David R. Elmaleh

Synthesis and evaluation of novel-N-[2-(bis-aryl-methoxy)ethyl-N'-aralkyl-α,ω-alkanediamines as potent and selective dopamine reuptake inhibitors : SECO analogs of GBR12935 and GBR12909

Abstract A series of analogs of the N-[2-bis arylmethoxy]-N′-phenylpropyl-piperazines GBR12909 and 12935 was synthesized and evaluated as inhibitors of synaptic monoamine transporters. The data indicated that all of the new compounds demonstrated a selectivity for the dopamine transporter compared to the other monoamine transporters with IC50 values approaching 10 nM. The results suggest that the internal piperazine moiety is not required for activity and may be replaced with a more flexible diamine unit.