GBR 12935 dihydrochloride

GBR 12935 dihydrochloride is a potent and selective inhibitor of dopamine uptake (KD = 5.5 nM in rat striatal membranes). GBR 12935 dihydrochloride also inhibit dopamine uptake into brain synaptic vesicles. The binding of GBR-12935 to CYP2D6 was decreased partially by substrates or inhibitors of CYP2D isoforms. In vivo, GBR 12935 elevated locomotion to a greater extent in C57BL/6J mice at the maximally active dose of 10 mg/kg.