(+)-UH 232 maleate

Biological Activity

(+)-UH 232 maleate is a D₂ antagonist (K_i = 72.7 nM in a ligand binding assay; apparent K_B = 14.5 nM in a cAMP accumulation assay); displays preferential activity at central dopamine autoreceptors. Stimulates a marked acceleration of dopamine synthesis and turnover. Produces locomotor stimulation. Exhibits little or no activity at central noradrenalin and 5-HT receptors. Also D₃ partial agonist.

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.

Background References

1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
   Fox JT, Sakamuru S, Huang R
   Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
2. The preferential DA D₃ receptor ligand, (+)-UH 232, is a partial agonist.
   Griffon et al.
   Eur.J.Pharmacol., 1995;282:R3
3. Evidence that antipsychotic drugs are inverse agonists at D₂ DA receptors.
   Hall and Strange
   Br. J. Pharmacol., 1997;121:731
4. Novel DA receptor agonists and antagonists with preferential action on autoreceptors.
   Johansson et al.
   J.Med.Chem., 1985;28:1049
5. (+)-AJ 76 and (+)-UH 232: central stimulants acting as preferential DA autoreceptor antagonists.
   Svensson et al.
   Naunyn Schmiedebergs Arch.Pharmacol., 1986;334:234

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