ADENOSINE RECEPTORS - TARGETS FOR FUTURE DRUGS
ADENOSINE RECEPTORS - TARGETS FOR FUTURE DRUGS
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DOI：
10.1021/jm00345a001
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发表时间：
1982-01-01
影响因子：
7.3
通讯作者：
DALY, JW
中科院分区：
文献类型：
--
作者：
DALY, JW
腺苷的显著的镇静、解痉和血管舒张作用在50多年前被首次认识到。[1]在此期间，腺苷和前体腺嘌呤核苷酸的生物学作用的数量大大增加。细胞外腺苷受体和腺嘌呤核苷酸受体已被鉴定。在许多细胞中，腺苷受体似乎与腺苷酸环化酶相连，而核苷酸受体可能控制离子流。近年来，各种腺苷类似物和ATP类似物被引入到这些受体功能的研究中。一些腺苷类似物如图I所示。烷基黄嘌呤，如咖啡因和茶碱，是最著名的腺苷受体拮抗剂。最近，一些非常有效的黄嘌呤拮抗剂已经开发出来。一些腺苷拮抗剂如图II所示。目前似乎还没有令人满意的特异性ATP受体拮抗剂，腺苷可能是一种通用的调节物质，因为似乎没有特定的细胞类型或组织专门负责其形成。在这方面，腺苷与各种内分泌激素不同。也没有任何证据表明腺苷能从神经或其他细胞中储存和释放出来。因此，腺苷不同于各种神经递质物质。嘌呤能的存在
The profound hypotensive, sedative, antispasmodic, and vasodilatory actions of adenosine were first recognized over 5 decades ago. 1 During the intervening years the number of biological roles proposed for adenosine and for precursor adenine nucleotides have increased considerably. Extracellular adenosine receptors and adenine nucleotide re-ceptors have been identified. The adenosine receptors appear linked in many cells to adenylate cyclase, while nucleotide receptors probably control ion fluxes. A variety of adenosine analogues and ATP analogues have been introduced in recentyears for the study of these receptor functions. Some of the adenosine analogues are shown in Chart I. Alkylxanthines, such as caffeine and theophyl-line, are the best known antagonists of adenosine receptors. Recently some extremely potent xanthine antagonists have been developed. Some of the adenosine antagonists are depicted in ChartII. There do not appear to be any satisfactory specific ATP-receptor antagonists at the present time.Adenosine perhaps represents a general regulatory substance, since no particular cell type or tissue appears uniquely responsible for its formation. In this regard, adenosine is unlike variousendocrine hormones. Nor is there any evidence for storage and release of adenosine from nerve or other cells. Thus, adenosine is unlike various neurotransmitter substances. The presence of purinergic