Department of Pharmacology, M.R. Medical College, Sedam Road, Gulbarga-585 105, India.
Indian J Pharmacol. 2009 Jun;41(3):97-105. doi: 10.4103/0253-7613.55202.
Adenosine, a purine nucleoside has been described as a 'retaliatory metabolite' by virtue of its ability to function in an autocrine manner and to modify the activity of a range of cell types, following its extracellular accumulation during cell stress or injury. These effects are largely protective and are triggered by binding of adenosine to any of the four adenosine receptor subtypes namely A1, A2a, A2b, A3, which have been cloned in humans, and are expressed in most of the organs. Each is encoded by a separate gene and has different functions, although overlapping. For instance, both A1 and A2a receptors play a role in regulating myocardial oxygen consumption and coronary blood flow. It is a proven fact that adenosine plays pivotal role in different physiological functions, such as induction of sleep, neuroprotection and protection against oxidative stress. Until now adenosine was used for certain conditions like paroxysmal supraventricular tachycardia (PSVT) and Wolff Parkinson White (WPW) syndrome. Now there is a growing evidence that adenosine receptors could be promising therapeutic targets in a wide range of conditions including cardiac, pulmonary, immunological and inflammatory disorders. After more than three decades of research in medicinal chemistry, a number of selective agonists and antagonists of adenosine receptors have been discovered and some have been clinically evaluated, although none has yet received regulatory approval. So this review focuses mainly on the newer potential role of adenosine and its receptors in different clinical conditions.
腺苷是一种嘌呤核苷,由于其在外周细胞应激或损伤时细胞外积累后,能够以自分泌的方式发挥作用并调节多种细胞类型的活性,因此被描述为一种“报复性代谢物”。这些作用在很大程度上是保护性的,是由腺苷与任何四种腺苷受体亚型(A1、A2a、A2b、A3)结合触发的,这四种受体亚型已在人类中被克隆,并在大多数器官中表达。每个受体都由一个单独的基因编码,具有不同的功能,尽管有重叠。例如,A1 和 A2a 受体都在调节心肌耗氧量和冠状动脉血流量方面发挥作用。事实证明,腺苷在不同的生理功能中起着关键作用,例如诱导睡眠、神经保护和对抗氧化应激。直到现在,腺苷一直被用于某些疾病,如阵发性室上性心动过速(PSVT)和沃夫-帕金森-怀特(WPW)综合征。现在有越来越多的证据表明,腺苷受体可能是包括心脏、肺、免疫和炎症性疾病在内的广泛疾病的有前途的治疗靶点。经过三十多年的药物化学研究,已经发现了一些腺苷受体的选择性激动剂和拮抗剂,并且已经进行了一些临床评估,尽管尚未获得监管部门的批准。因此,本综述主要关注腺苷及其受体在不同临床情况下的新的潜在作用。