Preparation and evaluation of radioiodinated (iodophenyl)cholines and their morpholinium and piperidinium analogues as myocardial perfusion imaging agents.
A series of nine radioiodinated quaternary ammonium salts related to phenylcholine were synthesized, characterized, and radiolabeled by exchange. These compounds were evaluated as myocardial perfusion imaging agents in mice, pigs, and humans. Mice biodistribution studies showed that five of the nine compounds were taken up in the heart to the same extent as 201Tl+ at 5 min. At 60 min myocardial retention was significantly better than 201Tl+ for six of the compounds. Several of the compounds showed more favorable heart/blood and heart/liver ratios when compared to 201Tl+. Evaluation of three of the more promising compounds in pigs and humans however revealed no selective myocardial uptake.
P L
PL
Zabel
Y
Y
Zea-Ponce
G W
GW
Brown
G
G
Morrissey
D H
DH
Hunter
A A
AA
Driedger
M J
MJ
Chamberlain
D000818:Animals; D002794:Choline / Q000031:analogs & derivatives* / Q000378:metabolism; D006321:Heart / Q000000981:diagnostic imaging*; D006801:Humans; D007536:Isomerism; D008099:Liver / Q000378:metabolism; D051379:Mice; D009206:Myocardium / Q000378:metabolism; D010477:Perfusion; D011877:Radionuclide Imaging; D013329:Structure-Activity Relationship; D013552:Swine; D013793:Thallium; D013997:Time Factors; D014018:Tissue Distribution
D013793:Thallium; D002794:Choline