University of Sydney, School of Chemistry, NSW 2006, Australia.
Expert Opin Ther Pat. 2010 May;20(5):625-46. doi: 10.1517/13543771003702424.
P2X channels are ionotropic purinergic receptors that are currently under scrutiny as attractive targets for novel therapeutics in areas including chronic inflammation, pain and depression. Their wide expression in the CNS, recent advances in the biochemical and pharmacological properties as well as increasing numbers of patents published in this research domain demand a review in this field.
The patent literature covering novel drug-like antagonists for each P2X receptor subtype (P2X1R to P2X7R) up to December 2009 is described in this review article together with their recent highlights in pharmacology.
Readers will gain an up-to-date overview of patents covering drug-like antagonists for seven P2X receptor subtypes within the last 4 years.
P2X7R antagonists and other P2X inhibitors will probably be on the market for combating rheumatoid arthritis and other diseases. Some P2X7R antagonists are already in Phase I and II clinical trials.
P2X 通道是离子型嘌呤能受体，目前正在审查作为有吸引力的目标，为新的治疗方法，包括慢性炎症，疼痛和抑郁。其广泛表达在中枢神经系统，近年来在生化和药理学特性以及越来越多的专利发表在这个研究领域需要审查在这个领域。
专利文献涵盖新的药物样拮抗剂的每个 P2X 受体亚型（P2X1R 到 P2X7R），截至 2009 年 12 月在这篇综述文章与他们最近的亮点在药理学。
读者将获得一个最新的概述专利涵盖药物样拮抗剂为七个 P2X 受体亚型在过去的 4 年。
P2X7R 拮抗剂和其他 P2X 抑制剂可能将在市场上对抗类风湿关节炎和其他疾病。一些 P2X7R 拮抗剂已经在 I 期和 II 期临床试验。
