Biological Activity
Antipsychotic agent. Displays high affinity for dopamine D4 and serotonergic 5-HT2A receptors and relatively weak affinity at D2 receptors (Ki values are 3.0, 5.8, 134, 181, 199, 240, 411 and > 678 nM for D4, 5-HT2A, 5-HT1A, α1, D2, D3, D1, α2 and muscarinic receptors respectively). Inhibits exploratory locomotor activity and antagonizes d-amphetamine-induced locomotor stimulation in rats.
Technical Data
| M. Wt | 413.36 |
| Formula | C21H25FN2O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 170856-41-4 |
| PubChem ID | 9909647 |
| InChI Key | OGMGYKPECFQXJJ-UHFFFAOYSA-N |
| Smiles | FC(C=C4)=CC=C4N(CC3)CCN3CCC2C1=CC=CC=C1CCO2.Cl.Cl |
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 | |||
| water | 4.13 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 413.36. 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 | 2.42 mL | 12.1 mL | 24.19 mL |
| 5 mM | 0.48 mL | 2.42 mL | 4.84 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.42 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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References
References are publications that support the products' biological activity.
Tang et al (1997) PNU-96415E, a potential antipsychotic agent with clozapine-like pharmacological properties. J.Pharmacol.Exp.Ther. 281 440 PMID: 9103528
Goudie et al (1998) Discriminative stimulus properties of the atypical neuroleptic clozapine in rats: tests with subtype selective receptor ligands. Behav.Pharmacol. 9 699 PMID: 9890260
Keywords: PNU 96415E, supplier, 5-HT2A, D4, antagonists, antipsychotic, Serotonin, Receptors, Dopamine, dopaminergic, PNU96415E, D4, Receptors, 5-HT2A, Receptors, D4, Receptors, Tocris Bioscience
