concentrations (around 10 microM), at least in neocortical neurons (IC50 about 4 microM) [3].in vivo: Gabapentin produced an anti-allodynic effect over the 7-day period, reducing the expression of pro-inflammatory cytokines but increasing the expression of IL-10 (TNF-α, 316.0 ± 69.7 pg/mL vs 88.8 ± 24.4 pg/mL; IL-1β, 1,212.9 ± 104.5 vs 577.4 ± 97.1 pg/mL; IL-6, 254.0 ± 64.8 pg/mL vs 125.5 ± 44.1 pg/mL; IL-10, 532.1 ± 78.7 pg/mL vs 918.9 ± 63.1 pg/mL). The suppressive effect of gabapentin on pro-inflammatory cytokine expression was partially blocked by the anti-IL-10 antibody [4].Toxicity: No new safety signals or adverse event trends relating to GEn exposure were identified [5].Clinical trial: N/A
References:
[1]. Pan CF, et al. Inhibitory mechanisms of gabapentin, an antiseizure drug, on platelet aggregation. J Pharm Pharmacol. 2007 Sep;59(9):1255-61.
[2]. Gee NS, et al. The novel anticonvulsant drug, gabapentin (Neurontin), binds to the alpha2delta subunit of a calcium channel. J Biol Chem. 1996 Mar 8;271(10):5768-76.
[3]. Abdel-Salam OM, et al. The effect of gabapentin on oxidative stress in a model of toxic demyelination in rat brain. J Basic Clin Physiol Pharmacol. 2012;23(2):61-8.
[4]. Yang JL, et al. Gabapentin reduces CX3CL1 signaling and blocks spinal microglial activation in monoarthritic rats. Mol Brain. 2012 May 30;5:18.
[5]. Zand L, et al. Gabapentin toxicity in patients with chronic kidney disease: a preventable cause of morbidity. Am J Med. 2010 Apr;123(4):367-73.
[6]. Hung TY, et al. Gabapentin toxicity: an important cause of altered consciousness in patients with uraemia. BMJ Case Rep. 2009;2009. pii: bcr11.2008.1268.
| Cell experiment [1]: | |
|
Cell lines |
Pyramidal neocortical cells |
|
Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
10 μM |
|
Applications |
Gabapentin inhibited calcium currents in pyramidal neocortical cells (up to 34%). The gabapentin-mediated inhibition of calcium currents saturated at particularly low concentrations (around 10 μM), at least in neocortical neurons (IC50 about 4 microM) |
| Animal experiment [1,2]: | |
|
Animal models |
Rat model of neuropathic pain dynamic allodynia, rat model of brain demyelination evoked by intracerebral injection (i.c.i) of ethidium bromide |
|
Dosage form |
Oral administration, 10-100 mg/kg |
|
Application |
In the rat model of neuropathic pain dynamic allodynia, gabapentin (10-100 mg/kg, p.o.) dose-dependently blocked both types of allodynia. The intrathecal administration of gabapentin dose-dependently (1-100 μg/animal) blocked both static and dynamic allodynia. Administration of similar doses of gabapentin into the hind paw failed to block these responses. In a rat model of brain demyelination evoked by intracerebral injection (i.c.i) of ethidium bromide, gabapentin administered at 300 mg/kg increased cortical MDA by 66%. Gabapentin decreased GPx activity by 54.3%. Gabapentin decreased nitrite by 21.4% and 29.2% at 100 and 300 mg/kg, respectively. Gabapentin increased AChE activity increased by 28.6% and 69.3% at 100 and 300 mg/kg, respectively. Gabapentin decreased paraoxonase activity by 83.3% and 73% at 100 and 300 mg/kg, respectively. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Abdel-Salam O M E, Khadrawy Y A, Mohammed N A, et al. The effect of gabapentin on oxidative stress in a model of toxic demyelination in rat brain[J]. 2012. [2]. Field M J, McCleary S, Hughes J, et al. Gabapentin and pregabalin, but not morphine and amitriptyline, block both static and dynamic components of mechanical allodynia induced by streptozocin in the rat[J]. Pain, 1999, 80(1): 391-398. | |
| Cas No. | 60142-96-3 | SDF | |
| 别名 | 加巴喷丁 | ||
| 化学名 | 2-[1-(aminomethyl)cyclohexyl]acetic acid | ||
| Canonical SMILES | C1CCC(CC1)(CC(=O)O)CN | ||
| 分子式 | C9H17NO2 | 分子量 | 171.24 |
| 溶解度 | ≥ 8.56mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 5.8398 mL | 29.1988 mL | 58.3976 mL |
| 5 mM | 1.168 mL | 5.8398 mL | 11.6795 mL |
| 10 mM | 0.584 mL | 2.9199 mL | 5.8398 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet