Biological Activity
Dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors respectively). May act as an antagonist in vivo, producing anti-Parkinsonian effects and antagonizing the behavioral effects of cocaine. Shown to potentiate agonist binding of the σ1 receptor.
Technical Data
M. Wt | 398.73 |
Formula | C18H20ClNO2.HBr |
Storage | Store at RT |
Purity | ≥98% (HPLC) |
CAS Number | 67287-95-0 |
PubChem ID | 11957685 |
InChI Key | FHYWNBUFNGHNCP-UHFFFAOYSA-N |
Smiles | Br.CN1CCC2=C(C=C(O)C(O)=C2Cl)C(C1)C1=CC(C)=CC=C1 |
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
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 15.89 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 398.73. 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 | 2.51 mL | 12.54 mL | 25.08 mL |
5 mM | 0.5 mL | 2.51 mL | 5.02 mL |
10 mM | 0.25 mL | 1.25 mL | 2.51 mL |
50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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References
References are publications that support the products' biological activity.
Platt et al (2000) Dissociation of cocaine-antagonist properties and motoric effects of the D1 receptor partial agonists SKF 83959 and SKF 77434. J.Pharmacol.Exp.Ther. 293 1017 PMID: 10869406
Cools et al (2002) SKF 83959 is an antagonist of dopamine D1-like receptors in the prefrontal cortex and nucleus accumbens: a key to its antiparkinsonian effect in animals? Neuropharmacology 42 237 PMID: 11804620
Neumeyer et al (2003) Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. Eur.J.Pharmacol. 474 137 PMID: 12921854
Guo et al (2013) SKF83959 is a potent allosteric modulator of sigma-1 receptor. Mol.Pharmacol. 83 577 PMID: 23295385
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