在hD2short多巴胺化合物的表征,hD4.2和hD4.7受体agonist-stimulated [35 s] GTPgammaS绑定化验。
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Gilliland SL,高山RH
在hD2short多巴胺化合物的表征,hD4.2和hD4.7受体agonist-stimulated [35 s] GTPgammaS绑定化验。
Naunyn Schmiedebergs拱杂志。2000年5月,361 (5):498 - 504。doi: 10.1007 / s002100000224。
- PubMed ID
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10832603 (在PubMed]
- 文摘
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多巴胺受体受体激动剂和拮抗剂在放射性配体结合试验都进行了广泛的特点;只有数量有限的实验室特点他们使用功能分析多个受体亚型。实验被设计来评估四个受体激动剂和7个克隆人类多巴胺受体拮抗剂三个使用agonist-stimulated [35 s] GTPgammaS绑定在膜量化分析最初的细胞事件后配体/受体的相互作用。在这个模型中有本构G蛋白活动(agonist-independent [35 s] GTPgammaS绑定)和潜在的本构多巴胺受体的活动。因此,沉默的对手之间的歧视,部分受体激动剂和反兴奋剂在理论上是可能的。是预期的差别可以关于功效的七个受体拮抗剂提供有关治疗抗精神病药物的使用。在膜准备转染CHO细胞表达人类D2short密度高,D4.2或D4.7受体,多巴胺受体受体激动剂阿朴吗啡,培高利特,quinelorane quinpirole产生浓度增加agonist-stimulated [35 s] GTPgammaS绑定。hD2short受体,培高利特,阿朴吗啡本质上都是均等的,更强大的比quinelorane quinpirole;所有四个在这个受体受体激动剂显示类似的功效。hD4.2和hD4.7阿朴吗啡受体是最有效和培高利特最有效的四个药物。 The ability (both potency and efficacy) of clozapine, haloperidol, olanzapine, quetiapine, risperidone, spiperone and ziprasidone to block apomorphine-stimulated [35S]GTPgammaS binding and alter basal [35S]GTPgammaS binding was also assessed. All of the antagonists inhibited apomorphine-stimulated [35S]GTPgammaS binding with potencies (Kb values) similar to and in rank order consistent with their affinities reported in the literature using radioligand binding assays. Additionally, none of the antagonists altered basal, agonist-independent [35S]GTPgammaS binding, thus they behaved as pure, silent antagonists at D2short, D4.2 and D4.7 receptors under our conditions. In summary, the data suggest that therapeutic distinctions between typical and atypical antipsychotic drugs cannot be made based on their function at D2short, D4.2 and D4.7 subtypes of dopamine receptors.