Radiosynthesis of [11C]nifedipine and [11C]nicardipine

Alan A. Wilson, Robert F. Dannals, Hayden T. Ravert, H. Donald Burns, Susan Z. Lever, Henry N. Wagner

Research output: Contribution to journalArticle

Abstract

The radiosyntheses of the dihydropyridine (DHP) calcium channel blockers [11C]nifedipine and [11C]nicardipine by alkylation of the appropriate DHP 3‐monocarboxylic acid anion with [11C]iodomethane are described. Isolated radiochemical yields of 30–50% were obtained 25 minutes after the end‐of‐bombardment, with specific activities of 400–1400 mCi/μmol at the end‐of‐synthesis. A variety of positron emitting DHPs with different ester side chains in the 3 and 5 positions on the DHP ring may be prepared by this approach using currently available labelled alkylating agents.

Original languageEnglish (US)
Pages (from-to)589-598
Number of pages10
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume27
Issue number5
DOIs
StatePublished - May 1989

Keywords

  • calcium channel blocker
  • carbon‐11
  • dihydropyridine derivatives
  • nicardipine
  • nifedipine
  • radiotracer

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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