Abstract
The title compound ([3H]INBMeO) was prepared by an O,O-dimethylation reaction of a t-BOC protected diphenolic precursor using no carrier added tritiated iodomethane in DMF with K(2)CO(3). Removal of the t-BOC protecting group and purification by HPLC afforded an overall yield of 43%, with a radiochemical purity of 99% and specific activity of 164Ci/mmol. The new radioligand was suitable for labeling human 5-HT(2A) receptors in two heterologous cell lines and had about 20-fold higher affinity than [(3)H]ketanserin.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Binding Sites
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Cell Line
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Cell Line, Tumor
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DNA-Binding Proteins
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Ethylamines / chemical synthesis*
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Ethylamines / metabolism
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Humans
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Intracellular Signaling Peptides and Proteins / genetics
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Intracellular Signaling Peptides and Proteins / metabolism
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Iodine Radioisotopes / metabolism
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Iodobenzenes / chemical synthesis*
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Iodobenzenes / metabolism
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Ketanserin / metabolism
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Ketanserin / pharmacology
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Nuclear Proteins / biosynthesis
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Nuclear Proteins / genetics
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Nuclear Proteins / metabolism
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Radioligand Assay
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / metabolism*
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Receptor, Serotonin, 5-HT2A / metabolism*
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Serotonin 5-HT2 Receptor Agonists*
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Serotonin 5-HT2 Receptor Antagonists
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Tritium
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Tumor Necrosis Factor alpha-Induced Protein 3
Substances
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DNA-Binding Proteins
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Ethylamines
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Intracellular Signaling Peptides and Proteins
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Iodine Radioisotopes
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Iodobenzenes
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N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine
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Nuclear Proteins
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Radiopharmaceuticals
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Receptor, Serotonin, 5-HT2A
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Serotonin 5-HT2 Receptor Agonists
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Serotonin 5-HT2 Receptor Antagonists
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Tritium
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Ketanserin
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TNFAIP3 protein, human
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Tumor Necrosis Factor alpha-Induced Protein 3