Neuronal K⁺-Cl^- cotransporter KCC2 as a promising drug target for epilepsy treatment.

ABSTRACT: Epilepsy is a prevalent neurological disorder characterized by unprovoked seizures. γ-Aminobutyric acid (GABA) serves as the primary fast inhibitory neurotransmitter in the brain, and GABA binding to the GABA_A receptor (GABA_AR) regulates Cl^- and bicarbonate (HCO₃^-) influx or efflux through the channel pore, leading to GABAergic inhibition or excitation, respectively. The neuron-specific K⁺-Cl^- cotransporter 2 (KCC2) is essential for maintaining a low intracellular Cl^- concentration, ensuring GABA_AR-mediated inhibition. Impaired KCC2 function results in GABAergic excitation associated with epileptic activity. Loss-of-function mutations and altered expression of KCC2 lead to elevated [Cl^-<

SUBMITTER: McMoneagle E 

PROVIDER: S-EPMC10770335 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature