背景 磷酸二酯酶抑制剂(phosphodiesterase inhibitors PDEIs)是一类抑制磷酸二酯酶（PDE）活性的药物，其主要作用是抑制磷酸二酯酶的活性，降低细胞内第二信使（cAMP或cGMP）的水解，因而提升cAMP或cGMP的浓度，产生多种生物学效应。选择性磷酸二酯酶3, 4，5抑制剂的临床应用研究早期多在心血管功能调整方面，近来扩展到其他治疗领域。目的 对PDE 3、PDE 4和PDE 5抑制剂在治疗肺水肿、肺高压和急性肺损伤中的应用进行介绍。内容 肺血管内皮细胞和肺血管平滑肌细胞分别有PDE 3、PDE 4和PDE 5分布，它们在维持血管内皮的完整性以及血管平滑肌的舒缩方面发挥着一定生物学作用。本文对PDEIs通过抑制PDE活性，影响肺血管内皮细胞完整性以及肺微血管的舒缩功能，达到保护和维持肺内皮和肺血管功能的作用机理及临床应用现状进行介绍。趋向 通过了解PDEIs药物治疗的药理学基础，有望在临床治疗肺高压、肺水肿和肺损伤方面发挥更大的作用。
Background Phosphodiesterase inhibitors (PDEIs) are kinds of drugs which inhibit phosphodiesterase, decrease hydrolysis the second of messengers the cAMP and cGMP , thus increase concentrations of intracellular of cAMP and cGMP which produce more biology effects. Last decade the research of PDE 3、PDE4 and PDE 5 inhibitors were about in clinic regulation of heart and vascular function, recent studies extend other therapy areas. Aim To introduce PDE 3、PDE 4 and PDE 5 inhibitors application in treatment lung edema, pulmonary hypertension and acute lung injury. Content It is widely recognized that PDE 3、PDE 4 and PDE 5 were existed in pulmonary vascular endothelial cells and pulmonary smooth muscle cells, the biologic function of them to maintain the integrity of the vascular endothelium and regulation vascular smooth muscle contraction. This paper review the application and mechanism about PDEIs through inhibit PDEs to keep the pulmonary endothelium and regulate vascular. Trend To understand the pharmacology of PDEIs mechanisms may lead to the development of novel therapeutic approaches for lung edema, pulmonary hypertension and acute lung injury.
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