| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
Nefazodone targets serotonin 5-HT2A receptors as an antagonist. It also has activity at 5-HT1A and 5-HT2C receptors, as well as weak α1-adrenergic antagonism and norepinephrine and serotonin reuptake inhibition. By blocking 5-HT2 receptors, Nefazodone modulates serotonergic signaling. Its antidepressant effect is mediated through a combination of 5-HT2 receptor antagonism and weak reuptake inhibition. The compound shows no significant cardiac toxicity.
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| ln Vitro |
Nefazodone hydrochloride, also known as BMY-13754, is a phenylpiperazine antidepressant that functions differently from other medications on the market. Nefazodone HydroHClide mildly inhibits serotonin and norepinephrine (norepinephrine) reuptake while potently and selectively blocking postsynaptic serotonin (5-hydroxytryptamine; 5-HT) 5-HT2A receptors. Another hepatic P-450 isoenzyme inhibitor is nevazodone hydrochloride (CYP3A4) [2].
In vitro, Nefazodone acts as a selective 5-HT2 receptor antagonist. It has been characterized in receptor binding and functional assays. The compound shows affinity for 5-HT2A, 5-HT2C, 5-HT1A receptors, and α1-adrenergic receptors. It weakly inhibits serotonin and norepinephrine reuptake. Detailed in vitro data are available in pharmacological literature. Nefazodone is a well-characterized antidepressant used as a reference compound in serotonin receptor research. |
| ln Vivo |
In vivo, Nefazodone is used clinically as an antidepressant for the treatment of major depressive disorder, aggressive behavior, and panic disorder. It shows efficacy in depression and has a favorable side effect profile compared to tricyclic antidepressants, with no significant cardiac toxicity or anticholinergic effects. The compound was marketed under brand names Serzone, Dutonin, and Nefadar.
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| Enzyme Assay |
In vitro receptor binding assays for Nefazodone typically use membrane preparations from cells expressing human serotonin receptors (5-HT2A, 5-HT2C, 5-HT1A) or brain tissue homogenates. Radioligand binding is performed using [³H]-ketanserin (5-HT2A), [³H]-mesulergine (5-HT2C), or [³H]-8-OH-DPAT (5-HT1A) as tracers. Membranes are incubated with radioligand and varying concentrations of Nefazodone in assay buffer at room temperature or 37°C for 60-90 minutes. Nonspecific binding is determined using excess unlabeled ligand. Bound radioactivity is measured by filtration and scintillation counting. Ki values are calculated from competition curves. Functional assays measure serotonin-induced calcium mobilization or cAMP accumulation.
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| Cell Assay |
For cell-based assays, cells expressing serotonin receptors (e.g., CHO or HEK-293 transfectants) are cultured in DMEM with 10% FBS and selection antibiotics. Cells are seeded in 96-well plates and treated with Nefazodone at various concentrations (0.001-10 μM) for 15-30 minutes. Cells are stimulated with serotonin, and downstream signaling (calcium mobilization or cAMP) is measured. IC₅₀ values for antagonist activity are calculated. Cell viability is assessed by standard assays. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, Nefazodone is typically administered orally to patients at doses of 100-600 mg daily. For animal studies, rodents are dosed orally or via other routes. Antidepressant efficacy is assessed in behavioral models such as forced swim test, tail suspension test, and learned helplessness. Blood samples are collected for pharmacokinetic analysis. All procedures follow institutional guidelines.
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| ADME/Pharmacokinetics |
Nefazodone HCl (MW 506.47, C₂₅H₃₂ClN₅O₂·HCl) is a 5-HT2 receptor antagonist. The compound is orally bioavailable. It is metabolized in the liver primarily by CYP3A4. Detailed pharmacokinetic parameters (bioavailability, half-life, clearance) are available from clinical pharmacology literature. The compound has a half-life of approximately 2-4 hours. It is a well-characterized pharmaceutical agent.
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| Toxicity/Toxicokinetics |
Nefazodone is a clinically approved antidepressant with an established safety profile. It was marketed under brand names Serzone, Dutonin, and Nefadar. Common side effects include sedation, dizziness, and dry mouth. Hepatotoxicity has been reported in rare cases, leading to restricted use in some countries. The compound is contraindicated in patients with liver disease. It is available as a pharmaceutical product in some countries.
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| References | |
| Additional Infomation |
Nefazodone hydrochloride is a hydrochloride salt. It contains nefazodone. Nefazodone hydrochloride is a synthetic derivative of phenylpiperazine, and its chemical structure is not related to selective serotonin reuptake inhibitors, tricyclic antidepressants, tetracyclic antidepressants, or monoamine oxidase inhibitors (MAOIs). Nefazodone hydrochloride antagonizes central 5-HT2 receptors, inhibiting the reuptake of serotonin and norepinephrine. (NCI04) See also: Nefazodone (containing the active moiety).
Nefazodone is an antidepressant that acts as a 5-HT2 receptor antagonist with weak serotonin and norepinephrine reuptake inhibition. It was formerly marketed under brand names Serzone, Dutonin, and Nefadar for the treatment of major depressive disorder, aggressive behavior, and panic disorder. Its use has been restricted in some countries due to hepatotoxicity concerns. It is available from chemical suppliers for research purposes. |
| Molecular Formula |
C25H33CL2N5O2
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|---|---|
| Molecular Weight |
506.47
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| Exact Mass |
505.201
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| CAS # |
82752-99-6
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| Related CAS # |
Nefazodone;83366-66-9;Nefazodone-d6 hydrochloride;Nefazodone-d6 dihydrochloride
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| PubChem CID |
54911
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| Appearance |
White to off-white solid powder
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| Boiling Point |
599.6ºC at 760 mmHg
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| Melting Point |
186-188ºC
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| Flash Point |
316.4ºC
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| LogP |
4.356
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
649
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DYCKFEBIOUQECE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H32ClN5O2.ClH/c1-2-24-27-31(25(32)30(24)18-19-33-23-10-4-3-5-11-23)13-7-12-28-14-16-29(17-15-28)22-9-6-8-21(26)20-22;/h3-6,8-11,20H,2,7,12-19H2,1H3;1H
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| Chemical Name |
2-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-5-ethyl-4-(2-phenoxyethyl)-1,2,4-triazol-3-one;hydrochloride
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| Synonyms |
BMY-13754; BMY13754; BMY 13754
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~98.72 mM)
H2O : ~2 mg/mL (~3.95 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9745 mL | 9.8723 mL | 19.7445 mL | |
| 5 mM | 0.3949 mL | 1.9745 mL | 3.9489 mL | |
| 10 mM | 0.1974 mL | 0.9872 mL | 1.9745 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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