Rolipram

Rolipram, an selective inhibitor of cyclic AMP - cAMP (type 4 cyclic adenosine monophosphate) phosphodiesterase (PDE4) - facilitates the establishment of long-lasting long-term potentiation and improves memory.

Chemical Formula: C16H21N03

Chemical Name: : 4-[3-(Cyclopentyloxy)-4-methoxy-phenyl]-2-pyrrolidinone, ZK-62711

Molecular Weight: M.W. 275.4

Appearance: White Solid

Storage: +4°C.

Rolipram is a selective inhibitor of phosphodiesterase IV. Inhibition of PDE4 causes an elevation of intracellular cAMP and norepinephrine which supress the expression of pro-inflammatory cytokines including TNF alpha.

Effects of this drug include a reduction in depression and inhibition of central nervous system inflammation. Though its modification of cAMP and cGMP Rolipram has an effect on cell cycle causing a cytostatic arrest at G1 and M phase.

Rolipram and Depression

Various results suggest that PDE4D is an essential mediator of the antidepressant-like effects of rolipram, and that PDE4D-regulated cyclic adenosine monophosphate signaling may play a role in the pathophysiology and pharmacotherapy of depression.

Some studies suggest that the discriminative stimulus effects of rolipram appear to be unrelated to its antidepressant-like effect, but may provide a surrogate marker for central nervous system-related side effects of PDE4 inhibitors.

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

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.

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