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ID: ALA1124460

Journal: J Med Chem

Title: Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.

Authors: Wilson AA, Dannals RF, Ravert HT, Frost JJ, Wagner HN.

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 with 125I and 123I at high specific activity. In vitro binding studies and in vivo biodistribution studies suggest that 123I-labeled 21 may be useful for imaging muscarinic cholinergic receptors in the living human brain with single photon emission computed tomography.

CiteXplore: 2785211

DOI: 10.1021/jm00125a021