Abstract
Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[(18)F]fluoroethyltosylate ([(18)F]FETos) was carried out in yields of approximately 90% synthesizing [(18)F]MHMZ in a specific activity of approximately 50MBq/nmol with a starting activity of approximately 3GBq. Overall radiochemical yield including [(18)F]FETos synthon synthesis, [(18)F]fluoroalkylation and preparing the injectable [(18)F]MHMZ solution was 42% within a synthesis time of approximately 100 min. The novel compound showed excellent specific binding to the 5-HT(2A) receptor (K(i)=9.0 nM) in vitro and promising in vivo characteristics.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Binding, Competitive
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Brain / diagnostic imaging
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Brain / metabolism
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Fluorine Radioisotopes / chemistry*
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Fluorobenzenes / chemical synthesis*
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Fluorobenzenes / chemistry
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Isotope Labeling
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Ketanserin / analogs & derivatives
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Ketanserin / pharmacokinetics
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Kinetics
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Radioligand Assay
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Radionuclide Imaging
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacokinetics
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Rats
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Receptor, Serotonin, 5-HT2A / metabolism
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Serotonin 5-HT2 Receptor Antagonists*
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Serotonin Antagonists / chemical synthesis*
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Serotonin Antagonists / pharmacokinetics
Substances
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2-(18F)fluoro-ethoxy-3-methoxyphenyl)-1-(2-(4-fluoro-phenyl)ethyl-4-piperidine-methanol
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Fluorine Radioisotopes
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Fluorobenzenes
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Piperidines
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Radiopharmaceuticals
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Receptor, Serotonin, 5-HT2A
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Serotonin 5-HT2 Receptor Antagonists
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Serotonin Antagonists
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altanserin
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Ketanserin
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volinanserin