Rolipram

Rolipram
(IUPAC) ime
(RS)-4-(3-ciklopentiloksi-4-metoksi-fenil)pirolidin-2-on
Klinički podaci
Identifikatori
CAS broj 61413-54-5
ATC kod nije dodeljen
PubChem[1][2] 5092
DrugBank DB04149
ChemSpider[3] 4913
UNII K676NL63N7 DaY
ChEBI CHEBI:104872 DaY
ChEMBL[4] CHEMBL63 DaY
Hemijski podaci
Formula C16H21NO3 
Mol. masa 275,347 g/mol
InChI
InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18) DaY
Key: HJORMJIFDVBMOB-UHFFFAOYSA-N DaY
Farmakokinetički podaci
Poluvreme eliminacije 1–3 h
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Investigational

Rolipram je PDE4-inhibitor. Poput većine PDE4-inhibitora, on je antiinflamatorni lek.[5] Rolipram je studiran kao mogući antidepresiv.[6][7] Nedavne studije su pokazale da rolipram manifestuje antipsihotičke efekte.[8][9] Drugi korisni efekti roliprama identifikovani u eksperimentima na životinjama su:

  • Poboljšana dugotrajna memorija[10]
  • Povećana budnost[11]
  • Povišena neuroprotekcija[12][13]

Ispitivanja su takođe pokazala da rolipram može da bude koristan u tretmanu Alchajmerove bolesti,[14] Parkinsonove bolesti[15] kao i u regeneraciji presečenih aksonskih tela kičmene moždane.[16]

Reference

  1. ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. ↑ 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. 
  6. ↑ 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. 
  7. ↑ 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. 
  8. ↑ 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. 
  9. ↑ 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. 
  10. ↑ 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. 
  11. ↑ 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. 
  12. ↑ 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. 
  13. ↑ 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. 
  14. ↑ Smith, Donna L; Pozueta J, Gong B, Arancio O, Shelanski M (2009-09-14). „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. Pristupljeno 2009-11-13. 
  15. ↑ 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. Arhivirano iz originala na datum 2012-05-23. Pristupljeno 13. 11. 2009. 
  16. ↑ Nikulina, E. (2004-06-08). „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. 

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