Gpp(NH)p stimulates [3H]raclopride binding to homogenates from human putamen and accumbens.
Gpp(NH)p stimulates [3H]raclopride binding to homogenates from human putamen and accumbens.
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Gpp(NH)p 刺激 [3H]raclopride 与人壳核和伏核的匀浆结合。
DOI：
10.1016/0304-3940(92)90652-n
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发表时间：
1992
影响因子：
2.5
通讯作者：
Sedvall,G
中科院分区：
文献类型：
--
作者：
Hall,H;Halldin,C;Sedvall,G
本文研究了稳定的GTP类似物GPP(NH)p(5‘-鸟氨酰亚胺二磷酸)对人死后脑组织标本中多巴胺D2受体与[~3H]拉氯普利体外结合的影响。与没有GPP(NH)p相比，在有GPP(NH)p存在的情况下，估计大脑中壳核和伏隔核的受体数量分别高出29%和38%。激动剂的相互作用是双相的，证实了受体-G-蛋白复合体的两种亲和态模型。GPP(NH)p的加入消除了阿朴吗啡与[~3H]拉氯普利结合的两个部位的竞争。GPP(NH)p的加入对高浓度阿朴吗啡的非特异性结合无明显影响，表明只有[~3H]雷氯普利与多巴胺D2受体的特异性结合增加。
The effects of the stable GTP analogue Gpp(NH)p (5′-guanylyl imido diphosphate) were examined on in vitro [3H]raclopride binding to dopamine D2receptors in preparations from post mortem human brains. The estimated number of receptors in the brain was 29% and 38% higher in putamen and accumbens, respectively, when determined in the presence of Gpp(NH)p as compared to its absence. The interaction of agonists was biphasic confirming the two affinity state model of the receptor - G-protein complex. The addition of Gpp(NH)p to the assay abolished the two site competition of apomorphine with [3H]raclopride binding in both regions studied. The non-specific binding at high concentrations of apomorphine was not significantly affected by the addition of Gpp(NH)p, indicating that only the specific binding of [3H]raclopride to the dopamine D2receptor is increased.