Rolipram

drugbox
IUPAC_name = 4-(3-cyclopentyloxy-4-methoxy-phenyl)pyrrolidin-2-one

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width = 180
CAS_number = 61413-54-5
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PubChem = 5092
DrugBank = EXPT00228
C = 16 | H = 21 | N = 1 | O = 3
molecular_weight = 275.347 g/mol
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elimination_half-life = 1-3 h
excretion =
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Rolipram is a PDE4-inhibitor. Like most PDE4-inhibitors, it is an anti-inflammatory drug.cite journal | author=Griswold DE, Webb EF, Breton J, White JR, Marshall PJ, Torphy TJ. | title=Effect of selective phosphodiesterase type IV inhibitor, rolipram, on fluid and cellular phases of inflammatory response. | journal=Inflammation. | year=1993 | pages=333–44 | volume=17 | issue=3 | pmid=7687237 | doi=10.1007/BF00918994] Rolipram is being researched as a possible alternative to current antidepressants.cite journal | author=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. | title=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. | journal=Eur Arch Psychiatry Neurol Sci. | year=1988 | pages=2–6 | volume=238 | issue=1 | pmid=3063534] cite journal | author=Wachtel H. | title=Potential antidepressant activity of rolipram and other selective cyclic adenosine 3',5'-monophosphate phosphodiesterase inhibitors. | journal=Neuropharmacology. | year=1983 | pages=267–72 | volume=22 | issue=3 | pmid=6302550 | doi=10.1016/0028-3908(83)90239-3] Recent studies show that rolipram may have antipsychotic effects.cite journal | author=Maxwell CR, Kanes SJ, Abel T, Siegel SJ. | title=Phosphodiesterase inhibitors: a novel mechanism for receptor-independent antipsychotic medications. | journal=Neuroscience. | year=2004 | pages=101–7 | volume=129 | issue=1 | pmid=15489033 | doi=10.1016/j.neuroscience.2004.07.038] cite journal | author=Kanes SJ, Tokarczyk J, Siegel SJ, Bilker W, Abel T, Kelly MP. | title=Rolipram: A specific phosphodiesterase 4 inhibitor with potential antipsychotic activity. | journal=Neuroscience. | year=2006 | pages=? | volume=? | issue=? | pmid=17081698] Other beneficial effects of rolipram are:
* Improved long term memory. cite journal | author=Barad M, Bourtchouladze R, Winder DG, Golan H, Kandel E. | title=Rolipram, a type IV-specific phosphodiesterase inhibitor, facilitates the establishment of long-lasting long-term potentiation and improves memory. | journal=Proceedings of the National Academy of Science of the USA. | year=1998 | pages=15020–5 | volume=95 | issue=25 | pmid=9844008 | doi=10.1073/pnas.95.25.15020]
* Increased wakefulness. cite journal | author=Lelkes Z, Alföldi P, Erdos A, Benedek G. | title=Rolipram, an antidepressant that increases the availability of cAMP, transiently enhances wakefulness in rats. | journal=Pharmacology, Biochemistry and Behaviour. | year=1998 | pages=835–9 | volume=60 | issue=4 | pmid=9700966 | doi=10.1016/S0091-3057(98)00038-0]
* Increased neuroprotection. cite journal | author=Block F, Schmidt W, Nolden-Koch M, Schwarz M. | title=Rolipram reduces excitotoxic neuronal damage. | journal=Neuroreport. | year=2001 | pages=1507–11 | volume=12 | issue=7 | pmid=11388438 | doi=10.1097/00001756-200105250-00041] cite journal | author=Chen RW, Williams AJ, Liao Z, Yao C, Tortella FC, Dave JR. | title=Broad spectrum neuroprotection profile of phosphodiesterase inhibitors as related to modulation of cell-cycle elements and caspase-3 activation. | journal=Neuroscience Letters. | year=2007 | pages=165–9 | volume=418 | issue=2 | pmid=17398001 | doi=10.1016/j.neulet.2007.03.033]

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