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Submit ReviewSumanirole maleate
说明： Selective D2 agonist
化学名： (R)-5,6-Dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (2Z)-2-butenedioate
纯度： ≥98% (HPLC)
生物活性 for Sumanirole maleate
Sumanirole maleate is a high affinity D2 receptor agonist (EC50 values are between 17 and 75 nM in cell-based assays). Originally reported to exhibit >200-fold selectivity for the D2 receptor versus other dopamine receptor subtypes (Ki values are 9.0, 1940, >2190 and >7140 for D2, D3, D4 and D1 receptors respectively). More recently reported to be around 32-fold selective for D2 over D3 receptors (Ki values are 17.1 and 546 nM respectively). Exhibits antiParkinsonian activity.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
化合物库 for Sumanirole maleate
Sumanirole maleate 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 Sumanirole maleate
| 分子量 | 319.31 |
| 公式 | C11H13N3O.C4H4O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 179386-44-8 |
| PubChem ID | 9818478 |
| InChI Key | VOJRMYBBPKNLLI-ORHWHDKWSA-N |
| Smiles | O=C3N2C1=C(N3)C=CC=C1C[C@@H](NC)C2.O=C(/C=C\C(O)=O)O |
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 Sumanirole maleate
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 31.93 | 100 | |
| DMSO | 31.93 | 100 |
制备储备液 for Sumanirole maleate
以下数据基于产品分子量 319.31。 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 |
|---|---|---|---|
| 1 mM | 3.13 mL | 15.66 mL | 31.32 mL |
| 5 mM | 0.63 mL | 3.13 mL | 6.26 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.13 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.63 mL |
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产品说明书 for Sumanirole maleate
参考文献 for Sumanirole maleate
参考文献是支持产品生物活性的出版物。
McCall et al (2005) Sumanirole, a highly DA D2-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease. J.Pharmacol.Exp.Ther. 314 1248 PMID: 15980060
Stephenson et al (2005) The effects of a selective DA D2 receptor agonist on behavioral and pathological outcome in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated squirrel monkeys. J.Pharmacol.Exp.Ther. 314 1257 PMID: 15980058
Zou et al (2016) Novel analogues of (R)-5-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) provide clues to DA D2/D3 receptor agonist selectivity. J.Med.Chem. 59 2973 PMID: 27035329
If you know of a relevant reference for Sumanirole maleate, please let us know.
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关键词: Sumanirole maleate, Sumanirole maleate supplier, pfizer, dopamine, dopaminergic, receptors, d2, selective, antiparkinsonian, parkinsons, parkinson's, D2, Receptors, 2773, Tocris Bioscience
2 篇 Sumanirole maleate 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Sumanirole maleate 的部分引用包括：
Chai et al (2017) Neural Circuit-Specialized Astrocytes: Transcriptomic, Proteomic, Morphological, and Functional Evidence. Neuron 95 531 PMID: 28712653
Saika (2018) Chemokine CXCL1 is responsible for cocaine-induced reward in mice. NeurosciPharm Reports 38 145 PMID: 30175527
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
Addiction Poster
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.