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

✍ Scribed by Josef Zezula; Hay-Yan J. Wang; Amina S. Woods; Roy A. Wise; Arthur E. Jacobson; Kenner C. Rice

Publisher: John Wiley and Sons
Year: 2006
Tongue: French
Weight: 111 KB
Volume: 49
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1069

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✦ Synopsis

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 3 H-labeled chlorisondamine (4,5,6,7-tetrachloro-2-[ 3 H]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-trimethylammoniumethylisoindolinium iodide with pertritiated methyl iodide in dimethylformamide at high temperature in a sealed vessel.

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