Determination of dopamine D4 receptor density in rat striatum using PB12 as a probe
Determination of dopamine D4 receptor density in rat striatum using PB12 as a probe
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DOI：
10.1016/s0014-2999(01)01129-3
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发表时间：
2001-09-07
影响因子：
5
通讯作者：
Tortorella, V
中科院分区：
文献类型：
--
作者：
Colabufo, NA;Berardi, F;Tortorella, V
以多巴胺D-4受体配体N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-tnethoxybenzamide(PB12)为探针，直接测定大鼠纹状体多巴胺D-4受体密度，以替代差减法。实验用[H-3]螺哌利多标记D-2、D-3和D-4受体，用PB12直接测定多巴胺D-4受体的特异性结合。测得B-max为82fmol/mg蛋白。多巴胺D4受体对D-2样受体总数的贡献率为63%；然而，由于观察到D-2、D-3和D-4受体的动力学特征不同，这个值不被认为是可靠的。(C)2001 Elsevier Science B.V.保留所有权利。
N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-tnethoxybenzamide (PB12), a potent and selective dopamine D-4 receptor ligand, was used as a probe for the direct determination of the dopamine D4 receptor density in rat striatum as an alternative to the subtraction method. The experiment was performed using [H-3]spiroperidol to label D-2, D-3 and D-4 receptors and PB12 to determine directly dopamine D-4 receptor specific binding. The determined B-max value was 82 fmol/mg protein. The contribution of the dopamine D4 receptor to the overall population of D-2-like receptors was 63%; however, this value cannot be considered reliable because of the observed difference in the kinetic profiles of D-2, D-3 and D-4 receptors. (C) 2001 Elsevier Science B.V. All rights reserved.