Rolipram

Rolipram is a selective inhibitor of phosphodiesterases 4 (PDE4s) originally developed as an antidepressant agent in 1990s, but fell out of favor because of its undesirable gastrointestinal side effects. Nowadays, rolipram continues to be used in research as a PDE4 inhibitor. PDE4s are responsible for hydrolysis of the cyclic nucleotides cAMP [A2381] and cGMP to 5’-AMP [A0158] and 5’-GMP [G0338], particularly in nerve and immune cells. The inhibition of PDE4s by rolipram induces the elevation of intracellular cAMP concentration. Consequences rolipram-induced elevation of cAMP suppress expression of proinflammatory cytokines and other mediators of inflammation. Rolipram has been reported as a drug for the treatment of autoimmune diseases, Alzheimer's disease, cognitive enhancement, and respiratory diseases like asthma and COPD. Rolipram is a racemic compound, and (R)-rolipram [R0182] is more potent than (S)-rolipram [R0183] as a PDE4 inhibitor. (The product is for research purpose only.)