Gabapentin

Licensed by Pfizer Catalog No.S2133

Gabapentin  Chemical Structure

Molecular Weight(MW): 171.24

Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.

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Biological Activity

Description Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
Targets
GABA receptor [1]
In vitro

Gabapentin produces concentration-dependent inhibitions of the K(+)-induced [Ca(2+)](i) increase in fura-2-loaded human neocortical synaptosomes with IC50 of 17 mM and maximal inhibition of 37%. Gabapentin may bind to the Ca(2+) channel alpha 2 delta subunit to selectively attenuate depolarization-induced Ca(2+) influx of presynaptic P/Q-type Ca(2+) channels; this results in decreased glutamate/aspartate release from excitatory amino acid nerve terminals leading to a reduced activation of AMPA heteroreceptors on noradrenergic nerve terminals. [1] Gabapentin produces alterations in the cytosolic and extracellular concentrations of several amino acids, including L-leucine, L-valine and L-phenylalanine, in rat cortical astrocytes and synaptosomes, effects that are postulated to be of pharmacological significance. Gabapentin reduces potassium-evoked calcium influx via voltage-gated calcium channels in a mouse pituitary cell line that constitutively expresses GABAB receptors comprising the functional gb1a–gb2 subunit heterodimer. Gabapentin can increase N-methyl-d-aspartate (NMDA)-evoked currents in GABA-positive rat dorsal horn neurones in the presence of protein kinase C, possibly by increasing the glycine sensitivity of the NMDA receptor complex. Gabapentin produces a delayed allosteric enhancement of an unspecified voltage-activated potassium current in rat dorsal root ganglion neurons. [2]

In vivo Gabapentin dose-dependently (10-100 mg/kg, p.o.) blocks both static and dynamic allodynia in the rats. [3]

Protocol

Solubility (25°C)

In vitro Water 34 mg/mL (198.55 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 171.24
Formula

C9H17NO2

CAS No. 60142-96-3
Storage powder
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02160301 Suspended Post Operative Pain Control University of North Carolina, Chapel Hill November 2017 Phase 4
NCT03053427 Not yet recruiting Restless Legs Syndrome (RLS) Astellas Pharma Inc March 2017 Phase 4
NCT03012815 Not yet recruiting Alcohol Withdrawal Syndrome Mayo Clinic March 2017 Phase 4
NCT02957097 Not yet recruiting Pain, Postoperative|Acute Pain|Facial Pain Massachusetts General Hospital February 2017 Phase 4
NCT02999724 Recruiting Pelvic Organ Prolapse Mount Sinai Hospital, Canada January 2017 Phase 3
NCT02987985 Not yet recruiting Anesthesia|General Anesthesia|Analgesics, Opioid|Postoperative Complications|Pathologic Processes|Physiologic Effects of Drugs|Narcotics|Analgesics|Sleep Disordered Breathing|Obstructive Sleep Apnea of Child|Tonsillectomy|Respiratory Depression|Dexmedetomidine|Ketamine|Lidocaine|Gabapentin|Pulse Oximetry University of Saskatchewan January 2017 Phase 3

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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.

Handling Instructions

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GABA Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID