Nefazodone
Based on 4 publication(s) in Google Scholar
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction.
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- Pureté: 98.01%
- CAS No.: 83366-66-9
- Formule: C25H32ClN5O2
- Masse moléculaire:470.01
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) Nefazodone
MoreVoir tous les produits spécifiques à Isoform 5-HT Receptor
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Activité biologique
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5-HT2A Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | IC50 |
4.7 μM
Compound: Nefazodone
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TP_TRANSPORTER: inhibition of Rhodamine 123 transepithelial transport (basal to apical) (R123: 5 uM) in Caco-2 cells
TP_TRANSPORTER: inhibition of Rhodamine 123 transepithelial transport (basal to apical) (R123: 5 uM) in Caco-2 cells
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[PMID: 11452702] |
| Sf21 | IC50 |
17.4 μM
Compound: Nefazodone
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
4.2 μM
Compound: Nefazodone
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
Nefazodone collapses mitochondrial membrane potential, and imposes oxidative stress, as detected via glutathione depletion, leading to cell death[2].
Nefazodone (200 μM; 24 h) depletes 100% of ATP in both, glucose and galactose-grown HepG2 cells[2].
Nefazodone (6.25, 12.5 and 25 μM; 0-120 min) profoundly inhibits oxygen consumption (OCR) in HepG2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (7-12 weeks old; stress model; subjected to a broad band noise at 100 dB daily for 5 s every minute during a 1- or 3-h period around midnight)[3]
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Dosage:10 mg/kg
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Administration:s.c.; for 16 days
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Result:Attenuated the reduction of thymus, spleen and peripheral blood cellularity caused by stress.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 83366-66-9
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Appearance Solid
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Masse moléculaire 470.01
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Formule C25H32ClN5O2
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Color Light yellow to yellow
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SMILES
O=C1N(N=C(N1CCOC2=CC=CC=C2)CC)CCCN3CCN(CC3)C4=CC=CC(Cl)=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Biomater Res
Distinct Roles of Matrigel Enabled the Production of Expandable Hepatoblast and Polarized Hepatocyte Organoids from Human Embryonic Stem Cells under 3-Dimensional Suspension Conditions. [Abstract]2025 Nov 7:29:0280. PMID: 41209312 -
ACS Omega
2025 Oct 17;10(42):50208-50217. PMID: 41179162 -
Biotechnol Bioeng
An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]2021 Dec;118(12):4687-4698. PMID: 34478150 -
Solvant et solubilité
DMSO : 125 mg/mL (265.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Davis R, et al. A review of its pharmacology and clinical efficacy in the management of major depression. Drugs. 1997 Apr;53(4):608-36. [Content Brief]
[2]. Dykens JA, et al. In vitro assessment of mitochondrial dysfunction and cytotoxicity of nefazodone, trazodone, and buspirone. Toxicol Sci. 2008 Jun;103(2):335-45. [Content Brief]
[3]. Freire-Garabal M, et al. Effects of nefazodone on the immune system of mice. Eur Neuropsychopharmacol. 2000 Jul;10(4):255-64. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1276 mL | 10.6381 mL | 21.2761 mL | 53.1904 mL |
| 5 mM | 0.4255 mL | 2.1276 mL | 4.2552 mL | 10.6381 mL | |
| 10 mM | 0.2128 mL | 1.0638 mL | 2.1276 mL | 5.3190 mL | |
| 15 mM | 0.1418 mL | 0.7092 mL | 1.4184 mL | 3.5460 mL | |
| 20 mM | 0.1064 mL | 0.5319 mL | 1.0638 mL | 2.6595 mL | |
| 25 mM | 0.0851 mL | 0.4255 mL | 0.8510 mL | 2.1276 mL | |
| 30 mM | 0.0709 mL | 0.3546 mL | 0.7092 mL | 1.7730 mL | |
| 40 mM | 0.0532 mL | 0.2660 mL | 0.5319 mL | 1.3298 mL | |
| 50 mM | 0.0426 mL | 0.2128 mL | 0.4255 mL | 1.0638 mL | |
| 60 mM | 0.0355 mL | 0.1773 mL | 0.3546 mL | 0.8865 mL | |
| 80 mM | 0.0266 mL | 0.1330 mL | 0.2660 mL | 0.6649 mL | |
| 100 mM | 0.0213 mL | 0.1064 mL | 0.2128 mL | 0.5319 mL |
Nefazodone Related Classifications
HY-119209 Related Classifications
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