Application of [125I] (S)-5-iodonicotine, a new radioiodinated ligand, in the assay of nicotinic acetylcholine receptor binding in the brain.
[125I](S)-5-Iodonicotine was prepared and its application in the assay of nicotinic acetylcholine receptor binding in the brain was studied. [125I](S)-5-Iodonicotine bound to the rat cortical membrane with high affinity (Kd, 15.0 nm). Various nicotinic cholinergic compounds showed competition with [125I](S)-5-iodonicotine for the binding sites in the rats cortical membrane, and the specificity of its binding was correlated well with that of [H3] cytisine (r = 0.98). These findings suggest that [125I](S)-5-iodonicotine binds to the same sites as [H3] cytisine and indicate that [125I](S)-5-iodonicotine can be applied as a brain nicotine receptor binding assay.
Saji
H
H
Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.
Watanabe
A
A
Kiyono
Y
Y
Magata
Y
Y
Iida
Y
Y
Takaishi
Y
Y
Yokoyama
A
A
D000470:Alkaloids / Q000378:metabolism; D000818:Animals; D001392:Azocines; D001667:Binding, Competitive; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D007700:Kinetics; D008024:Ligands; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D009538:Nicotine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D011807:Quinolizines; D051381:Rats; D017208:Rats, Wistar; D011978:Receptors, Nicotinic / Q000187:drug effects / Q000378:metabolism*; D000093843:Quinolizidine Alkaloids
D000470:Alkaloids; D001392:Azocines; D007457:Iodine Radioisotopes; D008024:Ligands; D009538:Nicotine; D011807:Quinolizines; D011978:Receptors, Nicotinic; C098439:5-iodonicotine; C004712:cytisine; D000093843:Quinolizidine Alkaloids