Biodistribution of [18F] SR144385 and [18F] SR147963: Selective radioligands for positron emission tomographic studies of brain cannabinoid receptors

William B. Mathews, Ursula Scheffel, Paige Finley, Hayden T. Ravert, Richard A. Frank, Murielle Rinaldi-Carmona, Francis Barth, Robert F. Dannals

Research output: Contribution to journalArticlepeer-review

Abstract

[18F] SR144385 and [18F] SR147963 were synthesized in a multistep reaction in which fluorine-18 was introduced by nucleophilic halogen displacement on a bromo precursor. The fluorine-18-labeled intermediate was deprotected and coupled with the appropriate alkyl amine to give the final products. Both radioligands had appropriate regional brain distribution for cannabinoid receptors with a target to nontarget ratio of 1.7 for [18F] SR147963 and 2.5 for [18F] SR144385 at 60 and 90 min postinjection, respectively. The uptake of both tracers was blocked with a 1 mg/kg dose of SR141716A.

Original languageEnglish (US)
Pages (from-to)757-762
Number of pages6
JournalNuclear Medicine and Biology
Volume27
Issue number8
DOIs
StatePublished - Dec 1 2000

Keywords

  • Cannabinoid antagonist
  • Fluorine-18
  • Mice
  • PET

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

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