Abstract
The serotonin transporter radioligand [11C]-3-amino-4-(2-dimethylaminomethylphenylsulfanyl)-benzonitrile, or [11C]DASB, was examined in order to assess its potential for measuring fluctuations in endogenous serotonin concentrations with positron emission tomography. Binding characteristics of [11C]DASB and the propensity for serotonin to displace the tracer were explored in rat brain homogenates. Experiments showed that serotonin displaced [11C]DASB in vitro. Ex vivo experiments performed after tranylcypromine injection (3 or 15 mg/kg) showed a dose-dependent trend in radioactivity uptake and suggested that serotonin may compete with [11C]DASB for transporter binding.
Publication types
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Evaluation Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Aniline Compounds / pharmacokinetics*
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Aniline Compounds / therapeutic use*
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Animals
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Brain / diagnostic imaging*
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Brain / metabolism*
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Feasibility Studies
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Male
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Metabolic Clearance Rate
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Neurotransmitter Agents / metabolism
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Organ Specificity
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Positron-Emission Tomography / methods*
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Protein Binding
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Radiopharmaceuticals / pharmacokinetics
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Rats
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Rats, Sprague-Dawley
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Serotonin / metabolism*
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Sulfides / pharmacokinetics*
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Sulfides / therapeutic use*
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Tissue Distribution
Substances
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3-amino-4-(2-dimethylaminomethylphenylsulfanyl)benzonitrile
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Aniline Compounds
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Neurotransmitter Agents
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Radiopharmaceuticals
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Sulfides
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Serotonin