K+/Cl- Cotransporter 2

K+/Cl- cotransporter 2 (KCC2, SLC12A5) is a neuron specific membrane protein that is responsible for the maintenance of the low intracellular Cl- concentration in adult neurons and has a key role in GABAA and glycine signaling.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
3888 VU 0240551
KCC2 inhibitor
4719 VU 0463271
Potent and selective KCC2 inhibitor

Activators

Cat No Product Name / Activity
5242 CLP 257
Selective KCC2 activator

K+/Cl- cotransporter 2 (KCC2, SLC12A5) is a neuron specific membrane protein that is responsible for the maintenance of the low intracellular Cl- concentration in adult neurons. It is one of four members of the solute carrier 12 (SLC12) family of electroneutral cation-chloride cotransporters and is expressed in most mature mammalian central neurons. KCC2 maintains the intracellular Cl- concentration by using energy from the electrochemical K+ gradient across the plasma membrane to drive Cl- efflux from the cell.

KCC2 has a key role in GABAA and glycine signaling, since low intracellular Cl- concentrations are necessary for the generation of inhibitory post-synaptic potentials (IPSPs) by GABAA and glycine receptors. Modulation of KCC2 function may therefore impact the effectiveness of GABA signaling. Indeed, prolonged intense neuronal firing, as seen in pathological conditions such as epilepsy, spinal cord injury or neuropathic pain, results in down-regulation of KCC2 and affects GABA signaling. Activation of KCC2 has been shown to alleviate pain in a rat model.

External sources of pharmacological information for K+/Cl- Cotransporter 2 :

    Literature for K+/Cl- Cotransporter 2

    GABA Receptors

    GABA Receptors Scientific Review

    Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.

    K+/Cl-Cotransporter 2 Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    SLC12A5 Human SLC12A5 NM_020708 Q9H2X9
    Mouse Slc12a5 NM_020333 Q91V14
    Rat Slc12a5 NM_134363 NP_599190