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Concept

Récepteur GABAA

Résumé

Les récepteurs GABA de type A (GABAA) sont des récepteurs canaux des membranes des neurones qui sont activés par fixation de l'acide γ-aminobutyrique (GABA). Ces récepteurs ionotropes ont une grande importance en physiologie des mammifères, le GABA étant le principal neurotransmetteur inhibiteur dans le cerveau. Ces canaux partagent des propriétés structurales importantes avec les récepteurs à l'acétylcholine ionotropes et les récepteurs à la sérotonine 5HT-3 ionotropes. Les canaux GABAA sont la cible de plusieurs molécules pharmacologiques de première importance sur le plan de la santé humaine :

les benzodiazépines, comme le diazépam.
les barbituriques
les alcools, ce qui explique leurs effets anesthésiques
Les anesthésiques généraux ** volatils (gazeux), comme l'halothane ou le chloroforme ** intraveineux, dits hypnotiques, comme le propofol
convulsivant, comme la picrotoxine
le gamma-hydroxybutyrate

Canal chlorure Le récepteur GABA est composé de cinq

Source officielle

https://fr.wikipedia.org/wiki/R%C3%A9cepteur_GABAA

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Concepts associés (52)

Les benzodiazépines (BZD) sont une classe de composés organiques formés d'un cycle benzénique fusionné à un cycle diazépine. On classe aussi parmi les benzodiazépines les thiénodiazépines, qui à la

L'acide γ-aminobutyrique, souvent abrégé en GABA (de l'anglais gamma-aminobutyric acid), est le principal neurotransmetteur inhibiteur du système nerveux central chez les mammifères et les

Un récepteur ionotrope sensible à un ligand est une protéine membranaire qui ouvre un canal ionique grâce à la liaison d'un messager chimique ou neurotransmetteur. Ils sont généralement sélectifs à u

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This course introduces the student to the fudamentals of pharmacology, pharmacokinetics and drug-receptor interactions. It discusses also pharmacogenetics and chronopharmacology, to exemplify the challenges of personalized medicine.

The course starts with fundamentals of electrical - and chemical signaling in neurons. Students then learn how neurons in the brain receive and process sensory information, and how other neurons control the behavior of an animal. Furthermore, memory, learning, and brain disorders will be introduced.

Presentation of selected signalling pathways with emphasis on both the mechanism of action of the molecules involved, molecular interactions and the role of their spatio-temporal organization within the cell, considering cellular dimensions and conditions.

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Séances de cours associées (26)

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A conditional GABAergic synaptic vesicle marker for Drosophila

Brian Donal McCabe

Background: Throughout the animal kingdom, GABA is the principal inhibitory neurotransmitter of the nervous system. It is essential for maintaining the homeostatic balance between excitation and inhibition required for the brain to operate normally. Identification of GABAergic neurons and their GABA release sites are thus essential for understanding how the brain regulates the excitability of neurons and the activity of neural circuits responsible for numerous aspects of brain function including information processing, locomotion, learning, memory, and synaptic plasticity, among others. New method: Since the structure and features of GABA synapses are critical to understanding their function within specific neural circuits of interest, here we developed and characterized a conditional marker of GABAergic synaptic vesicles for Drosophila, 9XV5-vGAT. Results: 9XV5-vGAT is validated for conditionality of expression, specificity for localization to synaptic vesicles, specificity for expression in GABAergic neurons, and functionality. Its utility for GABAergic neurotransmitter phenotyping and identification of GABA release sites was verified for ellipsoid body neurons of the central complex. In combination with previously reported conditional SV markers for acetylcholine and glutamate, 9XV5-vGAT was used to demonstrate fast neurotransmitter phenotyping of subesophageal ganglion neurons. Comparison with existing methods: This method is an alternative to single cell transcriptomics for neurotransmitter phenotyping and can be applied to any neurons of interest represented by a binary transcription system driver. Conclusion: A conditional GABAergic synaptic vesicle marker has been developed and validated for GABA neurotransmitter phenotyping and subcellular localization of GABAergic synaptic vesicles.

2022

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Cell-type-specific nicotinic input disinhibits mouse barrel cortex during active sensing

Sylvain Crochet, Célia Roxane Gasselin, Benoît Hohl, Carl Petersen

Fast synaptic transmission relies upon the activation of ionotropic receptors by neurotransmitter release to evoke postsynaptic potentials. Glutamate and GABA play dominant roles in driving highly dynamic activity in synaptically connected neuronal circuits, but ionotropic receptors for other neurotransmitters are also expressed in the neocortex, including nicotinic receptors, which are non-selective cation channels gated by acetylcholine. To study the function of non-glutamatergic excitation in neocortex, we used two-photon microscopy to target whole-cell membrane potential recordings to different types of genetically defined neurons in layer 2/3 of primary somatosensory barrel cortex in awake head-restrained mice combined with pharmacological and optogenetic manipulations. Here, we report a prominent nicotinic input, which selectively depolarizes a subtype of GABAergic neuron expressing vasoactive intestinal peptide leading to disinhibition during active sensorimotor processing. Nicotinic disinhibition of somatosensory cortex during active sensing might contribute importantly to integration of top-down and motor-related signals necessary for tactile perception and learning.

CELL PRESS2021

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Short-term ionic plasticity at GABAergic synapses

Henry Markram

Fast synaptic inhibition in the brain is mediated by the pre-synaptic release of the neurotransmitter γ-Aminobutyric acid (GABA)and the post-synaptic activation of GABA-sensitive ionotropic receptors. As with excitatory synapses, it is being increasinly appreciated that a variety of plastic processes occur at inhibitory synapses, which operate over a range of timescales. Here we examine a form of activity-dependent plasticity that is somewhat unique to GABAergic transmission. This involves short-lasting changes to the ionic driving force for the post-synaptic receptors, a process referred to as short-term ionic plasticity. These changes are directly related to the history of activity at inhibitory synapses and are influenced by a variety of factors including the location of the synapse and the post-synaptic cell's ion regulation mechanisms. We explore the processes underlying this form of plasticity, when and where it can occur, and how it is likely to impact network activity.

2012

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