Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands

[摘要] Selective sigma(2) ligands continue to be an active target for medications to attenuate the effects of psychostimulants. In the course of our studies to determine the optimal substituents in the sigma(2)-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorophenyl)-4-phenethylpiperazine actually had preferentially increased affinity for dopamine transporters (DAT), yielding a highly selective DAT ligand. (C) 2013 Elsevier Ltd. All rights reserved.

[发布日期] 2013-12-15

[关键词] Sigma receptor;Dopamine transporter;Structure-activity relationships;Neurotransmitter;Cocaine;Methamphetamine