Selective NKCC1 inhibitors for the treatment of brain disorders with defective chloride homeostasis
Annalisa Savardi, Danielle Walu Kasongo, Michal Rychlik, Marco Borgogno, Marco De Vivo, Laura Cancedda · FENS Forum 2024
Proper intracellular Cl concentration is fundamental for physiological brain development and function. Accordingly, the aberrant expression of Cl importer NKCC1 and/or exporter KCC2 is implicated in several brain conditions, including autism spectrum disorders (ASD), Down syndrome (DS), and drug-resistant epilepsy (DRE). Interestingly, NKCC1 inhibition rescues core symptoms of these brain conditions in rodent models and/or clinical trials. However, current NKCC1 inhibitors have diuretic effects by also inhibiting the kidney Cl transporter NKCC2. These diuretic effects pose critical health conc
ePoster · Neuroscience