Sumanirole maleate

Biological Activity

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.

Technical Data

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.

Additional Information

Background References

1. 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.
   Zou et al.
   J.Med.Chem., 2016;59:2973
2. Sumanirole, a highly DA D₂-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease.
   McCall et al.
   J.Pharmacol.Exp.Ther., 2005;314:1248
3. 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.
   Stephenson et al.
   J.Pharmacol.Exp.Ther., 2005;314:1257

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