Neuroscience Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW, UK.
Curr Top Med Chem. 2010;10(5):479-92. doi: 10.2174/156802610791111533.
This article highlights recent advances in the discovery of new agonists, antagonists and partial agonists of the 5-HT(1D) receptor. The field of 5-HT(1D) agonists continues to deliver a number of new potential therapeutic agents, although advances in this field are now more focussed on the clinical evaluation phase. The identification of novel compounds is greater for the 5-HT(1D) receptor antagonists, and whilst few truly selective ligands have been identified, a number of approaches are discussed towards defined mixed-pharmacology profiles. An overview is also given of recent advances in biological and clinical understanding of the receptor.
本文重点介绍了 5-HT(1D) 受体新激动剂、拮抗剂和部分激动剂的发现方面的最新进展。尽管该领域的进展现在更加集中在临床评估阶段，但 5-HT(1D) 激动剂仍在不断提供许多新的潜在治疗药物。新型化合物的鉴定在 5-HT(1D) 受体拮抗剂中更为广泛，尽管尚未确定真正的选择性配体，但讨论了一些针对特定混合药理学特征的方法。本文还概述了受体在生物学和临床理解方面的最新进展。
