Biological Activity
A potent D4 dopamine receptor agonist (Ki = 8.7 nM) with > 400-fold selectivity over D2 and > 300-fold selectivity versus D3 subtypes respectively. Induces synaptic translocation of CaMK II to postsynaptic sites in cultured prefrontal cortical neurons. Centrally active in vivo.
Technical Data
| M. Wt | 450.49 |
| Formula | C20H22N4O.C4H4O4 |
| Storage | Desiccate at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 630117-19-0 |
| PubChem ID | 11957665 |
| InChI Key | NAEUGRPISCANHO-BTJKTKAUSA-N |
| Smiles | OC(=O)C=C/C(O)=O.CC1=CC(=CC=C1)C(=O)NCN1CCN(CC1)C1=C(C=CC=C1)C#N |
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 | 45.05 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 450.49. 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 | 2.22 mL | 11.1 mL | 22.2 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.44 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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References
References are publications that support the products' biological activity.
Clifford and Waddington (2000) Topographically based search for an "Ethogram" among a series of novel D4 dopamine receptor agonists and antagonists. Neuropsychopharmacology 22 538 PMID: 10731629
Glase et al (1997) Substituted [(4-phenylpiperazinyl)methyl]benzamides: selective dopamine D4 agonists. J.Med.Chem. 40 1771 PMID: 9191952
Gu et al (2006) Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol.Pharmacol. 69 813 PMID: 16365279
Keywords: PD 168077 maleate, supplier, High, affinity, selective, D4, agonists, Dopamine, Receptors, dopaminergic, PD168077, maleate, D4, Receptors, D4, Receptors, Tocris Bioscience
