(R)-Rolipram

(R)-Rolipram is the R-enantiomer of rolipram, a selective phosphodiesterase 4 inhibitor with antidepressant properties. It acts by inhibiting the enzyme phosphodiesterase 4, leading to increased intracellular levels of cyclic AMP. This mechanism is associated with antidepressant effects and has been explored for potential use in neurodegenerative diseases, cognitive enhancement, autoimmune diseases, and respiratory conditions such as asthma and COPD. The R-enantiomer is more potent than the S-enantiomer as a PDE4 inhibitor[1][3][5]. Despite promising preclinical results, clinical development was discontinued due to a narrow therapeutic window and significant gastrointestinal side effects at effective doses[9].

Other names

(R)-(−)-rolipram(R)-4-(3-Cyclopentyloxy-4-methoxyphenyl)-pyrrolidin-2-one(-)-Rolipram