Description
Product Usage Information
Rolipram is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 1 mg of powder in 0.36 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Storage
Store lyophilized at room temperature, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles .
Background
The small-molecule Rolipram is an inhibitor of phosphodiesterase 4 (PDE4), which catalyzes the hydrolysis of cyclic-AMP (cAMP) to regulate cellular responses to a number of extracellular signals. Rolipram inhibits multiple isozymes of PDE4, including PDE4A (IC = 3 nM), PDE4B (IC = 130 nM), and PDE4D (IC = 240 nM). Treatment of myeloid cells with Rolipram resulted in phosphorylation of cAMP-response element-binding protein (CREB) and implied the presence of both high (PDE4A4) and low affinity (PDE4B, PDE4D) components (1). Rolipram and other phosphodiesterase inhibitors were seen as having potential therapeutic benefits in preclinical models of psychiatric and neurologic diseases. Unfortunately, severe dose-limiting side effects (e.g., nausea, vomiting) limited the clinical application of PDE inhibitors (2). Still, Rolipram treatment in a mouse model of intracerebral hemorrhage demonstrated some neuroprotective benefits through activation of the cAMP/AMPK/SIRT1 pathway (3). Rolipram treatment of fibroblasts from ligamentum flavum hypertrophy patients inhibited PDE4A and PDE4B activity, blocked TGF-β1 by restoring p-ERK1/2 expression, and inhibited expression of fibrosis-related proteins (4).
Alternate Names
4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone (racemic; R,S); ZK 62711
