Synthesis and Biological Evaluation of [125I]- and [123I]-4-Iododexetimide, a Potent Muscarinic Cholinergic Receptor Antagonist

Alan A. Wilson, Robert F. Dannals, Hayden T. Ravert, J. James Frost, Henry N. Wagner

Research output: Contribution to journalArticle

Abstract

A series of halogenated racemic analogues of dexetimide (1) was synthesized and their affinity for the muscarinic cholinergic receptor measured. One analogue, 4-iododexetimide (21), was efficiently labeled with125I and123I at high specific activity. In vitro binding studies and in vivo biodistribution studies suggest that123I-labeled 21 may be useful for imaging muscarinic cholinergic receptors in the living human brain with single photon emission computed tomography.

Original languageEnglish (US)
Pages (from-to)1057-1062
Number of pages6
JournalJournal of medicinal chemistry
Volume32
Issue number5
DOIs
StatePublished - May 1 1989

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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