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Submit ReviewRolipram
说明： PDE4 inhibitor
化学名： 4-(3-(Cyclopentyloxy)-4-methoxyphenyl)pyrrolidin-2-one
纯度： ≥98% (HPLC)
生物活性 for Rolipram
Rolipram is a selective inhibitor of cAMP phosphodiesterase (PDE4) (IC50 = 2.0 μM). Discriminates between two conformational states of PDE4 isoenzymes.
R-enantiomer also available.
化合物库 for Rolipram
Rolipram is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Rolipram
| 分子量 | 275.35 |
| 公式 | C16H21NO3 |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 61413-54-5 |
| PubChem ID | 5092 |
| InChI Key | HJORMJIFDVBMOB-UHFFFAOYSA-N |
| Smiles | COC1=CC=C(C=C1OC1CCCC1)C1CNC(=O)C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Rolipram
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 20.65 | 75 | |
| ethanol | 20.65 | 75 |
制备储备液 for Rolipram
以下数据基于产品分子量 275.35。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Rolipram
参考文献 for Rolipram
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Rolipram, please let us know.
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关键词: Rolipram, Rolipram supplier, PDE4, inhibitors, inhibits, Phosphodiesterases, 0905, Tocris Bioscience
20 篇 Rolipram 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Rolipram 的部分引用包括：
Ikezu et al (2018) Tau Phosphorylation is Impacted by Rare AKAP9 Mutations Associated with Alzheimer Disease in African Americans. J Neuroimmune Pharmacol 13 254 PMID: 29516269
Schapitz et al (2010) Neuroligin 1 is dynamically exchanged at postsynaptic sites. Biochim Biophys Acta 30 12733 PMID: 20861378
Russo et al (2018) Leucine-rich repeat kinase 2 controls protein kinase A activation state through phosphodiesterase 4. J Neuroinflammation 15 297 PMID: 30368241
Morales-Garcia et al (2011) Phosphodiesterase 7 inhibition preserves DArgic neurons in cellular and rodent models of Parkinson disease. PLoS One 6 e17240 PMID: 21390306
Adderley et al (2011) Inhibition of ATP release from erythrocytes: a role for EPACs and PKC. Microcirculation 18 128 PMID: 21166931
Orru et al (2013) Psychostimulant pharmacological profile of paraxanthine, the main metabolite of caffeine in humans. Neuropharmacology 67 476 PMID: 23261866
Lundegaard et al (2015) MEK Inhibitors Reverse cAMP-Mediated Anxiety in Zebrafish. Chem Biol 22 1335 PMID: 26388333
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
Franchini et al (2019) Linking NMDA Receptor Synaptic Retention to Synaptic Plasticity and Cognition. iScience 19 927 PMID: 31518901
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 isoprote. 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
Haynes (2000) A(2A) adenosine receptor mediated potassium channel activation in rat epididymal smooth muscle. Br J Pharmacol 130 685 PMID: 10821799
Hosoi et al (2002) Identification of a novel human eicosanoid receptor coupled to G(i/o). J Pharmacol Exp Ther 277 31459 PMID: 12065583
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