The antidepressant and antiinflammatory effects
of rolipram in the central nervous system

Zhu J, Mix E, Winblad B.
Division of Geriatric Medicine,
Department of Clinical Neuroscience,
Karolinska Institutet,
Huddinge Hospital,
S-141 86 Stockholm, Sweden.
CNS Drug Rev. 2001 Winter;7(4):387-98


Rolipram is a selective inhibitor of phosphodiesterases (PDE) IV, especially of the subtype PDE IVB. These phosphodiesterases are responsible for hydrolysis of the cyclic nucleotides cAMP and cGMP, particularly in nerve and immune cells. Consequences of rolipram-induced elevation of intracellular cAMP are increased synthesis and release of norepinephrine, which enhance central noradrenergic transmission, and suppress expression of proinflammatory cytokines and other mediators of inflammation. In humans and animals rolipram produces thereby a variety of biological effects. These effects include attenuation of endogenous depression and inflammation in the central nervous system (CNS), both effects are of potential clinical relevance. There are some discrepancies between in vitro and in vivo effects of rolipram, as well as between results obtained in animal models and clinical studies. The clinical use of rolipram is limited because of its behavioral and other side effects. Newly developed selective PDE IV inhibitors with presumably higher potency and lower toxicity are currently under investigation.
Rolipram plus imipramine
Cytokines and depression
Rolipram and wakefulness
Rolipram and new brain cells
Phosphodiesterase inhibitors
Antidepressant rolipram and PDE4D
Rolipram reduces excitotoxic neuronal damage
PDE4D inhibitor rolipram and glucocorticoid receptors

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