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

Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

3.3K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
3.3K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

15.0K
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
15.0K
Antiepileptic Drugs: GABAergic Pathway Potentiators01:18

Antiepileptic Drugs: GABAergic Pathway Potentiators

925
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...
925
Ligand-gated Ion Channels01:19

Ligand-gated Ion Channels

13.5K
Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
13.5K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

3.2K
G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
3.2K
The Two-State Receptor Model01:29

The Two-State Receptor Model

2.8K
The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
2.8K

You might also read

Related Articles

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

Sort by
Same author

Correcting congenital myasthenia-associated acetylcholine receptor defects.

Nature·2026
Same author

A sensory system for mating in octopus.

Science (New York, N.Y.)·2026
Same author

Honeybee GABA<sub>A</sub> receptor structure informs new insecticide development.

Neuron·2026
Same author

Shape-shifting conotoxins reveal divergent pore-targeting mechanisms in nicotinic receptors.

Structure (London, England : 1993)·2025
Same author

A sensory system for mating in octopus.

bioRxiv : the preprint server for biology·2025
Same author

Environmental microbiomes drive chemotactile sensation in octopus.

Cell·2025

Related Experiment Video

Updated: Nov 15, 2025

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

13.9K

Direct Structural Insights into GABAA Receptor Pharmacology.

Jeong Joo Kim1, Ryan E Hibbs1

  • 1Department of Neuroscience, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.

Trends in Biochemical Sciences
|March 6, 2021
PubMed
Summary

Recent structural biology advances reveal how drugs interact with GABAA receptors, the brain's primary inhibitory channels. This provides a foundation for understanding drug mechanisms and designing new therapeutics for neurological conditions.

Keywords:
Cys-loop receptor structurebenzodiazepinebicucullinecryo-EM structuregeneral anestheticpicrotoxin

More Related Videos

Inhibitory Synapse Formation in a Co-culture Model Incorporating GABAergic Medium Spiny Neurons and HEK293 Cells Stably Expressing GABAA Receptors
07:51

Inhibitory Synapse Formation in a Co-culture Model Incorporating GABAergic Medium Spiny Neurons and HEK293 Cells Stably Expressing GABAA Receptors

Published on: November 14, 2014

17.7K
Using an &#945;-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking
11:57

Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking

Published on: March 28, 2014

16.1K

Related Experiment Videos

Last Updated: Nov 15, 2025

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

13.9K
Inhibitory Synapse Formation in a Co-culture Model Incorporating GABAergic Medium Spiny Neurons and HEK293 Cells Stably Expressing GABAA Receptors
07:51

Inhibitory Synapse Formation in a Co-culture Model Incorporating GABAergic Medium Spiny Neurons and HEK293 Cells Stably Expressing GABAA Receptors

Published on: November 14, 2014

17.7K
Using an &#945;-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking
11:57

Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking

Published on: March 28, 2014

16.1K

Area of Science:

  • Neuroscience
  • Pharmacology
  • Structural Biology

Background:

  • GABAA receptors are crucial for fast neuronal inhibition in the brain.
  • These receptors are targets for major drugs treating anxiety, insomnia, and anesthesia.
  • Understanding drug interactions at a structural level has been limited until recently.

Purpose of the Study:

  • To review recent structural pharmacology of GABAA receptors.
  • To highlight how key drug classes and natural products interact with these receptors.
  • To focus on synaptic GABAA receptor subunit assemblies.

Main Methods:

  • Review of recent structural biology studies.
  • Analysis of molecular interactions between drugs and GABAA receptors.
  • Focus on cryo-electron microscopy and X-ray crystallography data.

Main Results:

  • Recent structural data elucidate binding sites and mechanisms of action for various drugs.
  • Specific subunit assemblies at synapses have been characterized structurally.
  • Insights into how positive modulators interact with the GABAA receptor have been gained.

Conclusions:

  • Structural information provides a foundation for understanding GABAA receptor pharmacology.
  • This knowledge facilitates structure-guided drug design for neurological disorders.
  • Future research can explore receptor dynamics and develop novel therapeutics.