Википедија

Rolipram

Rolipram je PDE4-inhibitor. Poput većine PDE4-inhibitora, on je antiinflamatorni lek.[1] Rolipram je studiran kao mogući antidepresiv.[2][3] Nedavne studije su pokazale da rolipram manifestuje antipsihotičke efekte.[4][5] Drugi korisni efekti roliprama identifikovani u eksperimentima na životinjama su:

Rolipram
IUPAC ime
(RS)-4-(3-ciklopentiloksi-4-metoksi-fenil)pirolidin-2-on
Pravni status
Pravni status
  • Investigational
Farmakokinetički podaci
Poluvreme eliminacije1–3 h
Identifikatori
CAS broj61413-54-5 ДаY
ATC kodnone
PubChemCID 5092
DrugBankDB04149 ДаY
ChemSpider4913 ДаY
UNIIK676NL63N7 ДаY
ChEBICHEBI:104872 ДаY
ChEMBLCHEMBL63 ДаY
Hemijski podaci
FormulaC16H21NO3
Molarna masa275,347 g/mol
  • 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) ДаY
  • Key:HJORMJIFDVBMOB-UHFFFAOYSA-N ДаY

Ispitivanja su takođe pokazala da rolipram može da bude koristan u tretmanu Alchajmerove bolesti,[10] Parkinsonove bolesti[11] kao i u regeneraciji presečenih aksonskih tela kičmene moždane.[12]

Vidi još уреди

Reference уреди

  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. PMID 7687237. doi:10.1007/BF00918994. 
  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. PMID 6302550. doi:10.1016/0028-3908(83)90239-3. 
  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. PMID 15489033. doi:10.1016/j.neuroscience.2004.07.038. 
  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. PMID 17081698. doi:10.1016/j.neuroscience.2006.09.026. 
  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. PMC 24568  . PMID 9844008. doi:10.1073/pnas.95.25.15020. 
  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. PMID 9700966. doi:10.1016/S0091-3057(98)00038-0. 
  8. ^ Block F, Schmidt W, Nolden-Koch M, Schwarz M (2001). „Rolipram reduces excitotoxic neuronal damage”. Neuroreport. 12 (7): 1507—11. PMID 11388438. doi:10.1097/00001756-200105250-00041. 
  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. PMID 17398001. doi:10.1016/j.neulet.2007.03.033. 
  10. ^ Smith, Donna L; J, Pozueta; et al. (14. 9. 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. PMC 2743726  . PMID 19805389. doi:10.1073/pnas.0908706106. Приступљено 13. 11. 2009. 
  11. ^ MF, Beal; C, Cleren; et al. (2005). „Oxidative Damage in Parkinson's Disease”. U.S. Army Medical Research and Materiel CommandFort Detrick, Maryland 21702-5012. Архивирано из оригинала 23. 05. 2012. г. Приступљено 13. 11. 2009. 
  12. ^ Nikulina, E. (8. 6. 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. JSTOR 3372336. doi:10.1073/pnas.0402595101. 

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