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Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.


ABSTRACT: Selective ?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 ?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.

SUBMITTER: Motel WC 

PROVIDER: S-EPMC3919026 | biostudies-literature | 2013 Dec

REPOSITORIES: biostudies-literature

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Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.

Motel William C WC   Healy Jason R JR   Viard Eddy E   Pouw Buddy B   Martin Kelly K   Matsumoto Rae R RR   Coop Andrew A  

Bioorganic & medicinal chemistry letters 20131015 24


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. ...[more]

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