Sumanirole maleate

Product Description

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 (K_i 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 (K_i values are 17.1 and 546 nM respectively). Exhibits antiParkinsonian activity.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Stephenson 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. 2005 PMID: 15980058
• Zou 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. 2016 PMID: 27035329
• McCall 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. 2005 PMID: 15980060