Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands

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 discovere...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2013-12, Vol.23 (24), p.6920-6922
Hauptverfasser: Motel, William C., Healy, Jason R., Viard, Eddy, Pouw, Buddy, Martin, Kelly E., Matsumoto, Rae R., Coop, Andrew
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Sprache:eng
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Zusammenfassung: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.09.038