Rolipram is a selective phosphodiesterase-4 inhibitor.

Rolipram was discontinued after clinical trials showed it could not be used  at high enough levels to be effective without causing significant gastrointestinal side effects.

Bioavailability 75%

Metabolism- Liver via CYP2C8, CYP2C9, CYP2C19 and CYP2D6

Elimination half-life 3 hours

Excretion Urine 80%

The etiology of many neurodegenerative diseases involves misfolded and clumped proteins which accumulate in the brain. 

The proteosome disposes, and in Alzheimer’s disease and some other conditions the activity of these proteasomes is impaired leading to a buildup of toxic aggregates. 

Rolipram has the ability to ramp up the activity of proteasomes and reduce the burden of these aggregates in laboratory studies, suggesting PDE4 inhibitors could be useful in autoimmune diseases, Alzheimer’s disease, cognitive enhancement, spinal cord injury, and respiratory diseases like asthma and COPD.

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