Abstract
Cocaine and several sigma receptor ligands inhibit dopamine uptake via a common site. This is evidenced by a concentration-dependent inhibition of dopamine uptake and displacement of the binding of [3H]WIN 35,428 (also called CFT), a cocaine analog with high affinity for the dopamine transporter. Since several sigma receptor ligands have been shown to block the stimulant effects of cocaine, this site may serve as a target for future drug development to treat cocaine abuse.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Affinity Labels
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Animals
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Binding, Competitive / drug effects
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Carrier Proteins / metabolism
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Caudate Nucleus / drug effects
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Caudate Nucleus / metabolism*
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Cocaine / analogs & derivatives
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Cocaine / pharmacology*
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Dopamine / metabolism*
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Dopamine Plasma Membrane Transport Proteins
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In Vitro Techniques
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Kinetics
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Male
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Membrane Glycoproteins*
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Membrane Transport Proteins*
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Nerve Tissue Proteins / metabolism
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Putamen / drug effects
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Putamen / metabolism*
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Rats
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Rats, Sprague-Dawley
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Receptors, Dopamine / drug effects
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Receptors, Dopamine / metabolism
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Receptors, sigma / drug effects*
Substances
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Affinity Labels
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Carrier Proteins
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Dopamine Plasma Membrane Transport Proteins
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Membrane Glycoproteins
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Membrane Transport Proteins
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Nerve Tissue Proteins
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Receptors, Dopamine
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Receptors, sigma
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(1R-(exo,exo))-3-(4-fluorophenyl)-8-methyl-8- azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester
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Cocaine
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Dopamine