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Related Concept Videos

Antiepileptic Drugs: GABAergic Pathway Potentiators01:18

Antiepileptic Drugs: GABAergic Pathway Potentiators

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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.
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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...
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G-Protein Gated Ion Channels01:21

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GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
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Antiepileptic Drugs: Potassium Channel Activators01:20

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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...
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GPCR Desensitization01:12

GPCR Desensitization

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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...
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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Related Experiment Video

Updated: Feb 26, 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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KCTD12 modulation of GABA(B) receptor function.

Melody Li1, Carol J Milligan1, Haiyan Wang2

  • 1The Florey Institute of Neuroscience and Mental Health Parkville Victoria Australia.

Pharmacology Research & Perspectives
|July 18, 2017
PubMed
Summary
This summary is machine-generated.

Human KCTD12 speeds up GABAB receptor kinetics and enhances allosteric modulation. KCTD12 knockout mice show reduced seizure susceptibility and ethanol consumption, highlighting its physiological role in GABAB receptor modulation.

Keywords:
BaclofenCGP7930GABA(B)RKCTD12

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Area of Science:

  • Neuroscience
  • Molecular Pharmacology
  • GABAergic Signaling

Background:

  • Native GABAB receptors (GABABR) and their functional diversity are not fully understood, limiting the development of selective ligands.
  • Potassium channel tetramerization domain-containing protein 12 (KCTD12) is an auxiliary subunit that modulates GABABR function.

Purpose of the Study:

  • To characterize the effects of human KCTD12 on GABABR kinetics and pharmacology in vitro.
  • To investigate the in vivo function of KCTD12 by examining seizure susceptibility and ethanol consumption in a KCTD12 knockout mouse model.

Main Methods:

  • Automated electrophysiological assays were used to study GABABR-mediated GIRK channel kinetics and pharmacology.
  • Concentration-response curves were analyzed for agonists and a positive allosteric modulator (CGP7930).
  • KCTD12 knockout mice were subjected to pentylenetetrazole challenge and a two-bottle preference test for ethanol.

Main Results:

  • Human KCTD12 co-expression accelerated GABABR activation and desensitization kinetics.
  • KCTD12 did not alter the effects of GABA or baclofen but enhanced the potentiation by CGP7930.
  • KCTD12 knockout mice exhibited reduced seizure susceptibility and lower ethanol consumption at high concentrations.

Conclusions:

  • Human KCTD12 significantly alters GABABR kinetics and allosteric modulation in vitro.
  • The KCTD12-GABABR interaction has physiological relevance in vivo, impacting seizure susceptibility and ethanol consumption.
  • Targeting the KCTD12-GABABR interaction may offer a novel strategy for selective GABABR modulation.