Biological Activity
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.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 319.31 |
| Formula | C11H13N3O.C4H4O4 |
| Storage | Store at -20°C |
| Purity | ≥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=CC(O)=O)O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.93 | 100 | |
| water | 31.93 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 319.31. 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 |
|---|---|---|---|
| 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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Product Datasheets
References
References are publications that support the products' biological activity.
McCall et al (2005) Sumanirole, a highly dopamine 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 dopamine 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 Dopamine D2/D3 receptor agonist selectivity. J.Med.Chem. 59 2973 PMID: 27035329
Keywords: Sumanirole maleate, supplier, pfizer, dopamine, dopaminergic, receptors, d2, selective, antiparkinsonian, parkinsons, parkinson's, D2, Receptors, D2, Receptors, Tocris Bioscience
Tocris Bioscience是一家专卖生命科学研究chemicals, peptides and antibodies的知名品牌，其产品也广为各大药厂、大学、研究机构，超过五万名科学研究者所采用。 目前，產品內容已超過一千六百種以上，並每年持續不斷的增加新的產品。目前，产品内容已超过一千六百种以上，并每年持续不断的增加新的产品。
Tocris bioscience是位于英国布里斯托尔（Bristol）的高品质试剂提供商，共有2000多种产品，主要集中在神经科学和信号传导领域，产品类型包括小分子、多肽、抗体、配体和化合物筛选文库等，主要产品包括GPCR ligands，神经传递素，离子通道调控剂，信号通路抑制剂等，这些产品被广泛选择性地用于阻断或激活生物学通路。Tocris是世界上神经科学研究领域无可争议的领导者，其生产的影响神经系统的化学物质被多次引用，这些物质很多都来自Jeff Watkins（Tocris 的创立人）在Bristol大学原创性的研究工作。
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