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Submit ReviewSumanirole maleate
Description: Selective D2 agonist
Chemical Name: (R)-5,6-Dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (2Z)-2-butenedioate
Purity: ≥98% (HPLC)
Biological Activity 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.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for Sumanirole maleate
Sumanirole maleate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Sumanirole maleate
| 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=C\C(O)=O)O |
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 for Sumanirole maleate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 31.93 | 100 | |
| DMSO | 31.93 | 100 |
Preparing Stock Solutions for Sumanirole maleate
The following data is based on the product molecular weight 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.
| 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 for Sumanirole maleate
References for Sumanirole maleate
References are publications that support the biological activity of the product.
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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Keywords: Sumanirole maleate, Sumanirole maleate supplier, pfizer, dopamine, dopaminergic, receptors, d2, selective, antiparkinsonian, parkinsons, parkinson's, D2, Receptors, 2773, Tocris Bioscience
2 Citations for Sumanirole maleate
Citations are publications that use Tocris products. Selected citations for Sumanirole maleate include:
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.