STRUCTURE AND FUNCTION OF ADENOSINE-A1-RECEPTORS
STRUCTURE AND FUNCTION OF ADENOSINE-A1-RECEPTORS
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DOI：
10.1096/fasebj.5.12.1916091
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发表时间：
1991-09-01
期刊：
影响因子：
4.8
通讯作者：
LINDEN, J
中科院分区：
文献类型：
--
作者：
LINDEN, J
A1腺苷受体是广泛分布的嘌呤能受体家族中最具特征的受体。 纯化的脑A1受体是单体35- 36-kDa糖蛋白。 根据与选择性配体的结构活性关系，A1受体可与A2腺苷受体明确区分。 最近的结构活性数据表明可能存在A1（A1 a，A1 b和A3）和A2（A2 a和A2 b）受体亚型。 A1受体介导的反应通过多种百日咳毒素敏感性GTP结合蛋白（G蛋白）与各种组织中的许多不同效应物偶联：腺苷酸环化酶、磷脂酶C、Na+-Ca 2+交换、Ca 2+通道、Cl-通道和K+通道。 钙动员磷酸肌醇的形成可以被增强或抑制。 一般来说，腺苷被发现与其他激素或神经递质一起以抑制或刺激的方式起作用。 腺苷的无数调节作用表明：1）腺苷可在同一细胞内同时产生多种效应; 2）A1受体的激活可导致其他受体与其G蛋白偶联的减少或增加。
The A1 adenosine receptor is the best characterized of the widely distributed purinergic receptor family. The purified brain A1 receptor is a monomeric 35- to 36-kDa glycoprotein. A1 receptors can be clearly distinguished from A2 adenosine receptors on the basis of structure activity relationships with selective ligands. Recent structure activity data suggest that subtypes of A1 (A1a, A1b, and A3) and A2 (A2a and A2b) receptors may exist. A1 receptor-mediated responses are coupled via multiple pertussis toxin-sensitive GTP binding proteins (G proteins) to many different effectors in various tissues: adenylate cyclase, phospholipase C, Na+-Ca2+ exchange, Ca2+ channels, Cl- channels, and K+ channels. The formation of calcium-mobilizing inositol phosphates can either be enhanced or inhibited. In general, adenosine has been found to act in concert with other hormones or neurotransmitters in either an inhibitory or a stimulatory way. The myriad modulatory actions of adenosine suggest that: 1) adenosine may simultaneously produce multiple effects within the same cell; and 2) activation of A1 receptors may lead to either a decrease or an increase in the coupling of other receptors to their G proteins.