Description: 5-HT2A antagonist and 5-HT uptake inhibitor. Antidepressant
Chemical Name: 2-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-3H-1,2,4-triazol-3-one hydrochloride
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Eisonet al (1990) Nefazodone: preclinical pharmacology of a new antidepressant. Psychopharmacol.Bull. 26 311 PMID: 2274630
Daviset al (1997) Nefazodone. A review of its pharmacology and clinical efficacy in the management of major depression. Drugs 53 608 PMID: 9098663
Pullaret 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