Radioiodinated 2-hydroxy-3-(4-iodophenyl)-1-(4-phenylpiperidinyl)propane: potential radiotracer for mapping central cholinergic innervation in vitro.
Radioiodinated 2-hydroxy-3-(4-iodophenyl)-1-(4-phenylpiperidinyl)propane, 5 (4-HIPP), was synthesized and evaluated as a simple vesamicol-like radiotracer for mapping cholinergic pathways in the brain. Both enantiomers of 5 exhibit significant accumulation (approx. 2% of injected dose) and prolonged retention (t1/2 greater than 3 h) within the rat brain. The accumulation of radioiodinated 5 in the rat brain was reduced by up to 70% in the presence of vesamicol and its analogs. The levorotary isomer (-)-4-[123I]HIPP exhibits significant accumulation in the monkey brain, with a half-life of about 9 h. Radioiodinated 5 may therefore be a useful tool for studying cholinergic pathways in the brain.
Efange
S M
SM
Department of Radiology, University of Minnesota, Minneapolis 55455.
Dutta
A K
AK
Michelson
R H
RH
Kung
H F
HF
Thomas
J R
JR
Billings
J
J
Boudreau
R J
RJ
D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D002799:Cholinergic Fibers / Q000000981:diagnostic imaging* / Q000378:metabolism; D007457:Iodine Radioisotopes; D007462:Iodobenzenes / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D008297:Male; D009206:Myocardium / Q000378:metabolism; D009467:Neuromuscular Depolarizing Agents / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology; D011877:Radionuclide Imaging; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; D007462:Iodobenzenes; D009467:Neuromuscular Depolarizing Agents; D010880:Piperidines; C075718:2-hydroxy-3-(4-iodophenyl)-1-(4-phenylpiperidinyl)propane; C006189:vesamicol