| Stereochemistry | RACEMIC |
| Molecular Formula | C16H21NO3 |
| Molecular Weight | 275.3428 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(OC2CCCC2)C=C(C=C1)C3CNC(=O)C3
InChI
InChIKey=HJORMJIFDVBMOB-UHFFFAOYSA-N
InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)
Rolipram is a selective phosphodiesterase-4 inhibitor discovered and developed by Schering AG as a potential antidepressant drug in the early 1990s. Rolipram was discontinued after clinical trials showed that its therapeutic window was too narrow. Rolipram could not be dosed at high enough levels to be effective without causing significant gastrointestinal side effects. Rolipram promotes apoptosis in HL60 cells through a cAMP-independent mechanism and has been shown to enhance neuronal survival.
CNS Activity
Originator
Approval Year
Cmax
AUC
T1/2
Doses
AEs
PubMed
Patents
Sample Use Guides
Rolipram in Stage I were dosed up to 9 mg/day (3 mg, three times daily), patients in Stage II were dosed only up to 7.5 mg/day
Route of Administration:
Oral
The Glioblastoma cancer stem-like cells isolated from T2 at 5th passages having a purity of >95% based on the assessment of CD133 and CD15 expressions were harvested and seeded in 24-well plates containing DMEM-F12 at a density of 2.5 × 104 cells/well, overnight. The cells were treated with various concentrations (1, 3, 10, 30, 100 μg/ml) of bevacizumab (Roche, Switzerland) for 48 h. All treatments were done in quadruplicate. After finding of half maximal inhibitory concentration (IC50) of bevacizumab, the cells incubated with bevacizumab at IC50 in the absence or presence of rolipram (103 μM).
ACTIVE MOIETY
