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1-(Aminomethyl)cyclohexaneacetic acid Gabapentin Neurontin
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Molecular Formula | C9H17NO2 |
Molar Mass | 171.24 |
Density | 1.058±0.06 g/cm3(Predicted) |
Melting Point | 162°C |
Boling Point | 314.4±15.0 °C(Predicted) |
Flash Point | 9℃ |
Water Solubility | H2O: 10 mg/mL |
Solubility | H2O: 10mg/mL |
Vapor Presure | 6.32E-05mmHg at 25°C |
Appearance | solid |
Color | off-white |
Merck | 14,4319 |
BRN | 2359739 |
pKa | pKa1 (25°) 3.68; pKa2 10.70 |
Storage Condition | 2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20°C for up to 3 months. |
Refractive Index | 1.484 |
Physical and Chemical Properties | Melting Point: 162°C |
In vitro study | Gabapentin concentration-dependent inhibition of potassium (+)-induced increases in [Ca(2 )] in fura-2-loaded human neocortical synaptosomes, the IC 50 is 17 mM and the maximum suppression is 37%. Gabapentin binds to the α2 delta subunit of the calcium channel to selectively attenuate the Ca(2) channel of the (2) internal flow of the P / Q type of the Ca presynaptic induced by depolarization, this will result in a decrease in the release of glutamate/aspartate from the excitatory amino acid nerve terminals to the noradrenergic nerve terminals by AMPA heteroreceptors. In rat cortical astrocytes and synaptosomes, Gabapentin causes production of cytoplasmic alterations and changes in extracellular concentrations of several amino acids, including L-leucine, L-valine, and L-phenylalanine, it is assumed to be an effect of pharmacological significance. In GABA B receptors constitutively expressing heterodimers of gb1a-GB2 subunits, Gabapentin reduces potassium-evoked calcium influx through voltage-gated calcium channels. In GABA-positive rat spinal dorsal horn neurons, Gabapentin increases N-methyl-D-aspartate (NMDA)-evoked currents in the presence of protein kinase C, possibly by increasing the glycine sensitivity of the NMDA receptor complex. In rat dorsal root ganglion neurons, Gabapentin enhances delayed allosteric activity of indeterminate voltage-activated potassium currents. |
In vivo study | In rats, Gabapentin dose-dependently (10-100 mg/kg, oral) blocks the effects of static and dynamic allodynia. |
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