Abstract
5-Methyl-6-nitroquipazine, a novel analogue of the potent and selective serotonin transporter inhibitor 6-nitroquipazine was synthesized and radiolabeled with tritium and the positron emitter carbon-11. [3H]5-methyl-6-nitroquipazine was found to have a K(d)=51+/-7 pM. The high affinity and the facile labeling of [11C]5-methyl-6-nitroquipazine makes it a promising radioligand for visualization of the serotonin transporter with positron emission tomography.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Carbon Radioisotopes
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Carrier Proteins / antagonists & inhibitors
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Ligands
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Membrane Glycoproteins / antagonists & inhibitors
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Membrane Transport Proteins*
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Nerve Tissue Proteins*
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Prefrontal Cortex / metabolism
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Quipazine / analogs & derivatives
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Quipazine / chemical synthesis
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Quipazine / metabolism
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Quipazine / pharmacology
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Radiopharmaceuticals / chemical synthesis
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Radiopharmaceuticals / metabolism
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Radiopharmaceuticals / pharmacology
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Rats
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Serotonin Antagonists / chemical synthesis*
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Serotonin Antagonists / metabolism
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Serotonin Antagonists / pharmacology
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Serotonin Plasma Membrane Transport Proteins
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Structure-Activity Relationship
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Tritium
Substances
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5-methyl-6-nitroquipazine
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Carbon Radioisotopes
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Carrier Proteins
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Ligands
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Membrane Glycoproteins
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Membrane Transport Proteins
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Nerve Tissue Proteins
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Radiopharmaceuticals
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Serotonin Antagonists
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Serotonin Plasma Membrane Transport Proteins
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Slc6a4 protein, rat
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Tritium
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Quipazine