GBR-12783

GBR-12783 is a potent and highly selective small molecule inhibitor of dopamine uptake, classified as a dopamine reuptake inhibitor. It acts by competitively inhibiting the dopamine transporter (DAT), thereby blocking the reuptake of dopamine into presynaptic neurons and increasing extracellular dopamine levels. The compound demonstrates high selectivity for the inhibition of dopamine uptake over norepinephrine and serotonin, with an IC50 for [3H]-dopamine uptake in rat striatal synaptosomes of approximately 1.8 nM, making it significantly less effective against norepinephrine (18–90 times less) and serotonin (85–300 times less). Its effects are rapid in onset and long-lasting following administration in animal models[1][2][7]. Originally developed by DSM BV, GBR-12783 has been used primarily as a research tool to study dopaminergic neurotransmission[5][7].

Other names

1-(2-(diphenylmethoxy)ethyl)-4-(3-phenyl-2-propenyl)piperazine1-(2-benzhydryloxyethyl)-4-cinnamylpiperazineGBR 12783 dihydrochlorideGBR12783 dihydrochlorideGBR-12783 dihydrochloride