Selective KCC2 K+-Cl- cotransporter activator (EC50 = 616 nM). Exhibits selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, as well as 55 other receptors. Enhances Cl- transport and increases KCC2 plasma membrane expression in spinal slices with reduced KCC2 function. Alleviates hypersensitivity in rats with peripheral nerve injury.
Gagnon et al (2013) Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat.Med. 19 1524 PMID:24097188