van Ryn J, Trummlitz G, Pairet M
Department of Pulmonary Research, Boehringer Ingelheim Pharma KG, Biberach/Riss, Germany.
Curr Med Chem. 2000 Nov;7(11):1145-61. doi: 10.2174/0929867003374255.
Increasing amounts of experimental and clinical data support the role of selective cyclooxygenase (COX)-2 inhibition in anti-inflammatory processes and the involvement of COX-1 inhibition in the side effects associated with non steroidal anti-inflammatory drug use. This review will focus on the differences in the structure of the COX-1 and COX-2 molecules, particularly the active site and how they are bound by various NSAIDs to achieve COX-2 selectivity. This COX-2 selectivity will then be characterized in pharmacological assays in vitro and in animal models in vivo. Finally, clinical information available for this new class of selective inhibitors will be discussed.
越来越多的实验和临床数据支持选择性环氧化酶（COX）-2抑制在抗炎过程中的作用，以及COX-1抑制与非甾体抗炎药使用相关副作用的关联。本综述将聚焦于COX-1和COX-2分子结构的差异，尤其是活性位点以及它们如何被各种非甾体抗炎药结合以实现COX-2选择性。然后将在体外药理试验和体内动物模型中对这种COX-2选择性进行表征。最后，将讨论这类新型选择性抑制剂的现有临床信息。
