Licensed by Pfizer Catalog No.S1338
Molecular Weight(MW): 207.7
Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
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|Description||Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.|
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. 
|In vitro||Water||42 mg/mL (202.21 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04068506||Recruiting||Drug: Gabapentin 600 mg Tab||Hand Injuries||Dow University of Health Sciences||September 1 2019||Phase 4|
|NCT03867240||Recruiting||Drug: Gabapentin|Other: Placebo||Pain Postoperative|Scoliosis Idiopathic||Emory University||June 25 2019||Phase 3|
|NCT03747562||Not yet recruiting||Drug: Gabapentin|Other: Placebo||Head Neck Cancer|Radiation Neuropathy|Pain Neuropathic||University Hospital Ghent|General Hospital Groeninge|Catholic University Leuven department Kortrijk (KULAK) Kortrijk Belgium|Anglia Ruskin University||March 1 2019||Phase 3|
|NCT03708237||Recruiting||Drug: Ropinirole|Drug: Gabapentin|Drug: Placebos||Restless Legs Syndrome|End Stage Renal Disease||University of Alberta||February 19 2019||Phase 2|
|NCT03583892||Recruiting||Drug: Gabapentin||Pain Postoperative||Centro Hospitalar do Porto||July 1 2018||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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