Skip to main content

Main menu

  • Home
  • Content
    • Current
    • Ahead of print
    • Past Issues
    • JNM Supplement
    • SNMMI Annual Meeting Abstracts
    • Continuing Education
    • JNM Podcasts
  • Subscriptions
    • Subscribers
    • Institutional and Non-member
    • Rates
    • Journal Claims
    • Corporate & Special Sales
  • Authors
    • Submit to JNM
    • Information for Authors
    • Assignment of Copyright
    • AQARA requirements
  • Info
    • Reviewers
    • Permissions
    • Advertisers
  • 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
  • Log out
  • My Cart

Search

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

Advanced Search

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

Development of high potency and highly selective ligands for Sphingosine 1-Phosphate Receptor

Adam Rosenberg, Hui Liu and Zhude Tu
Journal of Nuclear Medicine May 2015, 56 (supplement 3) 1107;
Adam Rosenberg
1Radiological Sciences, Mallinckrodt Institute of Radiology, St. Louis, MO
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Hui Liu
1Radiological Sciences, Mallinckrodt Institute of Radiology, St. Louis, MO
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Zhude Tu
1Radiological Sciences, Mallinckrodt Institute of Radiology, St. Louis, MO
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Info & Metrics
Loading

Abstract

1107

Objectives Sphingosine 1-phosphate receptor 1 (S1PR1) is highly expressed in inflamed tissues, such as multiple sclerosis lesions. A ligand possessing high potency and selectivity for S1PR1 and containing fluorine will have the potential to be radiolabeled with fluorine-18. An 18F labeled S1PR1 radioligand will be very useful for investigating the expression change of S1PR1 in vivo for inflammation relative diseases in animals.

Methods 11 novel selective S1PR1 ligands that containing a fluorine atom were synthesized in a four step sequence and characterized. The ligands were optimized for S1PR1 potency, as well as selective binding to S1PR1 over S1PR2/3. Binding affinities were determined by competing against the binding of [32P]S1P to S1PRs.

Results Structure activity relationship studies indicated that ligands containing an oxadiazole core were superior to those containing a benzoxazole core. Additionally the presence of an amino acid head group was beneficial for potency. Exploration of the non-polar tail group showed a narrow tolerance for derivatization. Using the in vitro radioligand binding assay five compounds showed <100 nM IC50, while two compounds demonstrated <10 nM binding affinities.

Conclusions 11 new S1PR1 selective compounds were prepared. Two compounds are highly active and selective. The lead compounds have excellent potency for S1PR1 (IC50 = 2.63 nM & 8.53 nM), excellent selectivity over S1PR2/3 (>1000 nM); they will be radiolabeled for performing in vivo evaluation in animal models of inflammation.

Research Support DESC0008432

Previous
Back to top

In this issue

Journal of Nuclear Medicine
Vol. 56, Issue supplement 3
May 1, 2015
  • 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.
Development of high potency and highly selective ligands for Sphingosine 1-Phosphate Receptor
(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
Development of high potency and highly selective ligands for Sphingosine 1-Phosphate Receptor
Adam Rosenberg, Hui Liu, Zhude Tu
Journal of Nuclear Medicine May 2015, 56 (supplement 3) 1107;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero
Share
Development of high potency and highly selective ligands for Sphingosine 1-Phosphate Receptor
Adam Rosenberg, Hui Liu, Zhude Tu
Journal of Nuclear Medicine May 2015, 56 (supplement 3) 1107;
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

Molecular Targeting Probes - Radioactive & Nonradioactive

  • SPECT and PET imaging of CD11b-positive immune cells in an orthotopic mouse model of glioma with Zr-89 and Lu-177 labeled Lumi804-anti-CD11b antibody
  • ‘In-loop’ [11C]CO2fixation: Application to the synthesis of a 11C-labeled cholesterol 24-hydroxylase inhibitor
  • N-(Maleimidoethyl)-3-(guanidinomethyl)-5-[131I]iodobenzmide ([131I]MEGMIB): A Residualizing Prosthetic Agent for Site-Specific Radioiodination of Internalizing Single Domain Antibody Fragments.
Show more Molecular Targeting Probes - Radioactive & Nonradioactive

Special MTA: Preclinical Probes for Neuroimaging Posters

  • Synthesis and Evaluation of PET Radiotracers for the Presynaptic High-affinity Choline Transporter
  • Targeting Translocator Protein (TSPO) with GE-180: Imaging brain inflammation and reactive gliosis
  • Synthesis of 1-(2-{2-[4-Fluoro-2-(4-[18F]fluorobenzoyl)phenyl]vinyloxy}ethyl)nipecotic Acid for PET imaging of GAT-1
Show more Special MTA: Preclinical Probes for Neuroimaging Posters

Similar Articles

SNMMI

© 2025 SNMMI

Powered by HighWire