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
