Doxylamine Succinate

Alias:
Cat No.:V1228 Purity: ≥98%
Doxylamine succinate (Decapryn; Unisom; Evigoa D), the succinate salt of Doxylamine, is an antihistamine drug that can be used as monotherapy (short-term sedative) or in combination with other drugs to relieve night-time allergy and cold.
Doxylamine Succinate Chemical Structure CAS No.: 562-10-7
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
500mg
1g
2g
5g
Other Sizes

Other Forms of Doxylamine Succinate:

  • Doxylamine
  • Doxylamine D5 succinate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Doxylamine succinate (Decapryn; Unisom; Evigoa D), the succinate salt of Doxylamine, is an antihistamine drug that can be used as monotherapy (short-term sedative) or in combination with other drugs to relieve night-time allergy and cold. It competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects. The effects of doxylamine (as the succinate salt) on microsomal enzyme activity and serum thyroid hormone levels are examined in B6C3F1 mice following dietary exposure for 7 or 15 days (0, 40, 375, 750, or 1500 ppm in diet, expressed as free base doxylamine).

Biological Activity I Assay Protocols (From Reference)
Targets
Histamine H1 receptor
ln Vitro

In vitro activity: The effects of doxylamine (as the succinate salt) on microsomal enzyme activity and serum thyroid hormone levels are examined in B6C3F1 mice following dietary exposure for 7 or 15 days (0, 40, 375, 750, or 1500 ppm in diet, expressed as free base doxylamine). The findings are in line with the theory that doxylamine raises the activity of the hepatic enzymes involved in T4 metabolism and indicate that it is a phenobarbital-type inducer of liver microsomal cytochrome P450 in B6C3F1 mice.

ln Vivo

Animal Protocol


References

[1]. Toxicol Appl Pharmacol . 1996 Dec;141(2):584-94.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H28N2O5
Molecular Weight
388.46
Exact Mass
388.2
Elemental Analysis
C, 64.93; H, 7.27; N, 7.21; O, 20.59
CAS #
562-10-7
Related CAS #
Doxylamine; 469-21-6; Doxylamine-d5 succinate; 1216840-94-6
Appearance
Solid powder
SMILES
CC(C1=CC=CC=C1)(C2=CC=CC=N2)OCCN(C)C.C(CC(=O)O)C(=O)O
InChi Key
KBAUFVUYFNWQFM-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H22N2O.C4H6O4/c1-17(20-14-13-19(2)3,15-9-5-4-6-10-15)16-11-7-8-12-18-16;5-3(6)1-2-4(7)8/h4-12H,13-14H2,1-3H3;1-2H2,(H,5,6)(H,7,8)
Chemical Name
butanedioic acid;N,N-dimethyl-2-(1-phenyl-1-pyridin-2-ylethoxy)ethanamine
Synonyms

Doxylamine Succinate; Decapryn; Unisom; Evigoa D

HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~78 mg/mL (~200.8 mM)
Water: ~78 mg/mL (~200.8 mM)
Ethanol: N/A
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 100 mg/mL (257.43 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5743 mL 12.8713 mL 25.7427 mL
5 mM 0.5149 mL 2.5743 mL 5.1485 mL
10 mM 0.2574 mL 1.2871 mL 2.5743 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00796315 Completed Drug: Doxylamine Succinate USP Allergic Rhinitis
Upper Respiratory Infection
Procter and Gamble December 2008 Phase 1
NCT05498233 Completed Drug: Doxylamine + Pyridoxine Pregnancy Related
Nausea
Valenta Pharm JSC August 18, 2022 Not Applicable
NCT04401384 Completed Drug: Diclectin placebo
Drug: Diclectin
Nausea and Vomiting of
Pregnancy
Xiaoke Wu June 21, 2020 Phase 3
NCT00614445 Completed Drug: Placebo
Drug: doxylamine succinate 10 mg
/pyridoxine hydrochloride 10 mg
Nausea and Vomiting of
Pregnancy
Duchesnay Inc. January 2008 Phase 3
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