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1 : 1 mixture (racemate)
Systematic (IUPAC) name
(RS)-4-(3-cyclopentyloxy-4-methoxy-phenyl)pyrrolidin-2-one
Identifiers
CAS number 61413-54-5
ATC code none
PubChem 5092
DrugBank EXPT00228
Chemical data
Formula C16H21NO3 
Mol. mass 275.347 g/mol
Pharmacokinetic data
Half life 1-3 h
Therapeutic considerations
Pregnancy cat.  ?
Legal status
 Yes check.svgY(what is this?)  (verify)

Rolipram is a PDE4-inhibitor. Like most PDE4-inhibitors, it is an anti-inflammatory drug.[1] Rolipram is being researched as a possible alternative to current antidepressants.[2][3] Recent studies show that rolipram may have antipsychotic effects.[4][5] Other beneficial effects of rolipram are:

Rolipram shows promise in ameliorating Alzheimer's [10] and Parkinson's [11] disease and also regeneration of severed spinal cord axonal bodies.[12]

See also

References

  1. ^ Griswold DE, Webb EF, Breton J, White JR, Marshall PJ, Torphy TJ. (1993). "Effect of selective phosphodiesterase type IV inhibitor, rolipram, on fluid and cellular phases of inflammatory response.". Inflammation. 17 (3): 333–44. doi:10.1007/BF00918994. PMID 7687237. 
  2. ^ Bobon D, Breulet M, Gerard-Vandenhove MA, Guiot-Goffioul F, Plomteux G, Sastre-y-Hernandez M, Schratzer M, Troisfontaines B, von Frenckell R, Wachtel H. (1988). "Is phosphodiesterase inhibition a new mechanism of antidepressant action? A double blind double-dummy study between rolipram and desipramine in hospitalized major and/or endogenous depressives.". Eur Arch Psychiatry Neurol Sci. 238 (1): 2–6. PMID 3063534. 
  3. ^ Wachtel H. (1983). "Potential antidepressant activity of rolipram and other selective cyclic adenosine 3',5'-monophosphate phosphodiesterase inhibitors.". Neuropharmacology. 22 (3): 267–72. doi:10.1016/0028-3908(83)90239-3. PMID 6302550. 
  4. ^ Maxwell CR, Kanes SJ, Abel T, Siegel SJ. (2004). "Phosphodiesterase inhibitors: a novel mechanism for receptor-independent antipsychotic medications.". Neuroscience. 129 (1): 101–7. doi:10.1016/j.neuroscience.2004.07.038. PMID 15489033. 
  5. ^ Kanes SJ, Tokarczyk J, Siegel SJ, Bilker W, Abel T, Kelly MP. (2006). "Rolipram: A specific phosphodiesterase 4 inhibitor with potential antipsychotic activity.". Neuroscience. ? (?):  ?. PMID 17081698. 
  6. ^ Barad M, Bourtchouladze R, Winder DG, Golan H, Kandel E. (1998). "Rolipram, a type IV-specific phosphodiesterase inhibitor, facilitates the establishment of long-lasting long-term potentiation and improves memory.". Proceedings of the National Academy of Science of the USA. 95 (25): 15020–5. doi:10.1073/pnas.95.25.15020. PMID 9844008. 
  7. ^ Lelkes Z, Alföldi P, Erdos A, Benedek G. (1998). "Rolipram, an antidepressant that increases the availability of cAMP, transiently enhances wakefulness in rats.". Pharmacology, Biochemistry and Behaviour. 60 (4): 835–9. doi:10.1016/S0091-3057(98)00038-0. PMID 9700966. 
  8. ^ Block F, Schmidt W, Nolden-Koch M, Schwarz M. (2001). "Rolipram reduces excitotoxic neuronal damage.". Neuroreport. 12 (7): 1507–11. doi:10.1097/00001756-200105250-00041. PMID 11388438. 
  9. ^ Chen RW, Williams AJ, Liao Z, Yao C, Tortella FC, Dave JR. (2007). "Broad spectrum neuroprotection profile of phosphodiesterase inhibitors as related to modulation of cell-cycle elements and caspase-3 activation.". Neuroscience Letters. 418 (2): 165–9. doi:10.1016/j.neulet.2007.03.033. PMID 17398001. 
  10. ^ Smith, Donna L; Pozueta J, Gong B, Arancio O, Shelanski M (September 14, 2009). "Reversal of long-term dendritic spine alterations in Alzheimer disease models". Proceedings of the National Academy of Sciences of the United States 106 (39): 16877-16882. PMID 15173585 doi:doi: 10.1073/pnas.090870. http://www.pnas.org/content/106/39/16877.full. Retrieved 2009-11-13. 
  11. ^ MF, Beal; Cleren C, Calingasan NY, Yang L, Klivenyi P, Lorenzl S (2005). "Oxidative Damage in Parkinson's Disease". U.S. Army Medical Research and Materiel CommandFort Detrick, Maryland 21702-5012. http://handle.dtic.mil/100.2/ADA434051. Retrieved 2009-11-13. 
  12. ^ Nikulina, E; Tidwell JL, Dai HN, Bregman BS, Filbin MT, Goodman CS (Jun. 8, 2004). "The Phosphodiesterase Inhibitor Rolipram Delivered after a Spinal Cord Lesion Promotes Axonal Regeneration and Functional Recovery". Proceedings of the National Academy of Sciences of the United States 101 (23): 8786-8790. PMID 15173585. http://www.ncbi.nlm.nih.gov/pubmed/15173585. Retrieved 2009-11-13. 
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