The high specific activity tritium labeling of the ganglion-blocking nicotinic antagonist chlorisondamine

Josef Zezula, Hay Yan J Wang, Amina S. Woods, Roy A. Wise, Arthur E. Jacobson, Kenner C. Rice

Research output: Contribution to journalArticlepeer-review

Abstract

Chlorisondamine is a bisquaternary ganglion-blocking nicotinic antagonist that accumulates in dopaminergic, serotonergic, and noradrenergic cell bodies; the mechanism of uptake and time-course of retrograde transport are not known. Chlorisondamine could possibly be taken into monoaminergic neurons when blocked nicotinic receptors on those cells are internalized. In order to more easily study the mechanism of the capture and recycling of chlorisondamine, a ligand is needed that has high specific activity. For that purpose, we now report the preparation of 3H-labeled chlorisondamine (4,5,6,7-tetrachloro-2- [3H]methyl-2-(2-trimethylammoniumethyl)-isoindolinium diiodide) of high specific activity (94 Ci/mmol). The compound was synthesized by quarternization of 4,5,6,7-tetrachloro-2-(2-trimethylammoniumethyl-isoindolinium iodide with pertritiated methyl iodide in dimethylformamide at high temperature in a sealed vessel.

Original languageEnglish (US)
Pages (from-to)471-478
Number of pages8
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume49
Issue number5
DOIs
StatePublished - Apr 2006
Externally publishedYes

Keywords

  • Chlorisondamine
  • Nicotinic antagonist
  • Tritiation

ASJC Scopus subject areas

  • Analytical Chemistry
  • Drug Discovery
  • Organic Chemistry
  • Clinical Biochemistry
  • Molecular Medicine
  • Pharmacology

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