Abstract
A series of reboxetine analogs was synthesized and evaluated for in vitro binding as racemic mixtures. The best candidate (INER) was synthesized as the optically pure (S,S) enantiomer, labeled with iodine-123 and its in vivo binding determined by SPECT imaging in baboons. The in vivo specificity, selectivity, and kinetics of [123I]INER make it a promising agent for imaging NET in vivo by noninvasive SPECT imaging.
MeSH terms
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Adrenergic Uptake Inhibitors / chemical synthesis
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Adrenergic Uptake Inhibitors / pharmacology
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Animals
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Brain Chemistry / drug effects
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Female
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Indicators and Reagents
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Morpholines / chemical synthesis*
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Morpholines / pharmacology*
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Norepinephrine Plasma Membrane Transport Proteins / metabolism*
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Papio
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacology*
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Rats
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Reboxetine
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Stereoisomerism
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Tomography, Emission-Computed, Single-Photon*
Substances
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(123I)INER
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Adrenergic Uptake Inhibitors
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Indicators and Reagents
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Morpholines
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Norepinephrine Plasma Membrane Transport Proteins
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Radiopharmaceuticals
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Reboxetine