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.
Keywords:
Cocaine; Dopamine transporter; Methamphetamine; Neurotransmitter; Sigma receptor; Structure–activity relationships.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Dopamine Plasma Membrane Transport Proteins / chemistry*
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Dopamine Plasma Membrane Transport Proteins / metabolism
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Ligands*
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Norepinephrine Plasma Membrane Transport Proteins / chemistry
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Norepinephrine Plasma Membrane Transport Proteins / metabolism
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Piperazines / chemistry*
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Piperazines / metabolism
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Protein Binding
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Receptors, sigma / chemistry
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Receptors, sigma / metabolism
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Serotonin Plasma Membrane Transport Proteins / chemistry
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Serotonin Plasma Membrane Transport Proteins / metabolism
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Structure-Activity Relationship
Substances
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Dopamine Plasma Membrane Transport Proteins
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Ligands
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Norepinephrine Plasma Membrane Transport Proteins
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Piperazines
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Receptors, sigma
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Serotonin Plasma Membrane Transport Proteins
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phenylpiperazine