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.
|Animal models||Male Hartley guinea pigs|
|Formulation||S-(+)-Rolipram is dissolved in 100% PEG at an appropriate concentration.|
|Administration||Administered via i.v.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL|
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