Literature DB >> 15820767

Optimizing an online SPE-HPLC method for analysis of (R)-[11C]1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide [(R)-[11C]PK11195] and its metabolites in humans.

Henri N J M Greuter1, Patricia L B van Ophemert, Gert Luurtsema, Bart N M van Berckel, Eric J F Franssen, Bert D Windhorst, Adriaan A Lammertsma.   

Abstract

(R)-[11C]PK11195 is used as a positron emission tomography tracer for activated microglia in several neurological disorders. Quantification of specific binding requires a metabolite-corrected plasma input function. In this study, a high-performance liquid chromatography (HPLC) procedure with online solid phase extraction was modified for analyzing (R)-[11C]PK11195 plasma samples, yielding total sample recoveries of more than 98%. When applied to human studies, the use of two HPLC systems enabled analysis of up to seven plasma samples under regular conditions. Online radioactivity detection was compared with offline sample measurements of HPLC profiles. Offline measurements provided the most reliable results especially for late plasma samples. In 10 patients, an average decrease of parent compound from 94.6% at 2.5 min to 45.2% at 1 h after administration was observed.

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Year:  2005        PMID: 15820767     DOI: 10.1016/j.nucmedbio.2004.12.005

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


  8 in total

1.  Whole-body distribution and metabolism of [N-methyl-11C](R)-1-(2-chlorophenyl)-N-(1-methylpropyl)-3-isoquinolinecarboxamide in humans; an imaging agent for in vivo assessment of peripheral benzodiazepine receptor activity with positron emission tomography.

Authors:  Anne Roivainen; Kjell Någren; Jussi Hirvonen; Vesa Oikonen; Pauliina Virsu; Tuula Tolvanen; Juha O Rinne
Journal:  Eur J Nucl Med Mol Imaging       Date:  2008-12-03       Impact factor: 9.236

2.  Fluorine-18 Radiolabeled PET Tracers for Imaging Monoamine Transporters: Dopamine, Serotonin, and Norepinephrine.

Authors:  Jeffrey S Stehouwer; Mark M Goodman
Journal:  PET Clin       Date:  2009-01

3.  Human dosimetry of carbon-11 labeled N-butan-2-yl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide extrapolated from whole-body distribution kinetics and radiometabolism in rats.

Authors:  Pauliina Luoto; Iina Laitinen; Sami Suilamo; Kjell Någren; Anne Roivainen
Journal:  Mol Imaging Biol       Date:  2009-11-26       Impact factor: 3.488

4.  Quantification of (R)-[11C]PK11195 binding in rheumatoid arthritis.

Authors:  M A Kropholler; R Boellaard; E H Elzinga; C J van der Laken; K Maruyama; R W Kloet; A E Voskuyl; B A C Dijkmans; A A Lammertsma
Journal:  Eur J Nucl Med Mol Imaging       Date:  2008-11-29       Impact factor: 9.236

5.  Development of N-methyl-(2-arylquinolin-4-yl)oxypropanamides as leads to PET radioligands for translocator protein (18 kDa).

Authors:  Chad Brouwer; Kimberly Jenko; Sami S Zoghbi; Robert B Innis; Victor W Pike
Journal:  J Med Chem       Date:  2014-07-01       Impact factor: 7.446

6.  Combined [(18)F]DPA-714 micro-positron emission tomography and autoradiography imaging of microglia activation after closed head injury in mice.

Authors:  Ina Israel; Andrea Ohsiek; Ehab Al-Momani; Christiane Albert-Weissenberger; Christian Stetter; Stine Mencl; Andreas K Buck; Christoph Kleinschnitz; Samuel Samnick; Anna-Leena Sirén
Journal:  J Neuroinflammation       Date:  2016-06-07       Impact factor: 8.322

7.  Improved Automated Radiosynthesis of [(11)C]PBR28.

Authors:  Kiran Kumar Solingapuram Sai; Don Gage; Mike Nader; Robert H Mach; Akiva Mintz
Journal:  Sci Pharm       Date:  2015-06-19

8.  Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors.

Authors:  Kazunori Kawamura; Wakana Mori; Masayuki Fujinaga; Tomoteru Yamasaki; Yiding Zhang; Hidekatsu Wakizaka; Akiko Hatori; Lin Xie; Katsushi Kumata; Takayuki Ohkubo; Yusuke Kurihara; Masanao Ogawa; Nobuki Nengaki; Ming-Rong Zhang
Journal:  EJNMMI Radiopharm Chem       Date:  2019-02-18
  8 in total

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