Trazodone
Based on 6 publication(s) in Google Scholar
Trazodone (AF-1161 free base) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone has anti-depressant and anti-insomnious activity. Trazodone exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects.
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- Pureza: 99.84%
- No. CAS: 19794-93-5
- Fòrmula: C19H22ClN5O
- Peso molecular:371.86
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Trazodone
MoreVer todos los productos específicos de isoformas 5-HT Receptor
MoreVer todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
Trazodone binds to 5-HT1A receptor with a Ki of 23.6 nM[3].
Trazodone (1 nM–10 μM, 24 h or 72 h) reduces the expression of neuroinflammatory markers by inhibiting key signaling pathways such as NF-κB, p38 MAPK, and JNK, exhibiting neuroprotective effects[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neuronal-like cells differentiated from H9-derived NSCs
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Concentration:1 nM–10 μM
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Incubation Time:24 h or 72 h
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Result:Increased mRNA expression of BDNF and CREB, reduced IFN-γ release.
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Cell Line:Neuronal-like cells differentiated from H9-derived NSCs
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Concentration:1 nM–10 μM
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Incubation Time:24 h or 72 h
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Result:Showed increased levels of phosphorylated ERK1/2 and decreased phosphorylated p38 levels.
Trazodone (100 mg/kg, i.p., single dose) reduces hyperactivity, prostration and clonic convulsions in cats and dogs[2].
Trazodone (12.5-25 mg/kg, i.p., single dose) inhibits nicotine- and Oxotremorine (HY-170032)-induced tremor[2].
Trazodone (5-20 mg/kg/day, s.c., 2-14 d) significantly decreases the spontaneous firing rate of DR 5-HT neurons by 40% and 37% with 10 and 20 mg/kg dose in SD rats[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (250-350 g)[4]
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Dosage:5, 10, 20 mg/kg/day
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Administration:Subcutaneous injection (s.c.), 2 or 14 d
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Result:Induced a marked physiological action on 5-HT neurons.
Significantly decreased the spontaneous firing rate of DR 5-HT neurons by 40% and 37% with 10 and 20 mg/kg dose, respectively.
Blocked 5-HT reuptake process.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 19794-93-5
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Appearance Solid
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Peso molecular 371.86
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Fòrmula C19H22ClN5O
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Color White to off-white
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SMILES
O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)N=C4C=CC=CN41
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Synonyms
AF-1161 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (6)
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Journal Impact Factor
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Most Recent
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Clin Chem
Discovering Cross-Reactivity in Urine Drug Screening Immunoassays through Large-Scale Analysis of Electronic Health Records. [Abstract]2019 Dec;65(12):1522-1531. PMID: 31578215 -
Int Immunopharmacol
Innovative role of the antidepressant imipramine in esophageal squamous cell carcinoma treatment: Promoting apoptosis and protective autophagy. [Abstract]2025 Jan 6:147:113969. PMID: 39764996 -
ACS Omega
2025 Oct 17;10(42):50208-50217. PMID: 41179162 -
Anal Bioanal Chem
Dispersive solid-phase extraction as sample pretreatment for determination of chemotherapeutic agents revumenib and venetoclax by HPLC-DAD. [Abstract]2025 Jul;417(16):3703-3714. PMID: 40323377 -
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Solvente y solubilidad
DMSO : 5 mg/mL (13.45 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Fagiolini A, et, al. Rediscovering trazodone for the treatment of major depressive disorder. CNS Drugs. 2012 Dec;26(12):1033-49. [Content Brief]
[2]. Brogden, R. N., et al., (1981). Trazodone: a review of its pharmacological properties and therapeutic use in depression and anxiety. Drugs, 21(6), 401–429. [Content Brief]
[3]. Raffa, R. B., et al., (1992). Etoperidone, trazodone and MCPP: in vitro and in vivo identification of serotonin 5-HT1A (antagonistic) activity. Psychopharmacology, 108(3), 320–326. [Content Brief]
[4]. Ghanbari, R., et al., (2010). Sustained administration of trazodone enhances serotonergic neurotransmission: in vivo electrophysiological study in the rat brain. The Journal of pharmacology and experimental therapeutics, 335(1), 197–206. [Content Brief]
[5]. Jay AR, Krotscheck U, Parsley E, Benson L, Kravitz A, Mulligan A, Silva J, Mohammed H, Schwark WS. Pharmacokinetics, bioavailability, and hemodynamic effects of trazodone after intravenous and oral administration of a single dose to dogs. Am J Vet Res. 2013 Nov;74(11):1450-6. [Content Brief]
[6]. Daniele S, et al. Trazodone treatment protects neuronal-like cells from inflammatory insult by inhibiting NF-κB, p38 and JNK. Cell Signal. 2015 Aug;27(8):1609-29. [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 (protect from light). 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 | 2.6892 mL | 13.4459 mL | 26.8918 mL | 67.2296 mL |
| 5 mM | 0.5378 mL | 2.6892 mL | 5.3784 mL | 13.4459 mL | |
| 10 mM | 0.2689 mL | 1.3446 mL | 2.6892 mL | 6.7230 mL |
Trazodone Related Classifications
HY-B0478A Related Classifications
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