A review of the discovery, pharmacological characterization, and behavioral effects of the dopamine D2-like receptor antagonist eticlopride.
A review of the discovery, pharmacological characterization, and behavioral effects of the dopamine D2-like receptor antagonist eticlopride.
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DOI：
10.1111/j.1755-5949.2008.00047.x
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发表时间：
2008
影响因子：
5.5
通讯作者：
Nader MA
中科院分区：
文献类型：
--
作者：
Martelle JL;Nader MA
依替氯必利是一种取代的苯甲酰胺类似物，对多巴胺（DA）D2样受体具有高亲和力和选择性，最初被开发为潜在的抗精神病药物。大量的研究已经利用这种药物来更好地了解中枢DA受体功能，D2样受体在行为中的作用，以及阻断这些受体对几种临床前动物模型的影响。这篇综述强调了利用这种药物的研究，并将其与临床上使用的典型和非典型抗精神病药物进行了比较。首先，我们描述了结构-活性关系，因为它涉及到DA受体的结合和行为的后果。其次是几种成像策略的讨论，包括使用依替氯必利在体内，体外和离体检查DA D2样受体的密度和功能。最后，我们讨论了使用依替氯必利在几个行为模型预测抗精神病药物活性，锥体外系副作用（EPS），学习和记忆。虽然依替氯必利未用于临床，但它仍然是了解DA受体功能和行为的可行研究工具。
Eticlopride is a substituted benzamide analog with high affinity and selectivity for dopamine (DA) D2-like receptors that was initially developed as a potential antipsychotic agent. A great deal of research has utilized this drug to better understand central DA receptor function, the role of D2-like receptors in behavior, and the influence of blockade of these receptors on several preclinical animal models. This review highlights research utilizing this drug and compares it to typical and atypical antipsychotics used clinically. First, we describe structure–activity relationships as it relates to binding at DA receptors and the consequences on behavior. This is followed by a discussion of several imaging strategies including the use of eticlopride for in vivo, in vitro, and ex vivo examination of DA D2-like receptor densities and function. Finally, we discuss the use of eticlopride in several behavioral models predictive of antipsychotic activity, extrapyramidal side effects (EPS), and learning and memory. While eticlopride is not used clinically, it remains a viable research tool for understanding DA receptor function and behavior.
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影响因子：
5
作者：
COSTALL, B;NAYLOR, RJ
通讯作者：
NAYLOR, RJ
影响因子：
2.5
作者：
COOLS, AR;HONIG, WMM;VANROSSUM, JM
通讯作者：
VANROSSUM, JM
影响因子：
6.7
作者：
COLLIN, S;ELTAYAR, N;TESTA, B
通讯作者：
TESTA, B
影响因子：
2.3
作者：
Czoty, PW;Gage, HD;Nader, MA
通讯作者：
Nader, MA
DOI：
10.1097/00004850-198901000-00007
发表时间：
1989-01-01
影响因子：
2.6
作者：
COOKSON, JC;NATORF, B;UPPFELDT, G
通讯作者：
UPPFELDT, G