Gabapentin
Gabapentin is structurally similar to GABA and is reported in various research studies to increase GABA concentrations within the brain. Gabapentin is also noted to bind to a novel site on voltage-sensitive Ca2+ channels. Additionally, Gabapentin is reported to demonstrate inhibition of dopamine release from caudate nucleus, prevent neuronal cell death, and is antinociceptive.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 171.24 |
| Cas No. | 60142-96-3 |
| Formula | C9H17NO2 |
| Solubility | ≥2.6 mg/mL in EtOH; ≥25.85 mg/mL in H2O; insoluble in DMSO |
| Chemical Name | 2-[1-(aminomethyl)cyclohexyl]acetic acid |
| SDF | Download SDF |
| Canonical SMILES | C1CCC(CC1)(CC(=O)O)CN |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Pyramidal neocortical cells |
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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. |
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Reacting condition |
10 μM |
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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]: | |
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Animal models |
Rat model of neuropathic pain dynamic allodynia, rat model of brain demyelination evoked by intracerebral injection (i.c.i) of ethidium bromide |
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Dosage form |
Oral administration, 10-100 mg/kg |
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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. |
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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. |
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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. |
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Quality Control & MSDS
- View current batch:
Chemical structure
