Fredholm B B
Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden.
Pharmacol Toxicol. 1995 Apr;76(4):228-39. doi: 10.1111/j.1600-0773.1995.tb00135.x.
The purine nucleoside adenosine and the purine nucleotide ATP play different roles in the nervous system. Adenosine acts on a family of G protein coupled receptors, collectively called adenosine receptors or P1 purinoceptors. Four members of this family have been cloned and pharmacologically characterized: A1, A2A, A2B and A3. Their distribution, pharmacology and biological roles are briefly discussed. In particular, the evidence that adenosine acting at A1 receptors regulates the release of several neurotransmitters and that adenosine acting at A2A receptors modulates dopaminergic transmission is summarized. ATP acts on receptors called P2 purinoceptors, which appear to fall into at least two main families--G protein coupled receptors and intrinsic ion channels. Their subclassification is becoming clearer as receptors are cloned and new selective agonists and/or antagonists are becoming available. There is an interesting potential for development of drugs targeted at purines or their receptors.
嘌呤核苷腺苷和嘌呤核苷酸ATP在神经系统中发挥着不同作用。腺苷作用于一类G蛋白偶联受体,统称为腺苷受体或P1嘌呤受体。该家族的四个成员已被克隆并进行了药理学表征:A1、A2A、A2B和A3。简要讨论了它们的分布、药理学和生物学作用。特别总结了腺苷作用于A1受体调节几种神经递质释放以及腺苷作用于A2A受体调节多巴胺能传递的证据。ATP作用于称为P2嘌呤受体的受体,这些受体似乎至少分为两个主要家族——G蛋白偶联受体和内在离子通道。随着受体的克隆以及新的选择性激动剂和/或拮抗剂的出现,它们的亚分类越来越清晰。针对嘌呤或其受体的药物开发具有有趣的潜力。