| 应用 |
Roflumilast-d is intended for use as an internal standard for the quantification of roflumilast by GC- or LC-MS. Roflumilast is an inhibitor of phosphodiesterase 4 (PDE4; IC = 0.8 nM). It is selective for PDE4 over PDE1, -2, -3, and -5 (ICs = >10, >10, >10, and 8 µM, respectively). Roflumilast inhibits the production of leukotriene B (LTB;) induced by fMLP in isolated human neutrophils with an IC value of 2 nM. It reduces the proliferation of anti-CD3 and anti-CD28-stimulated isolated human CD4 T cells (IC = 7 nM). Roflumilast (5mg/kg) prevents pulmonary inflammatory cell infiltration and emphysema in mice exposed to cigarette smoke. Formulations containing roflumilast have been used in the treatment of chronic obstructive pulmonary disease (COPD). |
