Biological Activity
Serotonin 5-HT2A receptor antagonist (Ki = 5.8 nM) and inhibitor of serotonin and noradrenalin uptake (IC50 values are 290 and 300 nM respectively). Displays no activity at 5-HT1B and 5-HT1D receptors. Active in models predictive of antidepressant potential.
Technical Data
| M. Wt | 506.47 |
| Formula | C25H32ClN5O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 82752-99-6 |
| PubChem ID | 54911 |
| InChI Key | DYCKFEBIOUQECE-UHFFFAOYSA-N |
| Smiles | Cl.CCC1=NN(CCCN2CCN(CC2)C2=CC(Cl)=CC=C2)C(=O)N1CCOC1=CC=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 | |||
| 1eq. HCl | 5.06 | 10 | |
| DMSO | 12.66 | 25 | |
| ethanol | 5.06 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 506.47. 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 | 1.97 mL | 9.87 mL | 19.74 mL |
| 5 mM | 0.39 mL | 1.97 mL | 3.95 mL |
| 10 mM | 0.2 mL | 0.99 mL | 1.97 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Eison et al (1990) Nefazodone: preclinical pharmacology of a new antidepressant. Psychopharmacol.Bull. 26 311 PMID: 2274630
Davis et al (1997) Nefazodone. A review of its pharmacology and clinical efficacy in the management of major depression. Drugs 53 608 PMID: 9098663
Pullar et al (2000) LY367265, an inhibitor of the 5-hydroxytryptamine transporter and 5-hydroxytryptamine2A receptor antagonist: a comparison with the antidepressant, nefazodone. Eur.J.Pharmacol. 407 39 PMID: 11050288
Keywords: Nefazodone hydrochloride, supplier, 5-HT2A, antagonists, reuptake, inhibitors, inhibits, Antidepressant, Serotonin, Receptors, Transporters, SERT, 5-Hydroxytryptamine, Monoamine, Neurotransmitter, 5-HT2A, Receptors, 5-HT, Transporters, 5-HT2A, Receptors, Tocris Bioscience
