Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Gabapentin (Neurontin) is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
10 mg | In stock | $ 42.00 | |
25 mg | In stock | $ 57.00 | |
50 mg | In stock | $ 70.00 | |
100 mg | In stock | $ 97.00 | |
200 mg | In stock | $ 143.00 | |
500 mg | In stock | $ 243.00 | |
1 mL * 10 mM (in H2O) | In stock | $ 39.00 |
Description | Gabapentin (Neurontin) is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity. |
Targets&IC50 | Ca2+ channel:140 nM |
In vitro | Administering 10-100 mg/kg of Gabapentin orally to rats results in a dose-dependent blockade of both static and dynamic allodynia. |
In vivo | Gabapentin induces alterations in the cytoplasmic and extracellular concentrations of several amino acids (including L-leucine, L-valine, and L-phenylalanine) in rat cortical astrocytes and synaptosomes, suggesting pharmacological significance. In GABA B receptors composed of gb1a-GB2 subunit heterodimers, gabapentin decreases potassium-stimulated calcium influx via voltage-gated calcium channels. It potentiates N-methyl-D-aspartate-evoked currents in GABAergic rat spinal dorsal horn neurons in the presence of protein kinase C, possibly by enhancing the glycine sensitivity of the NMDA receptor complex. Gabapentin causes a delayed enhancement of indeterminate voltage-activated potassium currents in rat dorsal root ganglion neurons. In fura-2-loaded human neocortical synaptosomes, it concentration-dependently inhibits potassium(+)-induced [Ca(2+)] elevations with an IC50 of 17 mM and maximal inhibition of 37%. Gabapentin binds to the α2 delta subunit of calcium channels, selectively attenuating depolarization-induced presynaptic Ca(2+) influx through P/Q-type Ca(2+) channels, resulting in reduced glutamate/aspartate release from excitatory amino acid nerve terminals to AMPA heteroreceptors on noradrenergic nerve endings. |
Synonyms | Neurontin, Gabapentine, Aclonium |
Molecular Weight | 171.24 |
Formula | C9H17NO2 |
CAS No. | 60142-96-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Insoluble
H2O: 10 mM
You can also refer to dose conversion for different animals. More
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Gabapentin 60142-96-3 Membrane transporter/Ion channel Metabolism Neuroscience GABA Receptor Calcium Channel Inhibitor Neurontin inhibit Ca2+ channels Ca channels Gabapentine Aclonium inhibitor