Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands

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• 作者：William C. Motel ; Jason R. Healy ; Eddy Viard ; Buddy Pouw ; Kelly E. Martin ; Rae R. Matsumoto ; Andrew Coop
• 关键词：Sigma receptor ; Dopamine transporter ; Structure&ndash ; activity relationships ; Neurotransmitter ; Cocaine ; Methamphetamine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 December, 2013
• 年：2013
• 卷：23
• 期：24
• 页码：6920-6922
• 全文大小：271 K

文摘

Selective 蟽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 蟽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.