Doxepin Hydrochloride
Based on 7 publication(s) in Google Scholar
Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant.. Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system.. Doxepin has also been proposed as a protective factor against oxidative stress..
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 1229-29-4
- Formula: C19H22ClNO
- Molecular Weight:315.84
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Doxepin Hydrochloride
More- Nat Commun. 2022 Nov 10;13(1):6796. [Abstract]
- Cell Commun Signal. 2023 May 25;21(1):123. [Abstract]
- Int J Pharm. 2026 Feb 18:126680. [Abstract]
- Pharm Res. 2025 Aug;42(8):1315-1329. [Abstract]
- Antiviral Res. 2025 Dec:244:106307. [Abstract]
- J Appl Toxicol. 2023 Oct;43(10):1421-1435. [Abstract]
- Virus Res. 2022 Aug:317:198816. [Abstract]
All Histamine Receptor Isoforms
More
Biological Activity
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H1 Receptor |
The protective effect of doxepin is associated with the enhancement of PSD-95 and synapsin 1 expression via PI3K/AKT/mTOR signaling pathway[6]..
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y human neuroblastoma cell line
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Concentration:10 ng/ml
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Incubation Time:2 h
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Result:Improved the protein expre-ssion levels of PSD-95, synapsin 1 and p-AKT in SH-SY5Y cells, and decreased the protein expression level of p-mTOR in SH-SY5Y cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD male rats[6].
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Dosage:1, 5mg/kg
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Administration:Doxepin (intraperitoneal injection of 1 mg/kg and 5 mg/kg doxepin once a day for 21 days)
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Result:Improved the protein expression levels of PSD-95 and synapsin 1 in hippocampus and tem-poral lobe, and decreased the protein expression level of p-AKT in hippocampus and temporal lobe after treatment of 1 mg/kg of doxepin.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1229-29-4
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Appearance Solid
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Molecular Weight 315.84
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Formula C19H22ClNO
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Color White to off-white
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SMILES
CN(C)CC/C=C1C2=CC=CC=C2OCC3=CC=CC=C/13.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
Maprotiline restores ER homeostasis and rescues neurodegeneration via Histamine Receptor H1 inhibition in retinal ganglion cells. [Abstract]2022 Nov 10;13(1):6796. PMID: 36357388 -
Cell Commun Signal
Tricyclic antidepressants induce liver inflammation by targeting NLRP3 inflammasome activation. [Abstract]2023 May 25;21(1):123. PMID: 37231437 -
Int J Pharm
2026 Feb 18:126680. PMID: 41720364 -
Pharm Res
Investigation of the Binding Characteristics of Agonists and Various Antagonists Targeting Histamine 1 Receptor. [Abstract]2025 Aug;42(8):1315-1329. PMID: 40760405 -
Antiviral Res
Repurposed doxepin targeting host AXL kinase to disrupt viral 2C-mediated immune evasion in Coxsackievirus B infection. [Abstract]2025 Dec:244:106307. PMID: 41197812 -
J Appl Toxicol
Inhibitory interaction of flavonoids with organic cation transporter 2 and their structure-activity relationships for predicting nephroprotective effects. [Abstract]2023 Oct;43(10):1421-1435. PMID: 37057715 -
Virus Res
2022 Aug:317:198816. PMID: 35598772
Solvent & Solubility
DMSO : ≥ 100 mg/mL (316.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (158.31 mM)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (7.92 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 (7.92 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 140 mg/mL (443.26 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Handling Instructions (2659 KB)
References
[1]. http://pdsp.med.unc.edu/pdsp.php
[2]. Hajak, G., et al., Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study. J Clin Psychiatry, 2001. 62(6): p. 453-63. [Content Brief]
[3]. AnnemiekVermeeren, etal. Effects of the use of hypnotics on cognition. Progress in brain research vol. 190 (2011): 89-103. [Content Brief]
[4]. G Hajak, etal. Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study. The Journal of clinical psychiatry vol. 62,6 (2001): 453-63. [Content Brief]
[5]. Mahsa Gharzi, etal. Effects of different doses of doxepin on passive avoidance learning in rats. Advanced biomedical research vol. 2 66. 30 Jul. 2013. [Content Brief]
[6]. Jimei Bu, etal. Mechanism underlying the effects of doxepin on β-amyloid -induced memory impairment in rats. Iran J Basic Med Sci. 2017 Sep;20(9):1044-1049. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.1662 mL | 15.8308 mL | 31.6616 mL | 79.1540 mL |
| 5 mM | 0.6332 mL | 3.1662 mL | 6.3323 mL | 15.8308 mL | |
| 10 mM | 0.3166 mL | 1.5831 mL | 3.1662 mL | 7.9154 mL | |
| 15 mM | 0.2111 mL | 1.0554 mL | 2.1108 mL | 5.2769 mL | |
| 20 mM | 0.1583 mL | 0.7915 mL | 1.5831 mL | 3.9577 mL | |
| 25 mM | 0.1266 mL | 0.6332 mL | 1.2665 mL | 3.1662 mL | |
| 30 mM | 0.1055 mL | 0.5277 mL | 1.0554 mL | 2.6385 mL | |
| 40 mM | 0.0792 mL | 0.3958 mL | 0.7915 mL | 1.9789 mL | |
| 50 mM | 0.0633 mL | 0.3166 mL | 0.6332 mL | 1.5831 mL | |
| 60 mM | 0.0528 mL | 0.2638 mL | 0.5277 mL | 1.3192 mL | |
| 80 mM | 0.0396 mL | 0.1979 mL | 0.3958 mL | 0.9894 mL | |
| 100 mM | 0.0317 mL | 0.1583 mL | 0.3166 mL | 0.7915 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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