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Gamma-aminobutyric acid type A receptors (GABAARs) are pivotal regulators of neuronal activity and brain function through the inhibition of signals. This chapter integrates key aspects of GABAAR biology, focusing on their activation, trafficking, regulation and implications in neurological disorders. GABAARs, composed of diverse subunits, exhibit varied pharmacological responses influenced by gamma-aminobutyric acid (GABA) binding, leading to chloride ion movement and modulation of neuronal membrane potential. Allosteric modulators like benzodiazepines enhance GABAAR function, impacting neurotransmission dynamics. GABAARs undergo dynamic trafficking processes, shuttling between intracellular compartments and the plasma membrane, crucial for modulating brain excitability and synaptic inhibition. Dysregulation of GABAAR trafficking contributes to synaptic imbalance in neurodegenerative disorders such as epilepsy, schizophrenia and Alzheimer’s disease, altering synaptic strength and neuronal viability. Understanding GABAAR biology provides insights into therapeutic strategies targeting GABAergic signalling for restoring synaptic homeostasis in neurological conditions.

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Activation Mechanisms, Trafficking and Signalling of GABAA Receptors

  • 章节

  • 发表日期：

    2025年

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  • Mohamed Shalaby,
  • Vijay K. Pabbathi,
  • Samantha L. McLean,
  • Sriharsha Kantamneni

摘要

Gamma-aminobutyric acid type A receptors (GABAARs) are pivotal regulators of neuronal activity and brain function through the inhibition of signals. This chapter integrates key aspects of GABAAR biology, focusing on their activation, trafficking, regulation and implications in neurological disorders. GABAARs, composed of diverse subunits, exhibit varied pharmacological responses influenced by gamma-aminobutyric acid (GABA) binding, leading to chloride ion movement and modulation of neuronal membrane potential. Allosteric modulators like benzodiazepines enhance GABAAR function, impacting neurotransmission dynamics. GABAARs undergo dynamic trafficking processes, shuttling between intracellular compartments and the plasma membrane, crucial for modulating brain excitability and synaptic inhibition. Dysregulation of GABAAR trafficking contributes to synaptic imbalance in neurodegenerative disorders such as epilepsy, schizophrenia and Alzheimer’s disease, altering synaptic strength and neuronal viability. Understanding GABAAR biology provides insights into therapeutic strategies targeting GABAergic signalling for restoring synaptic homeostasis in neurological conditions.