Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Antiepileptic Drugs: GABAergic Pathway Potentiators01:18

Antiepileptic Drugs: GABAergic Pathway Potentiators

γ-aminobutyric acid or GABA, plays a pivotal role as an inhibitory neurotransmitter in the brain. GABA pathway potentiators, also known as GABAergic drugs, are a class of pharmaceutical agents designed to enhance the functioning of the GABAergic system. These medications primarily treat epilepsy, a neurological disorder characterized by recurrent seizures.
The key GABA pathway potentiators used in epilepsy management are as follows.
Benzodiazepines are a well-known class of drugs used for their...
Antiepileptic Drugs: Glutamate Antagonists01:14

Antiepileptic Drugs: Glutamate Antagonists

Glutamate is a fundamental neurotransmitter in the central nervous system, playing a vital role in neuronal communication and various cognitive processes. Glutamate stands as the principal excitatory neurotransmitter in the brain. Its presence is crucial for the communication between neurons, underpinning essential processes such as synaptic transmission, neuronal excitability, and plasticity. These functions are vital for higher-order cognitive processes, including learning and memory. The...
Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein01:20

Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein

Antiepileptic drugs, such as levetiracetam (Keppra) and brivaracetam (Briviact), have emerged as crucial tools in managing epilepsy. These medications exert their therapeutic effects by targeting the synaptic vesicle protein SV2A, a transmembrane glycoprotein primarily found in the brain.
SV2A is a transmembrane glycoprotein located predominantly in the brain, modulating the release of neurotransmitters for neuronal communication. Both levetiracetam and brivaracetam exhibit a high affinity for...
Antiepileptic Drugs: Potassium Channel Activators01:20

Antiepileptic Drugs: Potassium Channel Activators

Ezocgabine or retigabine, an antiepileptic drug of remarkable efficacy, has revolutionized the management of seizures. It is a potassium channel activator, explicitly targeting the family of Q subtype potassium channels. It enhances the transmembrane potassium currents, regulating neuronal excitability. This action stabilizes the resting membrane potential, a pivotal factor in mitigating the hyperexcitability that characterizes epilepsy.
Ezogabine has gained approval as an adjunctive treatment...
Drugs Affecting Neurotransmitter Release or Uptake01:21

Drugs Affecting Neurotransmitter Release or Uptake

Certain drugs can affect how neurotransmitters called catecholamines, are released or taken back up in the adrenergic neuron. They can have different effects on the body's sympathetic transmission. Reserpine, a natural compound found in the Rauwolfia shrub, blocks a transporter called vesicular monoamine transporter (VMAT), which leads to a buildup of catecholamines in the cell and reduces sympathetic transmission. Another drug called guanethidine works in multiple ways, including blocking...
Desensitization and Tachyphylaxis01:20

Desensitization and Tachyphylaxis

Tachyphylaxis is described as a rapid decrease in response to a drug after repeated or continuous administration of the same drug dose. It is a phenomenon where the body becomes less responsive to a particular substance or intervention over time, requiring higher doses or stronger interventions to achieve the same effect. It results from adaptive changes in the body's receptors, signaling pathways, or physiological processes that occur in response to prolonged exposure to a stimulus.
Several...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Novel fenoterol derivatives as suppressors of ERK1/2 phosphorylation in melanoma.

Naunyn-Schmiedeberg's archives of pharmacology·2026
Same author

Pilot study comparing three analgesia approaches for rib fractures.

Regional anesthesia and pain medicine·2026
Same author

Performing Dual Glucose Clamp Experiments in Sedated Farm Swine: A Practical Method.

Methods and protocols·2025
Same author

The Association Between Intraoperative Heparin and Postoperative Thrombotic Complications after Total Hip and Knee Arthroplasty: A Retrospective Analysis.

The Journal of arthroplasty·2025
Same author

A comprehensive analysis of in-hospital adverse events after scopolamine administration: insights from a retrospective cohort study using a large nationwide inpatient database.

BMC anesthesiology·2024
Same author

Randomized Controlled Trial of Enhanced Recovery After Surgery Protocols in Live Kidney Donors: ERASKT Study.

Transplantation direct·2024
Same journal

Dynorphinergic neuroadaptations in the islands of Calleja: implications for alcohol use disorder.

Neuroscience letters·2026
Same journal

Differential vulnerability of cochlear nuclei to Lmx1 deficiency: abnormal patterning and implications for auditory circuitry.

Neuroscience letters·2026
Same journal

Role of nNOS/sGC pathway in the insular cortex in control of cardiovascular, autonomic and corticosterone responses to restraint stress in rats.

Neuroscience letters·2026
Same journal

Jak1 inhibition reduces acute allodynia induced by specific upstream cytokines in rats: implications for the onset of Jak1 pain modulation.

Neuroscience letters·2026
Same journal

Glucocorticoids-induced depressive-like behaviors in mice: oral ingestion of corticosterone or hydrocortisone - A comparative study.

Neuroscience letters·2026
Same journal

Data-driven clustering of prefrontal activation identifies functional phenotypes under prioritized dual-task walking conditions in Parkinson's disease.

Neuroscience letters·2026
See all related articles

Related Experiment Video

Updated: May 15, 2026

A High-throughput Calcium-flux Assay to Study NMDA-receptors with Sensitivity to Glycine/D-serine and Glutamate
04:48

A High-throughput Calcium-flux Assay to Study NMDA-receptors with Sensitivity to Glycine/D-serine and Glutamate

Published on: July 10, 2018

Gabapentin and (S)-pregabalin decrease intracellular D-serine concentrations in PC-12 cells.

Nagendra S Singh1, Rajib K Paul, Marc C Torjman

  • 1Laboratory of Clinical Investigation, National Institute on Aging, National Institutes of Health, Baltimore, MD 21224, USA.

Neuroscience Letters
|January 1, 2013
PubMed
Summary
This summary is machine-generated.

Gabapentin (GBP) and (S)-pregabalin (PGB) reduce intracellular d-serine levels by decreasing serine racemase activity, potentially acting as N-methyl D-aspartate receptor antagonists. This mechanism may explain their therapeutic effects in neuropathic pain.

More Related Videos

Exploring the Two Herb Combination Strategy to Treat Injured PC12 Cells
10:33

Exploring the Two Herb Combination Strategy to Treat Injured PC12 Cells

Published on: November 18, 2022

Seizure Activity Induced by Electroshock in Drosophila Larvae
06:10

Seizure Activity Induced by Electroshock in Drosophila Larvae

Published on: June 6, 2025

Related Experiment Videos

Last Updated: May 15, 2026

A High-throughput Calcium-flux Assay to Study NMDA-receptors with Sensitivity to Glycine/D-serine and Glutamate
04:48

A High-throughput Calcium-flux Assay to Study NMDA-receptors with Sensitivity to Glycine/D-serine and Glutamate

Published on: July 10, 2018

Exploring the Two Herb Combination Strategy to Treat Injured PC12 Cells
10:33

Exploring the Two Herb Combination Strategy to Treat Injured PC12 Cells

Published on: November 18, 2022

Seizure Activity Induced by Electroshock in Drosophila Larvae
06:10

Seizure Activity Induced by Electroshock in Drosophila Larvae

Published on: June 6, 2025

Area of Science:

  • Neuropharmacology
  • Cellular Neuroscience

Background:

  • d-Serine is a crucial co-agonist of the N-methyl D-aspartate receptor (NMDAR).
  • Gabapentin (GBP) and (S)-pregabalin (PGB) are widely used for neuropathic pain, but their precise mechanisms remain under investigation.

Purpose of the Study:

  • To investigate the effects of GBP and PGB on intracellular d-serine concentrations and serine racemase (SR) expression in PC-12 cells.
  • To elucidate the potential role of d-serine modulation in the NMDAR-mediated actions of GBP and PGB.

Main Methods:

  • PC-12 cells were treated with varying concentrations of GBP and PGB.
  • Intracellular d-serine concentrations were quantified using enantioselective capillary electrophoresis with laser-induced fluorescence detection.
  • Serine racemase expression was assessed via Western blotting.

Main Results:

  • Both GBP and PGB significantly decreased intracellular d-serine concentrations in a dose-dependent manner, with IC50 values around 3.4 μM.
  • Neither drug affected the expression levels of monomeric or dimeric serine racemase.
  • The observed reduction in d-serine is likely due to decreased serine racemase activity resulting from reduced Ca(2+) flux via the α(2)-δ subunit.

Conclusions:

  • GBP and PGB reduce basal serine racemase activity, leading to lower intracellular d-serine levels in PC-12 cells.
  • This modulation of d-serine may contribute to the indirect antagonism of NMDAR by GBP and PGB.
  • The findings suggest a novel mechanism for the clinical efficacy of these drugs in neuropathic pain management.