Expert Opin Emerg Drugs. 2011 Dec;16(4):597-602. doi: 10.1517/14728214.2011.644786. Epub 2011 Dec 7.
Adenosine receptors (ARs), the major targets of caffeine and theophylline, comprise four receptor subtypes designated as A(1), A(2A), A(2B) and A(3). Over a dozen AR agonists are currently in clinical trials for various conditions, including cardiac arrhythmias, neuropathic pain, myocardial perfusion imaging, cardiac ischemia, inflammatory diseases and cancer. Adenosine (nonselective), regadenoson (A(2A)) and dipyridamole (act indirectly via ARs) have received regulatory approval for clinical use. The present editorial will give a brief update on the current status of AR agonists in clinical trials.
腺苷受体(ARs)是咖啡因和茶碱的主要靶点,包括四个受体亚型,分别命名为 A(1)、A(2A)、A(2B)和 A(3)。目前,有十几种 AR 激动剂正在进行各种疾病的临床试验,包括心律失常、神经性疼痛、心肌灌注成像、心肌缺血、炎症性疾病和癌症。腺苷(非选择性)、雷腺苷(A(2A)) 和双嘧达莫(通过 AR 间接作用)已获得监管部门批准用于临床。本社论将简要介绍 AR 激动剂在临床试验中的最新进展。