Non‐Xanthine Antagonists for the Adenosine A1 Receptor
Non‐Xanthine Antagonists for the Adenosine A1 Receptor
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DOI：
10.1002/cbdv.200490122
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发表时间：
2004-11
影响因子：
2.9
通讯作者：
Lisa C W Chang;J. Brussee;A. IJzerman
中科院分区：
文献类型：
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作者：
Lisa C W Chang;J. Brussee;A. IJzerman
腺苷（图1）是一种内源性配体，通过三磷酸腺苷（ATP）的分解在细胞外空间形成。它作为一种局部激素，负责许多生理功能。腺苷的作用是通过具有相同名称的细胞膜受体进行的。这些受体是G蛋白偶联受体（GPCR）的实例，并且由通过内外环连接的七个跨膜螺旋结构域组成。腺苷受体有四种类型，A1，A2A，A2B和A3 [1] [2]。目前的命名法是基于货车Calker等人[1]提出的命名法，他将A1受体定义为抑制腺苷酸环化酶，A2受体因此对该第二信使具有刺激作用。A2受体的进一步分类是描述高和低亲和力结合位点的实验结果[3] [4]。A3腺苷受体是以一种反向的方式发现的，在发现其功能之前，首先克隆并测序了受体[5]。
Adenosine (Fig. 1) is an endogenous ligand formed in extracellular space by the breakdown of adenosine triphosphate (ATP). It acts as a local hormone and is responsible for many physiological functions. The actions of adenosine are conducted through cell-membrane receptors bearing the same name. These receptors are examples of G-protein-coupled receptors (GPCRs) and consist of seven transmembrane -helical domains connected by intraand extracellular loops. There are four categories of adenosine receptors, the A1, A2A, A2B, and the A3 [1] [2]. The current nomenclature is based on that proposed by Van Calker et al. [1], who defined the A1 receptor as being inhibitory to adenylate cyclase and the A2 receptor as consequently stimulatory to this secondary messenger. Further categorization of the A2 receptors was a result of experimental findings describing highand low-affinity binding sites [3] [4]. The A3 adenosine receptor was discovered in a −reversed× manner, where the receptor was first cloned and sequenced before its function was discovered [5].