Amlaiky N, Kilpatrick B F, Caron M G
FEBS Lett. 1984 Oct 29;176(2):436-40. doi: 10.1016/0014-5793(84)81213-2.
A novel high affinity dopaminergic ligand, N-(p-aminophenethyl)spiroperidol, has been synthesized and radioiodinated to a specific radioactivity of 2175 Ci/mmol. Binding of this ligand to bovine anterior pituitary membranes is: rapid (40-60 min to equilibrium at 25 degrees C) and reversible (t1/2 = 1 h at 25 degrees C); saturable and of high affinity (KD approximately 20 pM) and displays a typical D2-dopaminergic specificity. The ligand, which identifies the same number of receptor sites as other tritiated antagonist ligands, can be used in different tissues and preparations to delineate the characteristics of the D2 receptor. Thus, this high affinity, high specific radioactivity ligand (N-(p-amino-m-[125I]iodophenethyl)spiroperidol) represents a tool which until now had not been available for the characterization of the D2-dopamine receptor.
一种新型高亲和力多巴胺能配体N-（对氨基苯乙基）螺哌啶醇已被合成并进行放射性碘化，比活度为2175 Ci/mmol。该配体与牛垂体前叶膜的结合具有以下特点：迅速（25℃下40 - 60分钟达到平衡）且可逆（25℃下t1/2 = 1小时）；具有饱和性和高亲和力（KD约为20 pM），并表现出典型的D2多巴胺能特异性。该配体识别的受体位点数量与其他氚化拮抗剂配体相同，可用于不同组织和制剂中以描绘D2受体的特征。因此，这种高亲和力、高比活度的配体（N-（对氨基-m-[125I]碘苯乙基）螺哌啶醇）代表了一种迄今为止尚未用于表征D2-多巴胺受体的工具。
