CLP257 is a selective activator of the K+-Cl cotransporter KCC2, exhibiting an EC50 of 616 nM. It specifically enhances Cl transport in neurons with reduced KCC2 activity while showing no effects on NKCC1, GABAA receptors, KCC1, KCC3, or KCC4. This compound is shown to alleviate hypersensitivity in neuropathic pain models in rats and modulates KCC2 protein turnover at the plasmalemmal level post-translationally. CLP257 is valuable for research into neuron excitability and synaptic transmission.
CLP257 is a selective activator of the K+-Cl cotransporter KCC2, exhibiting an EC50 of 616 nM. It specifically enhances Cl transport in neurons with reduced KCC2 activity while showing no effects on NKCC1, GABAA receptors, KCC1, KCC3, or KCC4. This compound is shown to alleviate hypersensitivity in neuropathic pain models in rats and modulates KCC2 protein turnover at the plasmalemmal level post-translationally. CLP257 is valuable for research into neuron excitability and synaptic transmission.
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