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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.
Aggression01:47

Aggression

Humans engage in aggression when they seek to cause harm or pain to another person. Aggression takes two forms depending on one’s motives: hostile or instrumental. Hostile aggression is motivated by feelings of anger with intent to cause pain; a fight in a bar with a stranger is an example of hostile aggression. In contrast, instrumental aggression is motivated by achieving a goal and does not necessarily involve intent to cause pain (Berkowitz, 1993); a contract killer who murders for hire...
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high affinity and are together...
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...
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...
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: Jul 16, 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

GABA-B receptor activation and conflict behaviour.

C E Ketelaars1, E L Bollen, H Rigter

  • 1Dep. of Pharmacology, Medical Faculty, Erasmus University Rotterdam, The Netherlands.

Life Sciences
|January 1, 1988
PubMed
Summary

Baclofen, a GABA-B agonist, does not appear to affect the GABA-A/benzodiazepine receptor complex. This suggests baclofen

Area of Science:

  • Neuropharmacology
  • Behavioral Neuroscience
  • Receptor Binding Assays

Background:

  • Baclofen (GABA-B agonist) and benzodiazepines (GABA-A modulators) affect conflict behavior.
  • Baclofen's mechanism may involve indirect GABA-A/benzodiazepine receptor complex interaction.
  • Previous studies show baclofen and diazepam influence punished behavior.

Purpose of the Study:

  • To investigate if baclofen's behavioral effects are mediated via the GABA-A/benzodiazepine receptor complex.
  • To determine the impact of baclofen pretreatment on [3H]-diazepam binding.
  • To examine receptor binding in rat cortical and cerebellar membranes.

Main Methods:

  • Rat behavioral tests (Geller-Seifter, Vogel's conflict test).
  • Pretreatment of rats with baclofen.

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BS3 Chemical Crosslinking Assay: Evaluating the Effect of Chronic Stress on Cell Surface GABAA Receptor Presentation in the Rodent Brain
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BS3 Chemical Crosslinking Assay: Evaluating the Effect of Chronic Stress on Cell Surface GABAA Receptor Presentation in the Rodent Brain

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Last Updated: Jul 16, 2026

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

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BS3 Chemical Crosslinking Assay: Evaluating the Effect of Chronic Stress on Cell Surface GABAA Receptor Presentation in the Rodent Brain

Published on: May 26, 2023

  • [3H]-diazepam binding assays on rat cortical and cerebellar membranes (washed and unwashed).
  • Inclusion of bicuculline in incubation mixtures.

    • Main Results:

    • Baclofen pretreatment increased Bmax in washed cerebellar membranes with bicuculline present.
    • No significant effect of baclofen pretreatment on [3H]-diazepam binding in cortical membranes.
    • Baclofen did not alter diazepam binding in unwashed membranes or washed cerebellar membranes without bicuculline.

    Conclusions:

    • Baclofen's effects on conflict behavior extinction and punished drinking are unlikely mediated by the GABA-A/benzodiazepine receptor complex.
    • The study provides evidence against indirect modulation of GABA-A receptors by baclofen.
    • Findings suggest distinct mechanisms for GABA-B and GABA-A receptor modulation of behavior.