Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1-ynyl)-[11C]benzyl]-morpholine: evaluation of a potential PET ligand

The potent histamine H(3) receptor antagonist JNJ-10181457 (1) was successfully labeled with (11)C in a novel one-pot reaction sequence, with high chemical yield (decay-corrected yield, 28+/-8%) and high specific radioactivity (56+/-26 GBq/mumol). The binding of [(11)C]1 to H(3) receptors was studie...

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Veröffentlicht in:	Nuclear medicine and biology 2006-08, Vol.33 (6), p.801-810
Hauptverfasser:	Airaksinen, Anu J, Jablonowski, Jill A, van der Mey, Margreet, Barbier, Ann J, Klok, Rob P, Verbeek, Joost, Schuit, Robert, Herscheid, Jacobus D M, Leysen, Josee E, Carruthers, Nicholas I, Lammertsma, Adriaan A, Windhorst, Albert D
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Autoradiography Brain - metabolism Carbon Radioisotopes Histamine Antagonists - chemical synthesis Histamine Antagonists - pharmacokinetics Ligands Mice Mice, Inbred BALB C Mice, Inbred C57BL Morpholines - chemical synthesis Morpholines - pharmacokinetics Piperidines - chemical synthesis Piperidines - pharmacokinetics Positron-Emission Tomography Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - pharmacokinetics Rats Receptors, Histamine H3 - metabolism Tissue Distribution
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