Martelle Jennifer L, Nader Michael A
Department of Physiology and Pharmacology, Wake Forest University School of Medicine, Winston-Salem, NC 27157-1083, USA.
CNS Neurosci Ther. 2008 Fall;14(3):248-62. doi: 10.1111/j.1755-5949.2008.00047.x.
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.
依托必利是一种对多巴胺（DA）D2样受体具有高亲和力和选择性的取代苯甲酰胺类似物，最初被开发为一种潜在的抗精神病药物。大量研究利用这种药物来更好地理解中枢DA受体功能、D2样受体在行为中的作用，以及这些受体的阻断对几种临床前动物模型的影响。这篇综述重点介绍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比较。首先，我们描述与DA受体结合相关的构效关系及其对行为的影响。接下来讨论几种成像策略，包括使用依托必利进行体内、体外和离体DA D2样受体密度和功能的检测。最后，我们讨论依托必利在几种预测抗精神病活性、锥体外系副作用（EPS）以及学习和记忆的行为模型中的应用。虽然依托必利未用于临床，但它仍然是理解DA受体功能和行为的一种可行的研究工具。
