Synthesis of [3H]DIPPA: A potent irreversible antagonist selective for the κ opioid receptor

An‐Chih ‐C Chang, Joseph D. Trometer, Philip S. Portoghese

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

2‐(3,4‐Dichlorophenyl)‐N‐methyl‐N‐[(1S)‐1‐(3‐isothiocyanatophenyl)‐2‐(1‐pyrrolidinyl)ethyl]acetamide (1, DIPPA) has been previously reported to be an opioid receptor affinity label that produces selective and long‐lasting κ opioid receptor antagonism in mice, High specific activity [3H]DIPPA (39.7 Ci/mmol) was prepared by bromination and catalytic tritiation of the amino precursor of DIPPA followed by conversion to the isothiocyanate with thiophosgene.

Original languageEnglish (US)
Pages (from-to)553-557
Number of pages5
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume36
Issue number6
DOIs
StatePublished - Jun 1995

Keywords

  • DIPPA
  • affinity label
  • antagonist
  • kappa
  • radiolabeled
  • tritium

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