CAS: 1391737-01-1

VU0463271: KCC2 antagonist, IC50 61 nM, >100x selective over NKCC1, inactive on other GPCRs, channels, transporters.

VU0463271

VU0463271 is a benzodiazepine receptor ligand that has been shown to inhibit neuronal function in vitro. VU0463271 has been found to increase the membrane potential of cells in a fluorescence assay and inhibits actin polymerization in vitro. It also inhibits the chronic treatment-induced decrease in chloride currents, which suggests a possible therapeutic effect for epilepsy. In vivo, VU0463271 has been found to have an inhibitory effect on the hippocampus of mice, as well as on extracellular chloride levels. This drug can be used for the treatment of neurological disorders such as epilepsy or anxiety.