A phosphodiesterase-4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action of phosphodiesterase 4 (PDE4) on cyclic adenosine monophosphate (cAMP). It is a member of the larger family of PDE inhibitors .

2023年5月10日 · 磷酸二酯酶4 (phosphodiesterase4, PDE4)是磷酸二酯酶家族中重要成员之一，可特异性水解环磷酸腺苷 (cyclic adenosine monophosphate, cAMP)，通过改变cAMP浓度引发下游磷酸化级联反应，与多种疾病密切相关。 靶向PDE4的抑制剂临床研究包括呼吸系统疾病、自身免疫性疾病、中枢神经系统疾病及皮肤病等多种疾病领域。 但是在已上市的PDE4抑制剂临床研究中发现，大多数药物的恶心、呕吐等胃肠道不良反应发生率较高，限制了其临床应用。

2024年5月31日 · pde4是各种炎症性疾病的靶标，除ad外，还包括哮喘、慢性阻塞性肺疾病和类风湿性关节炎等疾病。 目前，具有AD适应症的临床或上市PDE4小分子抑制剂共有11种（表1）。

pde4抑制剂的抗炎作用机制主要涉及[5，8，9]：①抑制多种炎症介质/细胞因子的释放，能够抑制th 2细胞il-4、 il-5基因的表达。②抑制白细胞的激活(呼吸爆发)，抑制白细胞游走。③ 抑制细胞 粘附因子(cam)的表达或上调。④诱导产生具有抑制活性的细胞因子，如il-6。

PDE4:分布于被广泛表达于各种组织内。 其作用包括调节脑功能、调节单核细胞及巨噬细胞功能、血管平滑肌细胞增殖等； PDE5:分布于心脏、血小板、血管平滑肌、脑、肾、肺和骨骼肌;其主要作用包括调节血管收缩，尤其是阴茎和肺部血管的舒缩，同时通过调节 NO-cGMP 信号系统调节血小板聚集等； PDE6:分布于视觉系统中;其主要作用在于调节眼部视觉信号的传输; PDE7:分布于免疫系统、骨骼肌、内皮细胞、神经系统等;主要被报道作用于 T 细胞的活化及免疫调节方面; …

Phosphodiesterase-4 (PDE4) involves in the regulation of proinflammatory cytokines via the degradation of cyclic adenosine monophosphate. 磷酸二酯酶 4 (PDE4)，是一种属于 Phosphodiesterase (PDE) 的酯酶，负责降解 cAMP and cGMP。磷酸二酯酶 4 降解环磷酸腺苷参与调节促炎细胞因子。

The phosphodiesterase 4 (PDE4) enzyme family plays a pivotal role in regulating levels of the second messenger cAMP. Consequently, PDE4 inhibitors have been investigated as a therapeutic strategy to enhance cAMP signaling in a broad range of diseases, including several types of cancers, as well as i …

Phosphodiesterase-4 (PDE4), mainly present in immune cells, epithelial cells, and brain cells, manifests as an intracellular non-receptor enzyme that modulates inflammation and epithelial integrity. Inhibition of PDE4 is predicted to have diverse ...

2005年11月15日 · Here, we delineate the range of PDE4 isoforms, their role in signaling, their structural biology and related preclinical and clinical pharmacology. Cyclic nucleotide phosphodiesterases (PDEs) provide the only route for degrading cyclic AMP (cAMP), a key second messenger inside cells, thus providing a pivotal means of regulating cAMP levels.

Selective PDE4D inhibitors (PDE4Dis) could represent an innovative and valid therapeutic strategy for the treatment of various neurodegenerative diseases, such as Alzheimer’s, Parkinson’s, Huntington’s, and Lou Gehrig’s diseases, but also for stroke, traumatic brain and spinal cord injury, mild cognitive impairment, and all demyelinating disease...