Borea P A, Gessi S, Bar-Yehuda S, Fishman P
Faculty of Medicine, University of Ferrara, Department of Clinical and Experimental Medicine, Pharmacology Unit, 44100 Ferrara, Italy.
Handb Exp Pharmacol. 2009(193):297-327. doi: 10.1007/978-3-540-89615-9_10.
The study of the A(3) adenosine receptor (A(3)AR) represents a rapidly growing and intense area of research in the adenosine field. The present chapter will provide an overview of the expression patterns, molecular pharmacology and functional role of this A(3)AR subtype under pathophysiological conditions. Through studies utilizing selective A(3)AR agonists and antagonists, or A(3)AR knockout mice, it is now clear that this receptor plays a critical role in the modulation of ischemic diseases as well as in inflammatory and autoimmune pathologies. Therefore, the potential therapeutic use of agonists and antagonists will also be described. The discussion will principally address the use of such compounds in the treatment of brain and heart ischemia, asthma, sepsis and glaucoma. The final part concentrates on the molecular basis of A(3)ARs in autoimmune diseases such as rheumatoid arthritis, and includes a description of clinical trials with the selective agonist CF101. Based on this chapter, it is evident that continued research to discover agonists and antagonists for the A(3)AR subtype is warranted.
对A(3) 腺苷受体（A(3)AR）的研究是腺苷领域中一个迅速发展且备受关注的研究领域。本章将概述该A(3)AR亚型在病理生理条件下的表达模式、分子药理学及功能作用。通过利用选择性A(3)AR激动剂和拮抗剂或A(3)AR基因敲除小鼠进行的研究，现已明确该受体在缺血性疾病以及炎症和自身免疫性疾病的调节中起关键作用。因此，还将描述激动剂和拮抗剂的潜在治疗用途。讨论将主要涉及此类化合物在治疗脑和心脏缺血、哮喘、脓毒症和青光眼方面的应用。最后一部分聚焦于类风湿关节炎等自身免疫性疾病中A(3)AR的分子基础，并包括对选择性激动剂CF101的临床试验的描述。基于本章内容，显然有必要继续开展研究以发现A(3)AR亚型的激动剂和拮抗剂。
