Gabapentin hydrochloride

SKU: orb1300707

Description

Gabapentin hydrochloride is a γ-aminobutyric acid (GABA) analog employed in research models of epilepsy and neuropathic pain. It is utilized in both in vitro and in vivo studies to investigate its mechanisms of action on voltage-gated calcium channels.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 60142-95-2
• MW: 207.7
• Purity: 99.71%
• Formula: C₉H₁₇NO₂·HCl
• SMILES: Cl.NCC1(CC(O)=O)CCCCC1
• Target: GABA Receptor,Calcium Channel
• Solubility: DMSO:Insoluble;H2O:10 mM

Bioactivity

• Target IC50:
  α2δ Ca2+ channel:140 nM
• In Vitro:
  Gabapentin suppresses ectopic afferent discharge activity generated from injured peripheral nerves. Gabapentin, in a range of 30 to 90 mg/kg, significantly attenuates allodynia in nerve-injured rats. Gabapentin dose-dependently inhibits the ectopic discharge activity of 15 injured sciatic afferent nerve fibers through an action on impulse generation. Gabapentin inhibits KCl (30 mM)-evoked voltage-dependent Ca(2+) influx. Gabapentin potently inhibits the peak whole-cell Ca(2+) channel current (I(Ba)) in a dose-dependent manner with an estimated IC(50) value of 167 nM. Gabapentin inhibition is voltage-dependent, producing an approximately 7 mV hyperpolarizing shift in current voltage properties and reducing a non-inactivating component of whole-cell current activated at relatively depolarized potentials. Gabapentin selectively activates heterodimeric GABAB1a-B2 receptors, but not GABAB1b-B2 or GABAB1c-B2 receptors. Gabapentin selectively activates presynaptic GABAB heteroreceptors on glutamatergic terminals, but not GABAB autoreceptors on GABAergic terminals. Gabapentin is found to inhibit both the excitatory synaptic transmission in vitro and the neuronal response to noxious electrical and mechanical stimulation in vivo mediated by α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), but not those mediated by N-methyl-D-asparate (NMDA) receptors. Gabapentin acts as an AMPA-receptor antagonist in the rat spinal cord to exert its spinal antinociceptive effect. Gabapentin depresses, but NMDA enhanced, the presynaptic fiber volley in the CA1 region of rat hippocampal slices.

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

Calcium Channel, CalciumChannel, Ca channels, Ca2+ channels, GABAReceptor, GABAR, Gabapentin, Gabapentin HCl, Gabapentin hydrochloride, Gabapentin Hydrochloride, GABA Receptor, Neurontin HCl, inhibit, Inhibitor, α2δ calcium channels

Compound Identifiers

PubChem CID

6453919