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.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
If you know of a relevant reference for Sumanirole maleate, please let us know.
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Keywords: Sumanirole maleate, supplier, pfizer, dopamine, dopaminergic, receptors, d2, selective, antiparkinsonian, parkinsons, parkinson's, D2, Receptors, D2, Receptors, Tocris Bioscience
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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* or download 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.
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.
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 (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.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.