Skip to main content

Main menu

  • Home
  • Content
    • Current
    • Ahead of print
    • Past Issues
    • JNM Supplement
    • SNMMI Annual Meeting Abstracts
  • Subscriptions
    • Subscribers
    • Institutional and Non-member
    • Rates
    • Corporate & Special Sales
    • Journal Claims
  • Authors
    • Submit to JNM
    • Information for Authors
    • Assignment of Copyright
    • AQARA requirements
  • Info
    • Permissions
    • Advertisers
    • Continuing Education
  • About
    • About Us
    • Editorial Board
    • Contact Information
  • More
    • Alerts
    • Feedback
    • Help
    • SNMMI Journals
  • SNMMI
    • JNM
    • JNMT
    • SNMMI Journals
    • SNMMI

User menu

  • Subscribe
  • My alerts
  • Log in
  • My Cart

Search

  • Advanced search
Journal of Nuclear Medicine
  • SNMMI
    • JNM
    • JNMT
    • SNMMI Journals
    • SNMMI
  • Subscribe
  • My alerts
  • Log in
  • My Cart
Journal of Nuclear Medicine

Advanced Search

  • Home
  • Content
    • Current
    • Ahead of print
    • Past Issues
    • JNM Supplement
    • SNMMI Annual Meeting Abstracts
  • Subscriptions
    • Subscribers
    • Institutional and Non-member
    • Rates
    • Corporate & Special Sales
    • Journal Claims
  • Authors
    • Submit to JNM
    • Information for Authors
    • Assignment of Copyright
    • AQARA requirements
  • Info
    • Permissions
    • Advertisers
    • Continuing Education
  • About
    • About Us
    • Editorial Board
    • Contact Information
  • More
    • Alerts
    • Feedback
    • Help
    • SNMMI Journals
  • Follow JNM on Twitter
  • Visit JNM on Facebook
  • Join JNM on LinkedIn
  • Subscribe to our RSS feeds
Meeting ReportRadiopharmaceutical Chemistry: New Chemistry-Neurosciences

Synthesis and evaluation of an [18F] labelled imidazopyridine, for the study of the peripheral benzodiazepine binding sites using PET

Andrew Katsifis, Filomena Mattner, Tien Pham, Christopher Fookes, Ivan Greguric, Paula Berghofer, Patrice Ballantyne, Rachael Shepherd and Xiang Liu
Journal of Nuclear Medicine May 2007, 48 (supplement 2) 300P;
Andrew Katsifis
1ANSTO, Radiopharmaceutical Research Institute, Sydney, New South Wales, Australia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Filomena Mattner
1ANSTO, Radiopharmaceutical Research Institute, Sydney, New South Wales, Australia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Tien Pham
1ANSTO, Radiopharmaceutical Research Institute, Sydney, New South Wales, Australia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Christopher Fookes
1ANSTO, Radiopharmaceutical Research Institute, Sydney, New South Wales, Australia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Ivan Greguric
1ANSTO, Radiopharmaceutical Research Institute, Sydney, New South Wales, Australia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Paula Berghofer
1ANSTO, Radiopharmaceutical Research Institute, Sydney, New South Wales, Australia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Patrice Ballantyne
1ANSTO, Radiopharmaceutical Research Institute, Sydney, New South Wales, Australia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Rachael Shepherd
1ANSTO, Radiopharmaceutical Research Institute, Sydney, New South Wales, Australia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Xiang Liu
1ANSTO, Radiopharmaceutical Research Institute, Sydney, New South Wales, Australia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Info & Metrics
Loading

Abstract

1331

Objectives: The purpose of this study was to synthesise and evaluate the F-18 imidazopyridine 2-(2-(4-(3-fluoropropoxy)phenyl)-6,8-dichloroimidazo[1,2-a]pyridin-3-yl)-N-methyl-N-phenylacetamide 1 as a potential tracer for the study of PBBS using PET. Methods: [18F]1 has been prepared by nucleophilic substitution of the tosylethyloxy precursor with 18F-fluoride in the presence of K222, K2CO3 in ACN at 100°C for 5 mins followed by RP-HPLC purification. The biodistribution of [18F]1 was performed in SD rats and brain and peripheral tissues were analysised at 15, 30 min, 1, and 4 h p.i. The specificity and selectivity of the tracer was assessed by pre-treatment with the PBBS ligands PK11195 and Ro 5-4864 and with Flumazenil for CBR at 1 mg/kg 5 min prior to injection of [18F]1. Results: In vitro binding of 1 indicated an IC50 of 7.4 nM for PBBS and >4000 nM for the CBR. [18F]1 was synthesised in 40-55 % radiochemical yield non-decay corrected and with > 95 % radiochemical purity. The specific activity ranged from 37-80 GBq/μmol (non optimised). Biodistribution studies indicated uptake of [18F]1 in tissue expressing PBBS. The adrenals showed high uptake, increasing from 9% ID/g at 30 min p.i to 11% at 4 h. In the kidneys the activity peaked at 15 min p.i.(5%) and decreased over time to 3.6% at 4h. In the heart the uptake was maintained at 7% througout the experiment (15 min to 4 h). Bone uptake ranged from 1% (at 15 min) to 2.9% at 4h. [18F]1 readily penetrated the blood-brain barrier with uptake in the olfactory regions ranging from an initial 0.66% at 15 min to 0.26% at 4 h p.i. The concentration in the blood was significantly lower than the brain regions (0.7% at 15 min to 0.15% at 4 h). Pre-treatment with PK 11195, Ro 5-4864 and non radioactive analogue 1 significantly decreased the uptake in the brain and peripheral organs except in the adrenals which showed a modest increase or no change in uptake. Flumazenil had no effect in the uptake of [18F]1 in the brain or peripheral organs. Conclusions: These results demonstrate the specific PBBS uptake of [18F]1 in vivo. Therefore [18F]1 warrants further investigation as a potential PET tracer for the PBBS.

  • Society of Nuclear Medicine, Inc.
Back to top

In this issue

Journal of Nuclear Medicine
Vol. 48, Issue supplement 2
May 1, 2007
  • Table of Contents
  • Index by author
Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for your interest in spreading the word on Journal of Nuclear Medicine.

NOTE: We only request your email address so that the person you are recommending the page to knows that you wanted them to see it, and that it is not junk mail. We do not capture any email address.

Enter multiple addresses on separate lines or separate them with commas.
Synthesis and evaluation of an [18F] labelled imidazopyridine, for the study of the peripheral benzodiazepine binding sites using PET
(Your Name) has sent you a message from Journal of Nuclear Medicine
(Your Name) thought you would like to see the Journal of Nuclear Medicine web site.
Citation Tools
Synthesis and evaluation of an [18F] labelled imidazopyridine, for the study of the peripheral benzodiazepine binding sites using PET
Andrew Katsifis, Filomena Mattner, Tien Pham, Christopher Fookes, Ivan Greguric, Paula Berghofer, Patrice Ballantyne, Rachael Shepherd, Xiang Liu
Journal of Nuclear Medicine May 2007, 48 (supplement 2) 300P;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero
Share
Synthesis and evaluation of an [18F] labelled imidazopyridine, for the study of the peripheral benzodiazepine binding sites using PET
Andrew Katsifis, Filomena Mattner, Tien Pham, Christopher Fookes, Ivan Greguric, Paula Berghofer, Patrice Ballantyne, Rachael Shepherd, Xiang Liu
Journal of Nuclear Medicine May 2007, 48 (supplement 2) 300P;
Twitter logo Facebook logo LinkedIn logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One
Bookmark this article

Jump to section

  • Article
  • Info & Metrics

Related Articles

  • No related articles found.
  • Google Scholar

Cited By...

  • No citing articles found.
  • Google Scholar

More in this TOC Section

Radiopharmaceutical Chemistry: New Chemistry-Neurosciences

  • Synthesis, binding affinity and radiosynthesis of [18F]JHU87522, a radioligand with optimal properties for quantitative PET imaging of nicotinic acetylcholine receptors (nAChRs)
  • Radiosynthesis of (±)-N-(p-[11C]tolyl)-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide ([11C]methyl-PHCCC) as a specific mGluR4 PET ligand
  • Evaluation of the putative dopamine D3 PET tracer [11C]WC-10 in non-human primates
Show more Radiopharmaceutical Chemistry: New Chemistry-Neurosciences

New Chemistry-Neurosciences Posters

  • Synthesis and PET studies of [11C]letrozole, an aromatase inhibitor drug
  • Radiosynthesis and in vivo evaluation of [11C]papaverine as PDE10A PET tracer
  • Synthesis and evaluation of 18F-MDL 100907 derivatives for the 5-HT2A receptor
Show more New Chemistry-Neurosciences Posters

Similar Articles

SNMMI

© 2023 Journal of Nuclear Medicine

Powered by HighWire