Departments of Biomedical Sciences, School of Medicine, University of Missouri-Kansas City, Kansas City, MO 64108, USA.
Int J Mol Sci. 2024 Jul 19;25(14):7903. doi: 10.3390/ijms25147903.
Caffeine (1,3,7-trimethylxanthine) is a naturally occurring methylxanthine that acts as a potent central nervous system stimulant found in more than 60 different plants and fruits. Although caffeinated beverages are widely and casually consumed, the application of caffeine beyond dietary levels as pharmacologic therapy has been recognized since the beginning of its recorded use. The analgesic and vasoactive properties of caffeine are well known, but the extent of their molecular basis remains an area of active research. There is existing evidence in the literature as to caffeine's effect on TRP channels, the role of caffeine in pain management and analgesia, as well as the role of TRP in pain and analgesia; however, there has yet to be a review focused on the interaction between caffeine and TRP channels. Although the influence of caffeine on TRP has been demonstrated in the lab and in animal models, there is a scarcity of data collected on a large scale as to the clinical utility of caffeine as a regulator of TRP. This review aims to prompt further molecular research to elucidate the specific ligand-host interaction between caffeine and TRP by validating caffeine as a regulator of transient receptor potential (TRP) channels-focusing on the transient receptor potential vanilloid 1 (TRPV1) receptor and transient receptor potential ankyrin 1 (TRPA1) receptor subtypes-and its application in areas of pain.
咖啡因（1,3,7-三甲基黄嘌呤）是一种天然存在的甲基黄嘌呤，作为一种有效的中枢神经系统兴奋剂，存在于 60 多种不同的植物和水果中。尽管含咖啡因的饮料被广泛随意地消费，但咖啡因在饮食水平之外作为药物治疗的应用自其被记录使用以来就已经被认识到了。咖啡因的镇痛和血管活性特性是众所周知的，但它们的分子基础的程度仍然是一个活跃的研究领域。文献中有证据表明咖啡因对 TRP 通道的影响、咖啡因在疼痛管理和镇痛中的作用以及 TRP 在疼痛和镇痛中的作用；然而，还没有一篇综述专注于咖啡因与 TRP 通道之间的相互作用。尽管咖啡因对 TRP 的影响在实验室和动物模型中已经得到了证明，但关于咖啡因作为 TRP 调节剂的临床应用的大规模数据仍然很少。这篇综述旨在通过验证咖啡因作为瞬时受体电位 (TRP) 通道调节剂来促进进一步的分子研究，重点是瞬时受体电位香草素 1 (TRPV1) 受体和瞬时受体电位锚蛋白 1 (TRPA1) 受体亚型及其在疼痛领域的应用。
