Doxepin
Based on 7 publication(s) in Google Scholar
Doxepin is an orally active tricyclic antidepressant capable of crossing the blood-brain barrier. Doxepin enhances the expression of PSD-95 and synapsin-1 via the PI3K/AKT/mTOR signaling pathway and is metabolized in vivo into DesmethylDoxepin (NorDoxepin) (HY-100046). Doxepin binds to the serotonin transporter (SERT) and the norepinephrine transporter (NET), with Kd values of 68 nM and 29.5 nM, respectively. Doxepin can be used in research concerning various conditions, including depression, anxiety, obesity, and atopic dermatitis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.66%
- No. CAS: 1668-19-5
- Fòrmula: C19H21NO
- Peso molecular:279.38
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Doxepin
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]
- Antiviral Res. 2025 Dec:244:106307. [Abstract]
- Pharm Res. 2025 Aug;42(8):1315-1329. [Abstract]
- Virus Res. 2022 Aug:317:198816. [Abstract]
- J Appl Toxicol. 2023 Oct;43(10):1421-1435. [Abstract]
Actividad biológica
Descripciòn
|
Akt |
mTOR |
PSD-95 |
SERT 68 nM (Kd) |
NET 29.5 nM (Kd) |
In Vitro
Doxepin is almost ineffective in inhibiting serotonin (5-HT) uptake in rat platelets[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Doxepin (6.70-11.63 mg/kg; i.p.; single administration; 5 minutes prior to Isoniazid (HY-B0329) challenge) exhibits anticonvulsant activity against Isoniazid-induced seizures in Mus musculus mice, with an ED50 of 8.8 mg/kg and a protective index of 3.0[4].
Doxepin (3.88-8.04 mg/kg; intraperitoneal injection; single administration; 5 minutes prior to 3-mercaptopropionic acid challenge) exhibits anticonvulsant activity against 3-mercaptopropionic acid-induced seizures in mice, with an ED50 of 5.1 mg/kg and a protective index of 5.2[4].
Doxepin (4.65-8.04 mg/kg; i.p.; single administration; 5 min prior to Bicuculline (HY-N0219) challenge) exhibits anticonvulsant activity against Bicuculline-induced seizures in mice, with an ED50 of 5.9 mg/kg and a protective index of 4.5[4].
Doxepin (3.23-5.58 mg/kg; i.p.; single administration; 5 min prior to thiosemicarbazide challenge) exhibits the strongest anticonvulsant activity against thiosemicarbazide-induced seizures in mice, with an ED50 of 4.3 mg/kg and a protective index of 6.1[4].
Doxepin (24.11-72.00 mg/kg; intraperitoneal injection; single administration; 5-120 minutes before rotarod test) induces time-dependent neurotoxicity in mice by impairing motor coordination, with toxicity peaking at 5 minutes after intraperitoneal administration and a TD50 of 26.4 mg/kg[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1668-19-5
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Appearance < 25°C Solid, > 25°C Liquid
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Peso molecular 279.38
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Fòrmula C19H21NO
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Color Off-white to light yellow
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SMILES
CN(C)CC/C=C1C2=CC=CC=C2OCC3=CC=CC=C/13
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 -
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 -
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 -
Virus Res
2022 Aug:317:198816. PMID: 35598772 -
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
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (357.94 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)
In Vivo:
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 (8.95 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 (8.95 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (299 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.5794 mL | 17.8968 mL | 35.7935 mL | 89.4839 mL |
| 5 mM | 0.7159 mL | 3.5794 mL | 7.1587 mL | 17.8968 mL | |
| 10 mM | 0.3579 mL | 1.7897 mL | 3.5794 mL | 8.9484 mL | |
| 15 mM | 0.2386 mL | 1.1931 mL | 2.3862 mL | 5.9656 mL | |
| 20 mM | 0.1790 mL | 0.8948 mL | 1.7897 mL | 4.4742 mL | |
| 25 mM | 0.1432 mL | 0.7159 mL | 1.4317 mL | 3.5794 mL | |
| 30 mM | 0.1193 mL | 0.5966 mL | 1.1931 mL | 2.9828 mL | |
| 40 mM | 0.0895 mL | 0.4474 mL | 0.8948 mL | 2.2371 mL | |
| 50 mM | 0.0716 mL | 0.3579 mL | 0.7159 mL | 1.7897 mL | |
| 60 mM | 0.0597 mL | 0.2983 mL | 0.5966 mL | 1.4914 mL | |
| 80 mM | 0.0447 mL | 0.2237 mL | 0.4474 mL | 1.1185 mL | |
| 100 mM | 0.0358 mL | 0.1790 mL | 0.3579 mL | 0.8948 mL |
Doxepin Related Classifications
HY-B0725A Related Classifications
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Keywords
- Doxepin
- 1668-19-5
- Akt
- mTOR
- Drug Intermediate
- Serotonin Transporter
- PKB
- Protein kinase B
- Mammalian target of Rapamycin
- Drug Iintermediate
- 5-HTT
- SERT
- SLC6A4
- histamine H1 receptors
- guinea pig muscarinic acetylcholine receptor
- rat muscarinic acetylcholine receptor
- norepinephrine
- serotonin
- 5-hydroxytryptamine receptors
- human serotonin transporter
- alpha1-adrenergic receptors
- adenylate cyclase
- monoamine oxidase B
- Inhibitor
- inhibitor
- inhibit