Biological Activity
Selective, high affinity antagonist for the rat and human dopamine D4 receptor (Ki = 10 nM). Exhibits low affinity at other monoamine receptors (Ki > 2000 nM). Induces c-fos gene expression in medial prefrontal cortex in a similar manner to clozapine (Cat. No. 0444). Brain penetrant and orally available.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 401.52 |
| Formula | C21H27N3O3S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 170858-33-0 |
| PubChem ID | 133079 |
| InChI Key | WNUQCGWXPNGORO-NRFANRHFSA-N |
| Smiles | O=S(C1=CC=C(N2CCN(CC[C@H]3C(C=CC=C4)=C4CCO3)CC2)C=C1)(N)=O |
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 | 40.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 401.52. 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 | 2.49 mL | 12.45 mL | 24.91 mL |
| 5 mM | 0.5 mL | 2.49 mL | 4.98 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.49 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Merchant et al (1996) Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist. J.Pharm.Exp.Ther. 279 1392 PMID:
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