Powell William S
Meakins-Christie Laboratories, McGill University, 3626 St Urbain Street, Montreal, Quebec, Canada H2X 2P2.
Prostaglandins Leukot Essent Fatty Acids. 2003 Aug-Sep;69(2-3):179-85. doi: 10.1016/s0952-3278(03)00079-6.
PGD(2) is a major product of arachidonic acid metabolism by mast cells and is released in the lungs following allergen challenge. Activation of the classic PGD(2) receptor (DP receptor) results in stimulation of adenylyl cyclase, resulting in inhibition of platelet aggregation and smooth muscle relaxation. A second PGD(2) receptor has recently been identified and designated as the DP(2) receptor, or chemoattractant receptor-homologous molecule expressed on Th2 cells. PGD(2) acts through the DP(2) receptor to induce eosinophil chemotaxis, actin polymerization, calcium mobilization, and adhesion molecule expression. The most potent DP(2) receptor agonist yet identified is 15R-methyl-PGD(2), which has the unnatural R configuration at C(15). 15-Deoxy-Delta(12,14)-PGJ(2) is also a potent DP(2) receptor agonist that activates eosinophils at concentrations much lower than those required for its anti-inflammatory effects. Because of its critical location in the lung and its potent effects on eosinophils, PGD(2) may be an important proinflammatory mediator in asthma.
前列腺素D2（PGD(2)）是肥大细胞花生四烯酸代谢的主要产物，在变应原激发后于肺中释放。经典前列腺素D2受体（DP受体）的激活会刺激腺苷酸环化酶，从而抑制血小板聚集并使平滑肌舒张。最近已鉴定出第二种前列腺素D2受体，并将其命名为DP(2)受体，即Th2细胞上表达的趋化因子受体同源分子。PGD(2)通过DP(2)受体发挥作用，诱导嗜酸性粒细胞趋化、肌动蛋白聚合、钙动员以及黏附分子表达。目前已鉴定出的最有效的DP(2)受体激动剂是15R-甲基-PGD(2)，其在C(15)处具有非天然的R构型。15-脱氧-Δ(12,14)-PGJ(2)也是一种有效的DP(2)受体激动剂，其激活嗜酸性粒细胞的浓度远低于其发挥抗炎作用所需的浓度。由于其在肺中的关键位置以及对嗜酸性粒细胞的强效作用，PGD(2)可能是哮喘中一种重要的促炎介质。
