Biological Activity
D2 antagonist (Ki = 72.7 nM in a ligand binding assay; apparent KB = 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
| M. Wt | 391.51 |
| Formula | C18H29NO.C4H4O4 |
| Storage | Store at RT |
| CAS Number | 1217473-50-1 |
| PubChem ID | 46830250 |
| InChI Key | MEQAJDYHKYAPJE-GUUGRXDUSA-N |
| Smiles | OC(=O)C=C/C(O)=O.CCCN(CCC)[C@@H]1CCC2=C(C=CC=C2OC)[C@@H]1C |
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
| Solubility | Soluble to 50 mM in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 391.51. 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 | 2.55 mL | 12.77 mL | 25.54 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.11 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.55 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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Product Datasheets
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References
References are publications that support the products' biological activity.
Griffon et al (1995) The preferential dopamine D3 receptor ligand, (+)-UH 232, is a partial agonist. Eur.J.Pharmacol. 282 R3 PMID: 7498261
Hall and Strange (1997) Evidence that antipsychotic drugs are inverse agonists at D2 dopamine receptors. Br. J. Pharmacol. 121 731 PMID: 9208141
Johansson et al (1985) Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors. J.Med.Chem. 28 1049 PMID: 3927002
Svensson et al (1986) (+)-AJ 76 and (+)-UH 232: central stimulants acting as preferential dopamine autoreceptor antagonists. Naunyn Schmiedebergs Arch.Pharmacol. 334 234 PMID: 2880302
Keywords: (+)-UH 232 maleate, supplier, D2-like, autoreceptor, antagonists, D3, partial, agonists, Dopamine, Non-Selective, Receptors, dopaminergic, (+)-UH232, maleate, Non-selective, Dopamine, D2, Receptors, D2, Receptors, Tocris Bioscience
