CLP257 has been used as a K+- Cl- cotransporter 2 (KCC2) enhancer in human neuron culture.
Biochem/physiol Actions
In streptozotocin treated rats, by activating a K+- Cl- cotransporter 2 (KCC2) in the arginine-vasopressin neuron, CLP257 mediates ?-aminobutyric acid (GABA)ergic excitation. It is however inactive with KCC1, KCC3 and KCC4.
CLP257 is a selective K+-Cl− cotransporter KCC2 activator that restored impaired Cl− transport in neurons with reduced KCC2 activity. Apparently, CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.