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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Dexetimide / analogs & derivatives*
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Dexetimide / chemical synthesis
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Dexetimide / pharmacology
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Iodine Radioisotopes*
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Isotope Labeling / methods*
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Male
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Mice
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Parasympatholytics / chemical synthesis*
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Parasympatholytics / pharmacology
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Piperidines / chemical synthesis*
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Receptors, Muscarinic / drug effects*
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Tomography, Emission-Computed
Substances
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Iodine Radioisotopes
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Parasympatholytics
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Piperidines
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Receptors, Muscarinic
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4-iododexetimide
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Dexetimide