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

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A A Wilson; R F Dannals; H T Ravert; J J Frost; H N Wagner (Profiled Authors: John Frost; Robert Dannals; Hayden Ravert; Henry Wagner)

Division of Nuclear Medicine and Radiation Health Sciences, Johns Hopkins Medical Institutions, Baltimore, Maryland 21205-2179.
Journal of medicinal chemistry 1989;32(5):1057-62.

PubMed

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.

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