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.
K+/Cl-Cotransporter 2 Inhibitors |
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|---|---|
| Cat. No. | Product Name / Activity |
| 4719 | VU 0463271 |
| Potent and selective KCC2 inhibitor | |
K+/Cl-Cotransporter 2 Activators |
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| Cat. No. | Product Name / Activity |
| 5242 | CLP 257 |
| Selective KCC2 activator | |
| 6758 | CLP 290 |
| K+/Cl- cotransporter 2 (KCC2) activator; orally bioavailable prodrug of CLP 257 (Cat. No.5242) | |
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
Tocris offers the following scientific literature for K+/Cl- Cotransporter 2 to showcase our products. We invite you to request* your copy today!
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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.
Our GABA review gives an overview of the structure and function of the GABA receptors, as well as highlighting pharmacological ligands for their study.
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