Rolipram is a selective inhibitor of phosphodiesterasesPDE 4, especially thePDE 4B with IC50 of 130 nM while IC50 for PDE4D is 240 nM, it's an anti-inflammatory agent.
cAMP is a fundamental second-messenger molecule produced in essentially all mammalian cells. 3′5′-Cyclic nucleotide phosphodiesterases (PDEs) are the enzymatic machinery that is responsible for the degradation of cAMP in cells by catalysing the hydrolysis of cAMP to 5′AMP. PDE4 family members specifically degrade cAMP, and they are expressed essentially in all immune cells including macrophages, neutrophils, eosinophils and lymphocytes, and in many other cell types, including epithelial cells, endothelium and fibroblasts. Rolipram is a selective inhibitor of phosphodiesterase PDE4, especially the PDE4B with IC50 of 130 nM and IC50 of 240 nM for PDE4D, with anti-inflammatory activity. Transient global cerebral ischemia in rats was induced by BCCAO. Rolipram at 0.3 mg/kg, but not 0.1 mg/kg, increased the time spent in the open arms and Discrimination index in the object location task, and the number of DCX-immunoreactive (DCX is a microtubule protein transiently expressed in both cytoplasm and dendrites of newborn neurons) neurons in BCCAO mice as compared to the BCCAO + veh group[3]. Bevacizumab (6.5 μg/ml) and rolipram (103 μM) individually led to the significant increase in the relative values of p53 and cleaved-caspase3 expressions in glioblastoma cancer stem-like cells (GCSCs) and the effect was strongly amplified when bevacizumab and rolipram were added to culture medium simultaneously[4]. Rolipram inhibited LPS-induced TNF production and TNF mRNA levelsin a dose-dependent manner (IC50 25.9 nM) in J774 mouse macrophages, which was mediated by MAPK phosphatase-1 (MKP-1)[5].
Rolipram 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
COS7 cells
Function assay
Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis, IC50=0.105 μM
18222088
HEK293 cells
Function assay
Inhibition of PDE4 expressed in HEK293 cells coexpressing G-protein coupled receptor and cyclic nucleotide gated ion channel by fluorescence assay, EC50=0.1315 μM
19464886
human PBMC
Function assay
Inhibition of LPS-induced TNFalpha production in human PBMC, IC50=0.06 μM
19049349
human U937 cells
Function assay
Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting, IC50=0.86 μM
United States, Maryland
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National Institutes of Health Clinical Center
Recruiting
Bethesda, Maryland, United States, 20892
Contact: For more information at the NIH Clinical Center contact Office of Patient Recruitment (OPR) 800-411-1222 ext TTY8664111010 prpl@cc.nih.gov 收起 <<
Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis, IC50=0.105 μM
18222088
HEK293 cells
Function assay
Inhibition of PDE4 expressed in HEK293 cells coexpressing G-protein coupled receptor and cyclic nucleotide gated ion channel by fluorescence assay, EC50=0.1315 μM
19464886
human PBMC
Function assay
Inhibition of LPS-induced TNFalpha production in human PBMC, IC50=0.06 μM
19049349
human U937 cells
Function assay
Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting, IC50=0.86 μM
19303290
rat UMR106 cells
Function assay
Inhibition of PDE in rat UMR106 cells co-expressing CRE-luc assessed as PTH-induced cAMP accumulation by luciferase reporter gene assay, IC50=0.6 μM
22030030
Sf9 cells
Function assay
Inhibition of recombinant human PDE4A expressed in Sf9 cells, IC50=4 nM
United States, Maryland
... 展开 >>
National Institutes of Health Clinical Center
Recruiting
Bethesda, Maryland, United States, 20892
Contact: For more information at the NIH Clinical Center contact Office of Patient Recruitment (OPR) 800-411-1222 ext TTY8664111010 prpl@cc.nih.gov 收起 <<
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