Rolipram

Rolipram
Systematic (IUPAC) name
(RS)-4-(3-cyclopentyloxy-4-methoxy-phenyl)pyrrolidin-2-one
Clinical data
Pregnancy cat.  ?
Legal status  ?
Pharmacokinetic data
Half-life 1-3 h
Identifiers
CAS number 61413-54-5 Y
ATC code None
PubChem CID 5092
DrugBank EXPT00228
ChemSpider 4913 Y
UNII K676NL63N7 Y
ChEBI CHEBI:104872 Y
ChEMBL CHEMBL63 Y
Chemical data
Formula C16H21NO3 
Mol. mass 275.347 g/mol
 N(what is this?)  (verify)

Rolipram is a PDE4-inhibitor. Like most PDE4-inhibitors, it is an anti-inflammatory drug.[1] Rolipram is being studied 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 disease,[10] Parkinson's disease [11] and also in the 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 144 (1): 239–46. doi:10.1016/j.neuroscience.2006.09.026. 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. PMC 24568. PMID 9844008. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=24568. 
  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. doi:10.1073/pnas.0908706106. PMC 2743726. PMID 19805389. 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. (June 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: 8786. doi:10.1073/pnas.0402595101. JSTOR 3372336.