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 journalArticle

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 - 2000

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Cannabinoid Receptors
rimonabant
Fluorine
Electrons
Halogens
Brain
Amines

Keywords

  • Cannabinoid antagonist
  • Fluorine-18
  • Mice
  • PET

ASJC Scopus subject areas

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

Cite this

Biodistribution of [18F] SR144385 and [18F] SR147963 : Selective radioligands for positron emission tomographic studies of brain cannabinoid receptors. / Mathews, William B; Scheffel, Ursula; Finley, Paige; Ravert, Hayden T.; Frank, Richard A.; Rinaldi-Carmona, Murielle; Barth, Francis; Dannals, Robert F.

In: Nuclear Medicine and Biology, Vol. 27, No. 8, 2000, p. 757-762.

Research output: Contribution to journalArticle

Mathews, William B ; Scheffel, Ursula ; Finley, Paige ; Ravert, Hayden T. ; Frank, Richard A. ; Rinaldi-Carmona, Murielle ; Barth, Francis ; Dannals, Robert F. / Biodistribution of [18F] SR144385 and [18F] SR147963 : Selective radioligands for positron emission tomographic studies of brain cannabinoid receptors. In: Nuclear Medicine and Biology. 2000 ; Vol. 27, No. 8. pp. 757-762.
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T2 - Selective radioligands for positron emission tomographic studies of brain cannabinoid receptors

AU - Mathews, William B

AU - Scheffel, Ursula

AU - Finley, Paige

AU - Ravert, Hayden T.

AU - Frank, Richard A.

AU - Rinaldi-Carmona, Murielle

AU - Barth, Francis

AU - Dannals, Robert F

PY - 2000

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