[11C]-methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)methyl]-1-piperazinecarboxylate ([11C]GR89696): Synthesis and in vivo binding to kappa opiate receptors

Hayden T. Ravert, William B Mathews, John L. Musachio, Ursula Scheffel, Paige Finley, Robert F Dannals

Research output: Contribution to journalArticle

Abstract

GR89696, racemic methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl) methyl]-1-piperazinecarboxylate, a kappa opioid receptor ligand, was labeled with [11C]methyl chloroformate. The radiochemical yield was 20% with an observed specific radioactivity of 75.5 GBq/μmol at end of synthesis (2,040 mCi/μmol). Five minutes after intravenous administration, 5.4% of the injected dose accumulated in mouse whole brain. Brain region to cerebellar ratios increased over time with ratios at 90 min of 7.8, 5.6, and 4.5 for the hypothalamus, olfactory tubercle, and striatum, respectively. The uptake of [11C]GR89696 correlated with known kappa opioid receptor densities and was inhibited by kappa opioid selective drugs. Copyright (C) 1999 Elsevier Science Inc.

Original languageEnglish (US)
Pages (from-to)737-741
Number of pages5
JournalNuclear Medicine and Biology
Volume26
Issue number7
DOIs
Publication statusPublished - Oct 1999

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Keywords

  • C-11
  • Kappa opioid receptors
  • PET

ASJC Scopus subject areas

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

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