腺苷受体配体：急性治疗与慢性治疗的差异
Adenosine receptor ligands: differences with acute versus chronic treatment.
作者信息
Jacobson K A, von Lubitz D K, Daly J W, Fredholm B B
机构信息
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.
出版信息
Trends Pharmacol Sci. 1996 Mar;17(3):108-13. doi: 10.1016/0165-6147(96)10002-x.
Abstract
Adenosine receptors have been the target of intense research with respect to potential use of selective ligands in a variety of therapeutic areas. Caffeine and theophylline are adenosine receptor antagonists, and over the past three decades a wide range of selective agonists and antagonists for adenosine receptor subtypes have been developed. A complication to the therapeutic use of adenosine receptor ligands is the observation that the effects of acute administration of a particular ligand can be diametrically opposite to the chronic effects of the same ligand. This 'effect inversion' is discussed here by Ken Jacobson and colleagues, and has been observed for effects on cognitive processes, seizures and ischaemic damage.
摘要
腺苷受体一直是深入研究的对象，涉及在各种治疗领域中潜在使用选择性配体。咖啡因和茶碱是腺苷受体拮抗剂，在过去三十年里，已开发出多种针对腺苷受体亚型的选择性激动剂和拮抗剂。腺苷受体配体治疗应用中的一个复杂情况是，观察到特定配体急性给药的效果可能与同一配体的慢性效果截然相反。肯·雅各布森及其同事在此讨论了这种“效应反转”，并且在对认知过程、癫痫发作和缺血性损伤的影响方面已观察到这种现象。
相似文献
1
Adenosine receptor ligands: differences with acute versus chronic treatment.腺苷受体配体：急性治疗与慢性治疗的差异
Trends Pharmacol Sci. 1996 Mar;17(3):108-13. doi: 10.1016/0165-6147(96)10002-x.
2
Adenosine receptors as therapeutic targets.腺苷受体作为治疗靶点。
Nat Rev Drug Discov. 2006 Mar;5(3):247-64. doi: 10.1038/nrd1983.
3
The anxiogenic-like effect of caffeine in two experimental procedures measuring anxiety in the mouse is not shared by selective A(2A) adenosine receptor antagonists.在测量小鼠焦虑的两种实验程序中，咖啡因的致焦虑样作用并非选择性A(2A)腺苷受体拮抗剂所共有。
Psychopharmacology (Berl). 2000 Feb;148(2):153-63. doi: 10.1007/s002130050037.
4
A1 adenosine receptors and their ligands: overview and recent developments.A1 腺苷受体及其配体：概述与最新进展
Farmaco. 2001 Jan-Feb;56(1-2):77-80. doi: 10.1016/s0014-827x(01)01005-9.
5
Involvement of adenosine A1 and A2A receptors in the motor effects of caffeine after its acute and chronic administration.急性和慢性给予咖啡因后，腺苷A1和A2A受体在其运动效应中的作用。
Neuropsychopharmacology. 2003 Jul;28(7):1281-91. doi: 10.1038/sj.npp.1300167. Epub 2003 Apr 9.
6
New paradigms in purinergic receptor ligand discovery.嘌呤能受体配体发现的新范式。
Neuropharmacology. 2023 Jun 1;230:109503. doi: 10.1016/j.neuropharm.2023.109503. Epub 2023 Mar 13.
7
Recent progress in the development of adenosine receptor ligands as antiinflammatory drugs.作为抗炎药物的腺苷受体配体开发的最新进展。
Curr Top Med Chem. 2006;6(13):1375-99. doi: 10.2174/15680266106061375.
8
Medicinal chemistry of adenosine A1 receptor ligands.腺苷A1受体配体的药物化学
Curr Top Med Chem. 2003;3(4):355-67. doi: 10.2174/1568026033392165.
9
A(3) adenosine receptor ligands: history and perspectives.A(3) 腺苷受体配体：历史与展望
Med Res Rev. 2000 Mar;20(2):103-28. doi: 10.1002/(sici)1098-1128(200003)20:2<103::aid-med1>3.0.co;2-x.
10
Effects of adenosine receptor agonists and antagonists on audiogenic seizure-sensible DBA/2 mice.腺苷受体激动剂和拮抗剂对听源性癫痫敏感的DBA/2小鼠的影响。
Eur J Pharmacol. 1999 Apr 29;371(2-3):137-45. doi: 10.1016/s0014-2999(99)00132-6.
引用本文的文献
1
Chronic treatment with adenosine A1 receptor antagonist promotes neurogenesis and improves outcome after cerebral ischemia.腺苷A1受体拮抗剂的长期治疗可促进神经发生并改善脑缺血后的预后。
J Cereb Blood Flow Metab. 2025 May 24:271678X251345294. doi: 10.1177/0271678X251345294.
2
Beyond the hype: a comprehensive exploration of CBD's biological impacts and mechanisms of action.超越炒作：对CBD的生物学影响和作用机制的全面探索
J Cannabis Res. 2025 May 11;7(1):24. doi: 10.1186/s42238-025-00274-y.
3
Impact of acute caffeine intake on local tolerance to cold before and after total sleep deprivation.急性咖啡因摄入对完全睡眠剥夺前后局部冷耐受的影响。
Exp Physiol. 2025 Sep;110(9):1254-1270. doi: 10.1113/EP092356. Epub 2025 Mar 27.
4
Adenosine A and A Receptors: Distinct Cardioprotection.腺苷A1和A2受体：不同的心脏保护作用。
Drug Dev Res. 2001 Jan-Feb;52(1-2):366-378. doi: 10.1002/ddr.1136.
5
Caffeine Intake Alters Recovery Sleep after Sleep Deprivation.咖啡因摄入可改变睡眠剥夺后的恢复性睡眠。
Nutrients. 2024 Oct 11;16(20):3442. doi: 10.3390/nu16203442.
6
Relationship between Habitual Caffeine Consumption, Attentional Performance, and Individual Alpha Frequency during Total Sleep Deprivation.习惯性咖啡因摄入与总睡眠剥夺期间注意力表现和个体阿尔法频率的关系。
Int J Environ Res Public Health. 2023 Mar 11;20(6):4971. doi: 10.3390/ijerph20064971.
7
The role of the ATP-adenosine axis in ischemic stroke.三磷酸腺苷-腺苷轴在缺血性卒中中的作用。
Semin Immunopathol. 2023 May;45(3):347-365. doi: 10.1007/s00281-023-00987-3. Epub 2023 Mar 14.
8
Brain activity during a working memory task after daily caffeine intake and caffeine withdrawal: a randomized double-blind placebo-controlled trial.每日摄入咖啡因和戒断咖啡因后进行工作记忆任务时的大脑活动：一项随机、双盲、安慰剂对照试验。
Sci Rep. 2023 Jan 18;13(1):1002. doi: 10.1038/s41598-022-26808-5.
9
Changes in adenosine receptors and neurotrophic factors in the SOD1G93A mouse model of amyotrophic lateral sclerosis: Modulation by chronic caffeine.肌萎缩侧索硬化症 SOD1G93A 小鼠模型中腺苷受体和神经营养因子的变化：慢性咖啡因的调节作用。
PLoS One. 2022 Dec 14;17(12):e0272104. doi: 10.1371/journal.pone.0272104. eCollection 2022.
10
Caffeine intake exerts dual genome-wide effects on hippocampal metabolism and learning-dependent transcription.咖啡因摄入对海马代谢和学习相关转录产生全基因组的双重影响。
J Clin Invest. 2022 Jun 15;132(12). doi: 10.1172/JCI149371.
本文引用的文献
1
Effects of Combinations of Methylxanthines and Adenosine Analogs on Locomotor Activity in Control and Chronic Caffeine-Treated Mice.甲基黄嘌呤与腺苷类似物组合对正常及长期咖啡因处理小鼠运动活性的影响
Drug Dev Res. 1993 Oct;30(2):104-110. doi: 10.1002/ddr.430300209.
2
The role of adenosine receptors in the central action of caffeine.腺苷受体在咖啡因中枢作用中的角色。
Pharmacopsychoecologia. 1994;7(2):201-213.
3
Cerebral ischemia in gerbils: effects of acute and chronic treatment with adenosine A2A receptor agonist and antagonist.沙土鼠脑缺血：腺苷A2A受体激动剂和拮抗剂的急性及慢性治疗效果
Eur J Pharmacol. 1995 Dec 20;287(3):295-302. doi: 10.1016/0014-2999(95)00498-x.
4
Effect of long term caffeine treatment on A1 and A2 adenosine receptor binding and on mRNA levels in rat brain.长期咖啡因治疗对大鼠脑内A1和A2腺苷受体结合及mRNA水平的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1993 Apr;347(4):407-14. doi: 10.1007/BF00165391.
5
Caffeine treatment and withdrawal in mice: relationships between dosage, concentrations, locomotor activity and A1 adenosine receptor binding.小鼠中的咖啡因治疗与戒断：剂量、浓度、运动活性和A1腺苷受体结合之间的关系。
J Pharmacol Exp Ther. 1993 Sep;266(3):1563-72.
6
Downregulation of nicotinic receptor function after chronic nicotine infusion.长期输注尼古丁后烟碱受体功能的下调。
J Pharmacol Exp Ther. 1993 Sep;266(3):1268-76.
7
Long-term caffeine treatment leads to a decreased susceptibility to NMDA-induced clonic seizures in mice without changes in adenosine A1 receptor number.长期咖啡因治疗可使小鼠对N-甲基-D-天冬氨酸（NMDA）诱导的阵挛性癫痫的易感性降低，而腺苷A1受体数量无变化。
Brain Res. 1993 May 28;612(1-2):271-7. doi: 10.1016/0006-8993(93)91672-f.
8
Effects of chronic administration of adenosine A1 receptor agonist and antagonist on spatial learning and memory.慢性给予腺苷A1受体激动剂和拮抗剂对空间学习与记忆的影响。
Eur J Pharmacol. 1993 Nov 16;249(3):271-80. doi: 10.1016/0014-2999(93)90522-j.
9
Effects of N6-cyclopentyl adenosine and 8-cyclopentyl-1,3-dipropylxanthine on N-methyl-D-aspartate induced seizures in mice.N6-环戊基腺苷和8-环戊基-1,3-二丙基黄嘌呤对小鼠N-甲基-D-天冬氨酸诱导癫痫发作的影响。
Eur J Pharmacol. 1993 Nov 16;249(3):265-70. doi: 10.1016/0014-2999(93)90521-i.
10
Chronic caffeine alters the density of adenosine, adrenergic, cholinergic, GABA, and serotonin receptors and calcium channels in mouse brain.长期摄入咖啡因会改变小鼠大脑中腺苷、肾上腺素能、胆碱能、γ-氨基丁酸（GABA）和5-羟色胺受体以及钙通道的密度。
Cell Mol Neurobiol. 1993 Jun;13(3):247-61. doi: 10.1007/BF00733753.
Zotero 插件