Target intelligence / Profile preview

Potassium-chloride co-transporter 2 (KCC2)

Target
KCC2
Molecular classification
Solute Carrier Family 12, Cation-Chloride Cotransporter, Transporter
01

Overview

Potassium-chloride co-transporter 2 (KCC2), encoded by the SLC12A5 gene, is a member of the SLC12 family of cation-chloride cotransporters. It mediates the coupled export of potassium (K⁺) and chloride (Cl⁻) ions across the plasma membrane, maintaining low intracellular chloride concentrations. This is essential for cell volume regulation and inhibitory neurotransmission mediated by GABA and glycine. Dysfunction or downregulation of KCC2 is implicated in neurological disorders like epilepsy and neuropathic pain.

Other names
SLC12A5
02

Mechanism of action

Inhibition of KCC2 increases intracellular chloride concentration, reducing the hyperpolarizing effect of GABAergic signaling.

03

Biological functions

Ion transportCell volume regulationGABAergic neurotransmissionInhibitory neurotransmission
04

Disease associations

EpilepsyNeuropathic pain
05

Safety considerations

Pharmacological targeting remains challenging due to limited selectivity of available inhibitors.Dysregulation can lead to neuronal hyperexcitability.
06

Interacting drugs

Bumetanide

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