Gabapentin

SKU: orb1310370

Description

Gabapentin is a small molecule anticonvulsant that exerts its therapeutic effect by reducing disorganized neuronal excitability in the central nervous system. It is widely used in research models of neuropathic pain and epilepsy, supporting both in vivo behavioral studies and in vitro electrophysiological investigations.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 60142-96-3
• MW: 171.24
• Purity: 99.55%
• Formula: C₉H₁₇NO₂
• SMILES: NCC1(CC(O)=O)CCCCC1
• Target: GABA Receptor,Calcium Channel
• Solubility: H2O:80 mg/mL (467.18 mM);DMSO:Insoluble

Bioactivity

• Target IC50:
  Ca2+ channel:140 nM
• 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.
• In Vitro:
  Administering 10-100 mg/kg of Gabapentin orally to rats results in a dose-dependent blockade of both static and dynamic allodynia.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Aclonium, calcium channel, Ca2+ channels, Calcium Channel, CalciumChannel, Ca channels, Neurontin, Inhibitor, inhibit, GABA Receptor, Gabapentine, GABAR, Gabapentin, GABAReceptor

Compound Identifiers

PubChem CID

3446