Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.
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.
Wilson
A A
AA
Division of Nuclear Medicine and Radiation Health Sciences, Johns Hopkins Medical Institutions, Baltimore, Maryland 21205-2179.
Dannals
R F
RF
Ravert
H T
HT
Frost
J J
JJ
Wagner
H N
HN
D000818:Animals; D003909:Dexetimide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D007457:Iodine Radioisotopes; D007553:Isotope Labeling / Q000379:methods*; D008297:Male; D051379:Mice; D010276:Parasympatholytics / Q000138:chemical synthesis* / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis*; D011976:Receptors, Muscarinic / Q000187:drug effects*; D014055:Tomography, Emission-Computed
D007457:Iodine Radioisotopes; D010276:Parasympatholytics; D010880:Piperidines; D011976:Receptors, Muscarinic; C066812:4-iododexetimide; D003909:Dexetimide