Abstract
The mechanisms of interaction between lobeline and the dopamine transporter (DAT) or the vesicular monoamine transporter (VMAT-2) are not clear. The goal of this study was to elucidate the effects of lobeline on these transporters in a cell system co-expressing the DAT and VMAT-2. Lobeline caused release of [(3)H]dopamine to a similar extent as reserpine (VMAT-2 inhibitor), but was less efficacious than methamphetamine or dopamine. Additionally, lobeline decreased the [(3)H]dopamine-releasing effects of methamphetamine, unlike reserpine which increased release by methamphetamine. These results suggest that lobeline has unique properties at the DAT and VMAT-2 which may make it useful as a pharmacotherapeutic to treat methamphetamine abuse.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Amphetamine-Related Disorders / drug therapy
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Cell Line
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Cocaine / analogs & derivatives
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Cocaine / pharmacology
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Dopamine / metabolism*
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Dopamine / pharmacology
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Dopamine Agents / pharmacology*
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Dopamine Plasma Membrane Transport Proteins / antagonists & inhibitors
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Dopamine Plasma Membrane Transport Proteins / metabolism*
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Dopamine Uptake Inhibitors / pharmacology
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Humans
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Lobeline / pharmacology*
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Methamphetamine / pharmacology*
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Nomifensine / pharmacology
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Reserpine / pharmacology
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Vesicular Monoamine Transport Proteins / antagonists & inhibitors
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Vesicular Monoamine Transport Proteins / metabolism*
Substances
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Dopamine Agents
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Dopamine Plasma Membrane Transport Proteins
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Dopamine Uptake Inhibitors
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SLC18A2 protein, human
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Vesicular Monoamine Transport Proteins
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Nomifensine
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Methamphetamine
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2beta-carbomethoxy-3beta-(4-iodophenyl)tropane
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Reserpine
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Lobeline
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Cocaine
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Dopamine