Doxepin (hydrochloride) (Synonyms: Sinequan) |
Catalog No.GC12892
One-Click Copy Product Info
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El clorhidrato de doxepina es un agente antidepresivo tricíclico activo por vía oral.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1229-29-4
Sample solution is provided at 25 µL, 10mM.
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Doxepin, a tricyclic antidepressant, is a potent histamine H1 antagonist [1]. The histamine receptors belong to a family of G protein–coupled receptors activated by their primary endogenous ligand histamine. The H1 receptor has been expressed in smooth muscles, vascular endothelial cells, heart, and the central nervous system [2].
In vitro: Doxepin was a moderately potent competitive inhibitor of serotonin uptake in human blood platelets in vitro, with an inhibitory constant Ki of ～0.2 μM. Doxepin (100 μM) rapidly increased the efflux of serotonin from platelets [1].
In vivo: In rats and dog, oral administration of doxepin was well absorbed and quickly appeared in the blood. Numerous metabolites of doxepin were observed in liver and in urine, only doxepin and demethyl doxepin were found in the rat brain[3]..
Clinical trials: Doxepin has been marketed under many brand names worldwide. The oral topical formulations of doxepin are FDA-approved for the treatment of patients with major depressive disorder, primary insomnia, chronic urticaria, and anxiety [4,5,6].
References:
[1] Lingjrde O. Effect of doxepin on uptake and efflux of serotonin in human blood patelets in vitro[J]. Psychopharmacology, 1976, 47(2): 183-186.
[2] Hill S J, Ganellin C R, Timmerman H, et al. International Union of Pharmacology. XIII. Classification of histamine receptors[J]. Pharmacological reviews, 1997, 49(3): 253-278.
[3] Hobbs D C. Distribution and metabolism of doxepin[J]. Biochemical pharmacology, 1969, 18(8): 1941-1954.
[4] Hajak G, Rodenbeck A, Voderholzer U, et al. Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study[J]. Journal of Clinical Psychiatry, 2001, 62(6): 453-463.
[5] Feighner J P, Cohn J B. Double-blind comparative trials of fluoxetine and doxepin in geriatric patients with major depressive disorder[J]. The Journal of clinical psychiatry, 1985, 46(3 Pt 2): 20-25.
[6] Goldsobel A B, Rohr A S, Siegel S C, et al. Efficacy of doxepin in the treatment of chronic idiopathic urticaria[J]. Journal of allergy and clinical immunology, 1986, 78(5): 867-873.
| Cas No. | 1229-29-4 | SDF | |
| Sinónimos | Sinequan | ||
| Chemical Name | 3-(dibenz[b,e]oxepin-11(6H)-ylidene)-N,N-dimethyl-1-propanamine, monohydrochloride | ||
| Canonical SMILES | CN(C)CC/C=C1C2=C(C=CC=C2)COC3=C/1C=CC=C3.Cl | ||
| Formula | C19H21NO • HCl | M.Wt | 315.8 |
| Solubility | ≥ 15.85mg/mL in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1666 mL | 15.8328 mL | 31.6656 mL |
| 5 mM | 633.3 μL | 3.1666 mL | 6.3331 mL |
| 10 mM | 316.7 μL | 1.5833 mL | 3.1666 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)