GBR-12909

GBR-12909 is a potent and selective inhibitor of dopamine uptake (Ki = 1 nM). It inhibits dopamine uptake in tissue slices obtained from rat neostriatum at nanomolar concentrations. GBR-12909 (10 mg/kg IP) produces a dose-dependent decrease in the binding of cocaine to the dopamine transporter in rats. It antagonizes the ability of cocaine to elevate extracellular dopamine. It is also a potent blocker of cardiac hERG, sodium and calcium channels and shows cardiac antiarrhythmic properties. It is a potent ligand for sigma receptor. Regulators of sigma receptors are suggested to show activity against COVID-19, based on viral assay screens