S- (+)-Rolipram is a less active enantiomer of the PDE4 inhibitor with an EC50 of 1.0 uM. It is an anti-inflammatory drug. Rolipram is being studied as a possible alternative to current antidepressants. Recent studies show that rolipram may have antipsychotic effects. It displays activity 10-fold less than R-rolipram at inhibition of PDE IV. It inhibits antigen-induced contraction of guinea-pig colonic smooth muscle.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Hartley guinea pigs |
| Formulation | S-(+)-Rolipram is dissolved in 100% PEG at an appropriate concentration. |
| Dosages | 1 mL/kg |
| Administration | Administered via i.v. |
| Molecular Weight | 275.34 |
| Formula | C16H21NO3 |
| CAS Number | 85416-73-5 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Seyed Mohammad Nabavi, et al. Phosphodiesterase inhibitors say NO to Alzheimer's disease
[4] Kam Leung. 4-(3-Cyclopentoxy-4-[ 11 C]methoxy-phenyl)pyrrolidin-2-one
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