Rolipram

  • IUPAC: (RS ) -4 - (3- cyclopentyloxy-4 -methoxyphenyl ) pyrrolidin- 2-one
  • ZK 62711

White, crystalline, solid

Phosphodiesterase inhibitors

PDE4 inhibition

0.2 g · l -1 in water, 7 g · l-1 in ethanol, 7.3 g · l-1 in DMSO

Attention

Template: Infobox chemical / molecular formula search available

Rolipram is an experimental drug in 1979 for the first time and described in the literature. It is an inhibitor of phosphodiesterase -4 and reduces the degradation of the second messenger cAMP by intracellular phosphodiesterases. Rolipram is considered the archetype of phosphodiesterase -4 inhibitors.

Rolipram is a γ -lactam.

Animal effects

Rolipram be due to animal studies, among others the following effects attributed to:

  • Antidepressant effects
  • Antipsychotic effects
  • Anti-inflammatory effects, particularly in autoimmune diseases
  • Positive effects on memory function
  • Neuroprotective effects

Clinical Effects

Rolipram was developed by Schering AG, inter alia for the treatment of depression and multiple sclerosis. However, it was not yet approved as a drug.

Most of the published information on the application in humans are for the indication of depression before. The clinical development of depression has been set, however, since rolipram showed no additional benefit compared to conventional antidepressants.

The development of multiple sclerosis has been discontinued.

CAS registry number PubChem DrugBank Phosphodiesterase-4 inhibitor Dangerous Substances Directive (67/548/EEC) Active ingredient Archetype (disambiguation) Major depressive disorder Psychosis Neuroprotection Neuropharmacology (journal)
691134
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