In vivo labeling of nicotinic cholinergic receptors in brain with [3H]cytisine

J. E. Flesher, U. Scheffel, E. D. London, J. J. Frost

Research output: Contribution to journalArticle

Abstract

[3H]Cytisine was evaluated as an in vivo ligand for the nicotinic cholinergic receptor (nAchR) in mouse brain. The tracer was injected intravenously, and radioactivity in brain regions was analyzed. Radioactivity peaked in the brain at 30 minutes. It was highest in the thalamus, intermediate in the superior colliculi, prefrontal cortex and hippocampus, and low in the cerebellum. Pretreatment with unlabeled cytisine inhibited binding in the thalamus, but not in the cerebellum. Binding was displaced by l-nicotine, but not by d-nicotine or dexetimide. The results suggest that cytisine, appropriately labeled with a positron emitting radionuclide, may be useful for study of nicotinic cholinergic receptors in humans by emission computed tomography.

Original languageEnglish (US)
Pages (from-to)1883-1890
Number of pages8
JournalLife Sciences
Volume54
Issue number24
DOIs
StatePublished - 1994

Keywords

  • central nicotinic cholinergic receptors
  • in vivo binding
  • mouse brain
  • [H]cytisine

ASJC Scopus subject areas

  • Pharmacology

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