Literature DB >> 10962257

PET evaluation of [(18)F]FCWAY, an analog of the 5-HT(1A) receptor antagonist, WAY-100635.

R E Carson1, L Lang, H Watabe, M G Der, H R Adams, E Jagoda, P Herscovitch, W C Eckelman.   

Abstract

We synthesized [(18)F]FCWAY, an analog of [carbonyl-(11)C]WAY-100635 ¿[(11)C]N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2-(pyridi nyl))cyclohexanecarboxamide¿, by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [(18)F]FC and [(18)F]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [(18)F]FCWAY has very similar kinetic characteristics to [(11)C]WAY-100635.

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Year:  2000        PMID： 10962257     DOI： 10.1016/s0969-8051(00)00118-9

Source DB:  PubMed          Journal:  Nucl Med Biol        ISSN： 0969-8051            Impact factor:   2.408


  22 in total

1.  Measurement of 5-HT(1A) receptor density and in-vivo binding parameters of [(18)F]mefway in the nonhuman primate.

Authors:  Dustin W Wooten; Ansel T Hillmer; Jeffrey M Moirano; Elizabeth O Ahlers; Maxim Slesarev; Todd E Barnhart; Jogeshwar Mukherjee; Mary L Schneider; Bradley T Christian
Journal:  J Cereb Blood Flow Metab       Date:  2012-04-04       Impact factor: 6.200

2.  An automated one-step one-pot [(18)F]FCWAY synthesis: development and minimization of chemical impurities.

Authors:  Bik-Kee Vuong; Dale O Kiesewetter; Lixin Lang; Ying Ma; William C Eckelman; Michael A Channing
Journal:  Nucl Med Biol       Date:  2007-05       Impact factor: 2.408

3.  Effects of early-life stress on serotonin(1A) receptors in juvenile Rhesus monkeys measured by positron emission tomography.

Authors:  Simona Spinelli; Svetlana Chefer; Richard E Carson; Elaine Jagoda; Lixin Lang; Markus Heilig; Christina S Barr; Stephen J Suomi; J Dee Higley; Elliot A Stein
Journal:  Biol Psychiatry       Date:  2010-02-20       Impact factor: 13.382

4.  Reduced post-synaptic serotonin type 1A receptor binding in bipolar depression.

Authors:  Allison C Nugent; Earle E Bain; Paul J Carlson; Alexander Neumeister; Omer Bonne; Richard E Carson; William Eckelman; Peter Herscovitch; Carlos A Zarate; Dennis S Charney; Wayne C Drevets
Journal:  Eur Neuropsychopharmacol       Date:  2013-02-20       Impact factor: 4.600

5.  First-in-human evaluation of 18F-mefway, a PET radioligand specific to serotonin-1A receptors.

Authors:  Ansel T Hillmer; Dustin W Wooten; Alisha K Bajwa; Andrew T Higgins; Patrick J Lao; Tobey J Betthauser; Todd E Barnhart; Howard A Rowley; Charles K Stone; Sterling C Johnson; Jogeshwar Mukherjee; Bradley T Christian
Journal:  J Nucl Med       Date:  2014-11-13       Impact factor: 10.057

6.  The effect of 5-HT1A receptor antagonist on reward-based decision-making.

Authors:  Fumika Akizawa; Takashi Mizuhiki; Tsuyoshi Setogawa; Mai Takafuji; Munetaka Shidara
Journal:  J Physiol Sci       Date:  2019-11-08       Impact factor: 2.781

7.  5-HT 1A receptors are reduced in temporal lobe epilepsy after partial-volume correction.

Authors:  Giampiero Giovacchini; Maria T Toczek; Robert Bonwetsch; Anto Bagic; Lixin Lang; Charles Fraser; Pat Reeves-Tyer; Peter Herscovitch; William C Eckelman; Richard E Carson; William H Theodore
Journal:  J Nucl Med       Date:  2005-07       Impact factor: 10.057

8.  Using cerebral white matter for estimation of nondisplaceable binding of 5-HT1A receptors in temporal lobe epilepsy.

Authors:  Giampiero Giovacchini; Shielah Conant; Peter Herscovitch; William H Theodore
Journal:  J Nucl Med       Date:  2009-10-16       Impact factor: 10.057

9.  P-Glycoprotein, not BCRP, Limits the Brain Uptake of [(18)F]Mefway in Rodent Brain.

Authors:  Jae Yong Choi; Jin Sook Song; Minkyung Lee; Woon-Ki Cho; Jin Chung; Chul Hyoung Lyoo; Chul Hoon Kim; Jiae Park; Kyo Chul Lee; Kyeong Min Kim; Jee Hae Kang; Myung Ae Bae; Young Hoon Ryu
Journal:  Mol Imaging Biol       Date:  2016-04       Impact factor: 3.488

10.  Biodistribution and Radiation Dosimetry of [18F]Mefway in Humans.

Authors:  Jae Yong Choi; Chul Hyoung Lyoo; Jin Su Kim; Kyeong Min Kim; Minkyung Lee; Young Hoon Ryu
Journal:  Mol Imaging Biol       Date:  2016-12       Impact factor: 3.488
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