Chlorophenylpiperazine Analogues As High Affinity Dopamine Transporter Ligands

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2013 Nov 12

PMID 24211020

Authors

William C Motel

Jason R Healy

Eddy Viard

Buddy Pouw

Kelly Martin

Rae R Matsumoto

Andrew Coop

Affiliations

Soon will be listed here.

Abstract

Selective σ2 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 σ2-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.

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