PMID: 9553162May 30, 1998Paper

carbonyl-11C]Desmethyl-WAY-100635 (DWAY) is a potent and selective radioligand for central 5-HT1A receptors in vitro and in vivo

European Journal of Nuclear Medicine
V W PikeL Farde

Abstract

[carbonyl-11C]Desmethyl-WAY-100635 (DWAY) is possibly a low-level metabolite appearing in plasma after intravenous administration of [carbonyl-11C]WAY-100635 to human subjects for positron emission tomographic (PET) imaging of brain 5-HT1A receptors. In this study we set out to assess the ability of DWAY to enter brain in vivo and to elucidate its possible interaction with 5-HT1A receptors. Desmethyl-WAY-100635 was labelled efficiently with carbon-11 (t1/2 = 20.4 min) in high specific radioactivity by reaction of its descyclohexanecarbonyl analogue with [carbonyl-11C]cyclohexanecarbonyl chloride. The product was separated in high radiochemical purity by high-performance liquid chromatography (HPLC) and formulated for intravenous injection. Rats were injected intravenously with DWAY, sacrificed at known times and dissected to establish radioactivity content in brain tissues. At 60 min after injection, the ratios of radioactivity concentration in each brain region to that in cerebellum correlated with previous in vitro and in vivo measures of 5-HT1A receptor density. The highest ratio was about 22 in hippocampus. Radioactivity cleared rapidly from plasma; HPLC analysis revealed that DWAY represented 55% of the radioactivity in pl...Continue Reading

Citations

Jun 21, 2007·European Journal of Nuclear Medicine and Molecular Imaging·Julie A McCarronVictor W Pike
May 25, 2005·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Julie A McCarronLars Farde
Aug 30, 2000·Nuclear Medicine and Biology·B AndréeL Farde
Nov 28, 2002·Nuclear Medicine and Biology·D PapagiannopoulouE Chiotellis
May 3, 2012·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Cristina A J SternLeandro J Bertoglio
Nov 30, 2010·European Journal of Nuclear Medicine and Molecular Imaging·Anniek K D VisserRudi A J O Dierckx
Jul 24, 2014·Psychiatry Research·Soichiro KitamuraTetsuya Suhara
Oct 7, 2010·Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry·Cristina BolzatiGiuliano Bandoli
Mar 10, 2015·Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents·Joanne P ThioJogeshwar Mukherjee
Jul 18, 2006·Nuclear Medicine and Biology·Caroline DefraiteurAlain Plenevaux
Jun 16, 2011·Medicinal Research Reviews·Louise M PatersonGitte M Knudsen
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Luc Zimmer, Didier Le Bars
Apr 3, 2012·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·A ChiotellisM Papadopoulos

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