Rolipram

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Cat.No. 0905 - Rolipram | C16H21NO3 | CAS No. 61413-54-5
Description: PDE4 inhibitor
Chemical Name: 4-(3-(Cyclopentyloxy)-4-methoxyphenyl)pyrrolidin-2-one
Purity: ≥98% (HPLC)
Datasheet
Citations (17)
Reviews
Literature

Biological Activity

Selective inhibitor of cAMP phosphodiesterase (PDE4) (IC50 = 2.0 μM). Discriminates between two conformational states of PDE4 isoenzymes.

R-enantiomer and S-enantiomer also available.

Compound Libraries

Rolipram is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 275.35
Formula C16H21NO3
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 61413-54-5
PubChem ID 5092
InChI Key HJORMJIFDVBMOB-UHFFFAOYSA-N
Smiles COC1=CC=C(C=C1OC1CCCC1)C1CNC(=O)C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.65 75
ethanol 20.65 75

Preparing Stock Solutions

The following data is based on the product molecular weight 275.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.75 mM 4.84 mL 24.21 mL 48.42 mL
3.75 mM 0.97 mL 4.84 mL 9.68 mL
7.5 mM 0.48 mL 2.42 mL 4.84 mL
37.5 mM 0.1 mL 0.48 mL 0.97 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Kato et al (1995) Rolipram, a cyclic AMP-selective phosphodiesterase inhibitor, reduces neuronal damage following cerebral ischemia in the gerbil. Eur.J.Pharmacol. 272 107 PMID: 7713141

O'Donnell (1993) Antidepressant-like effects of rolipram and other inhibitors of cyclic adenosine monophosphate phosphodiesterase on behaviour maintained by differential reinforcement of low response rate. J.Pharmacol.Exp.Ther. 264 1168 PMID: 8383740

Teixeira et al (1997) Phosphodiesterase (PDE)4 inhibitors: anti-inflammatory drugs of the future? Trends Pharmacol.Sci. 18 164 PMID: 9184477


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Keywords: Rolipram, Rolipram supplier, PDE4, inhibitors, inhibits, Phosphodiesterases, 0905, Tocris Bioscience

17 Citations for Rolipram

Citations are publications that use Tocris products. Selected citations for Rolipram include:

Adderley et al (2011) Inhibition of ATP release from erythrocytes: a role for EPACs and PKC. Microcirculation 18 128 PMID: 21166931

Morales-Garcia et al (2011) Phosphodiesterase 7 inhibition preserves dopaminergic neurons in cellular and rodent models of Parkinson disease. PLoS One 6 e17240 PMID: 21390306

Schapitz et al (2010) Neuroligin 1 is dynamically exchanged at postsynaptic sites. Biochim Biophys Acta 30 12733 PMID: 20861378

Parnell et al (2015) Phosphorylation of ezrin on Thr567 is required for the synergistic activation of cell spreading by EPAC1 and protein kinase A in HEK293T cells. Eneuro 1853 1749 PMID: 25913012

Polito et al (2015) Selective Effects of PDE10A Inhibitors on Striatopallidal Neurons Require Phosphatase Inhibition by DARPP-32(1,2,3). J Neurosci 2 PMID: 26465004

Zhu et al (2015) Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways. J Neurosci 35 621 PMID: 25589756

Choi et al (2015) PDE-4 inhibition rescues aberrant synaptic plasticity in Drosophila and mouse models of fragile X syndrome. Pharmacol Res Perspect 35 396 PMID: 25568131

Pecha et al (2015) β 1 Adrenoceptor antagonistic effects of the supposedly selective β 2 adrenoceptor antagonist ICI 118,551 on the positive inotropic effect of adrenaline in murine hearts. PLoS One 3 e00168 PMID: 26516580

Merino et al (2015) Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with Isoproterenol. PLoS One 10 e0132884 PMID: 26222156

Ørstavik et al (2015) The inotropic effect of the active metabolite of levosimendan, OR-1896, is mediated through inhibition of PDE3 in rat ventricular myocardium. J Biol Chem 10 e0115547 PMID: 25738589

Townsend and Emala (2013) Quercetin acutely relaxes airway smooth muscle and potentiates β-agonist-induced relaxation via dual phosphodiesterase inhibition of PLCβ and PDE4. Am J Physiol Lung Cell Mol Physiol 305 L396 PMID: 23873842

Adderley et al (2012) Phosphodiesterases Regulate BAY 41-2272-Induced VASP Phosphorylation in Vascular Smooth Muscle Cells. Front Pharmacol 3 10 PMID: 22347188

Zhong et al (2012) Phosphodiesterase 4 inhibition impairs cocaine-induced inhibitory synaptic plasticity and conditioned place preference. Neuropsychopharmacology 37 2377 PMID: 22713909

Hosoi et al (2002) Identification of a novel human eicosanoid receptor coupled to G(i/o). J Pharmacol Exp Ther 277 31459 PMID: 12065583

Lundegaard et al (2015) MEK Inhibitors Reverse cAMP-Mediated Anxiety in Zebrafish. Chem Biol 22 1335 PMID: 26388333

Orru et al (2013) Psychostimulant pharmacological profile of paraxanthine, the main metabolite of caffeine in humans. Neuropharmacology 67 476 PMID: 23261866

Haynes (2000) A(2A) adenosine receptor mediated potassium channel activation in rat epididymal smooth muscle. Br J Pharmacol 130 685 PMID: 10821799


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