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Submit ReviewRolipram is a selective inhibitor of cAMP phosphodiesterase (PDE4) (IC50 = 2.0 μM). Discriminates between two conformational states of PDE4 isoenzymes.
R-enantiomer also available.
Rolipram is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 20.65 | 75 | |
ethanol | 20.65 | 75 |
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 |
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.
关键词: Rolipram, Rolipram supplier, PDE4, inhibitors, inhibits, Phosphodiesterases, 0905, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Rolipram 的部分引用包括:
Franchini et al (2019) Linking NMDA Receptor Synaptic Retention to Synaptic Plasticity and Cognition. iScience 19 927 PMID: 31518901
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
Schapitz et al (2010) Neuroligin 1 is dynamically exchanged at postsynaptic sites. Biochim Biophys Acta 30 12733 PMID: 20861378
Adderley et al (2011) Inhibition of ATP release from erythrocytes: a role for EPACs and PKC. Microcirculation 18 128 PMID: 21166931
Russo et al (2018) Leucine-rich repeat kinase 2 controls protein kinase A activation state through phosphodiesterase 4. J Neuroinflammation 15 297 PMID: 30368241
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
Hosoi et al (2002) Identification of a novel human eicosanoid receptor coupled to G(i/o). J Pharmacol Exp Ther 277 31459 PMID: 12065583
Haynes (2000) A(2A) adenosine receptor mediated potassium channel activation in rat epididymal smooth muscle. Br J Pharmacol 130 685 PMID: 10821799
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
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
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
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