Application of [125I] (S)-5-iodonicotine, a new radioiodinated ligand, in the assay of nicotinic acetylcholine receptor binding in the brain.
Application of [125I] (S)-5-iodonicotine, a new radioiodinated ligand, in the assay of nicotinic acetylcholine receptor binding in the brain.
复制标题
[125I](S)-5-碘烟碱（一种新的放射性碘配体）在大脑中烟碱乙酰胆碱受体结合测定中的应用。
DOI：
10.1248/bpb.18.1463
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发表时间：
1995
影响因子：
2
通讯作者：
A. Yokoyama
中科院分区：
文献类型：
--
作者：
H. Saji;A. Watanabe;Y. Kiyono;Y. Magata;Y. Iida;Y. Takaishi;A. Yokoyama
制备了[125 I]（S）-5-碘烟碱，并研究了其在脑内烟碱乙酰胆碱受体结合分析中的应用。[125 I]（S）-5-碘烟碱与大鼠皮层膜结合亲和力高（Kd，15.0 nm）。各种烟碱类胆碱能化合物与[125 I]（S）-5-碘烟碱竞争大鼠皮层膜上的结合位点，其结合特异性与[H3]金雀花碱的结合特异性相关（r = 0.98）。这些结果表明，[125 I]（S）-5-碘烟碱与[H3]野靛碱结合的位点相同，并表明[125 I]（S）-5-碘烟碱可用作脑烟碱受体结合试验。
[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.