Abstract
[3H]2-beta-carbomethoxy-3-beta-[4'-iodophenyl]tropane (beta-CIT) was prepared and evaluated. With rat forebrain tissue, [3H]beta-CIT showed high affinity for dopamine transporters (DAT), with selectivity for DAT over norepinephrine transporters, but not serotonin transporters, as well as DAT-stereoselectivity with beta-CIT, amphetamine and methylphenidate. Affinity and selectivity for 53 compounds assayed with [3H]beta-CIT and standard DAT radioligand [3H]GBR-12935 were highly correlated (r0.95). [3H]beta-CIT is proposed as a useful, high-affinity DAT radioprobe.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amphetamine / chemistry
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Amphetamine / metabolism
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Animals
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Autoradiography
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Binding, Competitive / drug effects
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Brain / metabolism
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Carrier Proteins / metabolism
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Cocaine / analogs & derivatives*
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Cocaine / chemistry
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Cocaine / metabolism
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Corpus Striatum / metabolism
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Dopamine Plasma Membrane Transport Proteins
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Dopamine Uptake Inhibitors / pharmacology
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Male
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Membrane Glycoproteins / metabolism
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Membrane Transport Proteins*
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Methylphenidate / chemistry
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Methylphenidate / metabolism
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Nerve Tissue Proteins*
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Piperazines / metabolism
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Piperazines / pharmacology
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Radioligand Assay
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Rats
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Rats, Sprague-Dawley
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Selective Serotonin Reuptake Inhibitors / pharmacology
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Serotonin Plasma Membrane Transport Proteins
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Stereoisomerism
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Tritium
Substances
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Carrier Proteins
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Dopamine Plasma Membrane Transport Proteins
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Dopamine Uptake Inhibitors
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Membrane Glycoproteins
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Membrane Transport Proteins
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Nerve Tissue Proteins
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Piperazines
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Serotonin Plasma Membrane Transport Proteins
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Serotonin Uptake Inhibitors
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Slc6a3 protein, rat
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Slc6a4 protein, rat
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Tritium
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Methylphenidate
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2beta-carbomethoxy-3beta-(4-iodophenyl)tropane
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vanoxerine
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1-(2 (diphenylmethoxy)ethyl)-4-(3-phenylpropyl)piperazine
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Amphetamine
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Cocaine