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Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
GPCR Desensitization01:12

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

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...
The Two-State Receptor Model01:29

The Two-State Receptor Model

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 one...
CNS Depressants: Alcohol and Nicotine01:27

CNS Depressants: Alcohol and Nicotine

Ethanol, a clear colorless alcohol, has been consumed by humans for millennia, but its effects on the body are far from benign. At lower doses, it induces decreased inhibitions and loquaciousness, leading to its social appeal. However, it can cause severe consequences at higher doses, such as coma and respiratory depression, due to its zero-order elimination kinetics. Chronic ethanol abuse wreaks havoc on multiple organ systems, particularly the CNS and the liver. Abrupt cessation of ethanol...
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...

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Related Experiment Video

Updated: Jun 29, 2026

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

Recombinant GABAA receptor function and ethanol

E Sigel1, R Baur, P Malherbe

  • 1Institute of Pharmacology, University of Bern, Switzerland.

FEBS Letters
|June 14, 1993
PubMed
Summary
This summary is machine-generated.

Ethanol only stimulated GABA receptors at high concentrations (>60 mM), with no difference observed between GABAA receptor variants containing different gamma 2 subunit splice variants. This suggests splice variants do not alter ethanol

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Chronic Intermittent Ethanol Vapor Exposure Paired with Two-Bottle Choice to Model Alcohol Use Disorder
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Chronic Intermittent Ethanol Vapor Exposure Paired with Two-Bottle Choice to Model Alcohol Use Disorder

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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

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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
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Chronic Intermittent Ethanol Vapor Exposure Paired with Two-Bottle Choice to Model Alcohol Use Disorder
05:12

Chronic Intermittent Ethanol Vapor Exposure Paired with Two-Bottle Choice to Model Alcohol Use Disorder

Published on: June 23, 2023

Area of Science:

  • Neuroscience
  • Molecular Biology
  • Pharmacology

Background:

  • GABAA receptors are crucial inhibitory neurotransmitter receptors in the brain.
  • Ethanol is known to modulate GABAA receptor function, but the precise mechanisms and subunit-specific effects are not fully understood.
  • Alternative splicing of GABAA receptor subunits, such as the gamma 2 subunit, can generate different receptor variants with potentially distinct pharmacological properties.

Purpose of the Study:

  • To investigate the effects of ethanol on GABAA receptor function.
  • To determine if alternative splicing of the gamma 2 subunit (gamma 2S vs. gamma 2L) influences the GABAA receptor's response to ethanol.
  • To characterize the ethanol sensitivity of different GABAA receptor subunit combinations expressed in Xenopus oocytes.

Main Methods:

  • Cloned subunits of rat brain GABAA receptors were expressed in Xenopus oocytes.
  • GABA-induced chloride currents were measured in the presence of varying ethanol concentrations.
  • Comparisons were made between receptor constructs containing either the gamma 2S or gamma 2L subunit variant.

Main Results:

  • A significant stimulation of GABA-induced chloride currents by ethanol was observed only at high concentrations (greater than 60 mM).
  • No significant difference in ethanol responsiveness was detected between GABAA receptor combinations expressing the gamma 2S subunit variant compared to those expressing the gamma 2L subunit variant.
  • The tested GABAA receptor subunit combinations showed limited sensitivity to ethanol within the tested concentration range.

Conclusions:

  • Alternative splicing of the gamma 2 subunit (gamma 2S vs. gamma 2L) does not appear to significantly alter the ethanol sensitivity of the expressed GABAA receptors.
  • High ethanol concentrations are required to elicit a significant modulatory effect on the studied GABAA receptor subtypes.
  • These findings contribute to understanding the molecular basis of ethanol's action on GABAA receptors and highlight the limited role of gamma 2 subunit splice variants in this interaction.