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 Experiment Videos

Neuroprotective agent riluzole potentiates postsynaptic GABA(A) receptor function.

Y He1, A Benz, T Fu

  • 1Department of Psychiatry, Washington University School of Medicine, St Louis, MO 63110, USA.

Neuropharmacology
|January 24, 2002
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

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

Sort by
Same author

Time- and momentum-resolved photoemission studies using time-of-flight momentum microscopy at a free-electron laser.

The Review of scientific instruments·2020
Same author

[Erratum to: Pulmonary lesion mimicking non-small lung cancer].

Der Chirurg; Zeitschrift fur alle Gebiete der operativen Medizen·2019
Same author

[Pulmonary lesion mimicking non-small lung cancer].

Der Chirurg; Zeitschrift fur alle Gebiete der operativen Medizen·2019
Same author

A neurosteroid analogue with T-type calcium channel blocking properties is an effective hypnotic, but is not harmful to neonatal rat brain.

British journal of anaesthesia·2018
Same author

[Hemoptysis with a rare cause].

Der Chirurg; Zeitschrift fur alle Gebiete der operativen Medizen·2018
Same author

Exclusive Activation of Caspase-3 in Mossy Fibers and Altered Dynamics of Autophagy Markers in the Mice Hippocampus upon Status Epilepticus Induced by Kainic Acid.

Molecular neurobiology·2017

The antiepileptic drug riluzole, a sodium channel blocker, also enhances postsynaptic GABA(A) receptor activity. This dual action suggests riluzole may represent a novel class of anticonvulsants with improved efficacy.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Riluzole is an established antiepileptic drug known for blocking voltage-gated sodium channels.
  • It also presynaptically inhibits glutamate release more than GABA release.

Purpose of the Study:

  • To investigate the postsynaptic effects of riluzole on GABA(A) receptors.
  • To determine if riluzole has additional mechanisms of action beyond its known presynaptic effects.

Main Methods:

  • Experiments were conducted on cultured hippocampal neurons and Xenopus oocytes expressing recombinant GABA(A) receptors.
  • Electrophysiological techniques, including patch-clamp recordings, were used to measure postsynaptic currents.
  • Pharmacological agents were employed to probe the binding sites and mechanisms of action.

Related Experiment Videos

Main Results:

  • Riluzole potentiated postsynaptic GABA(A) responses at higher concentrations (20-100 microM).
  • It selectively prolonged the decay of inhibitory postsynaptic currents (IPSCs) without altering their amplitude or frequency, indicating a postsynaptic mechanism.
  • Riluzole directly gated GABA(A) currents and lowered the EC(50) for GABA activation, suggesting a novel allosteric modulation site.

Conclusions:

  • Riluzole exhibits a dual mechanism of action, combining voltage-gated sodium channel blockade with postsynaptic potentiation of GABA(A) receptors.
  • This unique profile suggests riluzole may represent a new class of anticonvulsants with potentially enhanced therapeutic benefits.