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Dopamine D3 receptor ligands - Recent advances in the control of subtype selectivity and intrinsic activity

机译:多巴胺D3受体配体-控制亚型选择性和内在活性的最新进展

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摘要

Various pharmacological studies have implicated the dopamine D-3 receptor as an interesting therapeutic target in the treatment of different neurological disorders. Because of these putative therapeutic applications, D-3 receptor ligands with diverse intrinsic activities have been an active field of research in recent years. Separation of purely D-3-mediated drug effects from effects produced by interactions with similar biogenic amine receptors allows to verify the therapeutic impact of D-3 receptors and to reduce possible side-effects caused by "promiscuous" receptor interactions. The requirement to gain control of receptor selectivity and in particular subtype selectivity has been a challenging task in rational drug discovery for quite a few years. In this review, recently developed structural classes of D-3 ligands are discussed, which cover a broad spectrum of intrinsic activities and show interesting selectivities. (c) 2006 Elsevier B.V. All rights reserved.
机译:各种药理研究表明,多巴胺D-3受体是治疗不同神经系统疾病的有趣治疗靶标。由于这些推定的治疗应用,近年来具有多种固有活性的D-3受体配体已经成为研究的活跃领域。将纯D-3介导的药物作用与与相似的生物胺受体的相互作用所产生的作用分开,可以验证D-3受体的治疗作用,并减少“混杂”受体相互作用引起的可能的副作用。控制受体选择性,尤其是亚型选择性的控制要求,在合理的药物开发中已经有很多年了。在这篇综述中,讨论了最近开发的D-3配体的结构类别,这些结构类别涵盖了广泛的内在活性并显示出有趣的选择性。 (c)2006 Elsevier B.V.保留所有权利。

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