Diphenhydramine HCl

Alias:

PM 255; Diphenhydramine; Dabylen; PM255; PM-255;Debendrin; Difenhydramine.

Cat No.:V1221 Purity: ≥98%
Diphenhydramine HCl (Dabylen; PM255; PM-255; Debendrin; Difenhydramine), the hydrochloride salt of diphenhydramine, is a 1st-generation histamine H1 receptor antagonist which was approved as an antiemetic for treating various allergic conditions such as rhinitis, urticaria and conjunctivitis.
Diphenhydramine HCl Chemical Structure CAS No.: 147-24-0
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
500mg
1g
2g
5g
10g
25g
Other Sizes

Other Forms of Diphenhydramine HCl:

  • Diphenhydramine
  • Diphenhydramine-d6 hydrochloride (diphenhydramine d6 hydrochloride)
  • Diphenhydramine-d5 hydrochloride (diphenhydramine d5 hydrochloride (hydrochloride))
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Diphenhydramine HCl (Dabylen; PM255; PM-255; Debendrin; Difenhydramine), the hydrochloride salt of diphenhydramine, is a 1st-generation histamine H1 receptor antagonist which was approved as an antiemetic for treating various allergic conditions such as rhinitis, urticaria and conjunctivitis.

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

In vitro activity: Diphenhydramine blocks sodium currents that are sensitive to tetrodotoxin (TTX-S) and resistant to it (TTX-R), with K(d) values of 48 mM and 86 mM, respectively, at a holding potential of -80 mV. Diphenhydramine has little effect on the conductance-voltage curve for TTX-R sodium currents, but it shifts it in the depolarizing direction for TTX-S sodium currents. Diphenhydramine induces a hyperpolarizing shift in the steady-state inactivation curve for both kinds of sodium currents. Diphenhydramine produces a profound use-dependent block when the cells are repeatedly stimulated with high-frequency depolarizing pulses.[1] In CCRF-CEM and Jurkat cell lines, diphenhydramine causes apoptosis in a dose- and time-dependent manner, while at comparable concentrations, imimetidine has no discernible effects. The evaluation of diphenhydramine-induced apoptosis involves morphology analysis, flow cytometry, and cytochrome c release into the cytosol. Diphenhydramine stops human peripheral blood mononuclear cells from proliferating without causing them to undergo apoptosis.[2] The periaqueductal gray neurons' baseline firing is markedly reduced by diphenhydramine (500 nM) without significantly affecting the frequency of postsynaptic potentials. Diphenhydramine blocks the response to neurotensin and tomedial preoptic nucleus stimulation, but at low concentrations it has no effect on baseline firing rate and inhibits periaqueductal gray neurons. [3]

ln Vivo

Cell Assay
Cell Line: PANC-1 cells
Concentration: 0-10 μg/mL
Incubation Time: 24 or 48 h
Result: Increased the expression of Bad and Bax, and decreased Bcl2 level. Decreased the expression of p-AKT (Thr308), p-AKT (Ser 473), p-mTOR (Ser 2448), p-FoxO1 (Ser 256), p-MDM2 (Ser 166), p-NF-ĸB p65 (Ser 536), and p-GSK-3 (Ser 9).
Animal Protocol


References

[1]. Brain Res . 2000 Oct 27;881(2):190-8.

[2]. Oncol Res . 2004;14(7-8):363-72.

[3]. Neuroscience . 2002;114(4):935-43.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H22CLNO
Molecular Weight
291.82
Exact Mass
291.14
Elemental Analysis
C, 69.97; H, 7.60; Cl, 12.15; N, 4.80; O, 5.48
CAS #
147-24-0
Related CAS #
Diphenhydramine; 58-73-1; Diphenhydramine-d6 hydrochloride; 1189986-72-8; Diphenhydramine-d5 hydrochloride; 1219795-16-0; 88637-37-0 (citrate); 7491-10-3 (salicylate)
Appearance
Solid powder
SMILES
CN(C)CCOC(C1=CC=CC=C1)C2=CC=CC=C2.Cl
InChi Key
PCHPORCSPXIHLZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H21NO.ClH/c1-18(2)13-14-19-17(15-9-5-3-6-10-15)16-11-7-4-8-12-16;/h3-12,17H,13-14H2,1-2H3;1H
Chemical Name
2-benzhydryloxy-N,N-dimethylethanamine;hydrochloride
Synonyms

PM 255; Diphenhydramine; Dabylen; PM255; PM-255;Debendrin; Difenhydramine.

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 (e.g. under nitrogen), avoid exposure to moisture and light.
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: 58~100 mg/mL (198.8~342.7 mM)
Water: ~58 mg/mL (~198.8 mM)
Ethanol: ~58 mg/mL (~198.8 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.57 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 (8.57 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 (8.57 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: 130 mg/mL (445.48 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 3.4268 mL 17.1338 mL 34.2677 mL
5 mM 0.6854 mL 3.4268 mL 6.8535 mL
10 mM 0.3427 mL 1.7134 mL 3.4268 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

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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?
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  • 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:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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
NCT04175834 Active
Recruiting
Drug: antihistamine Multiple Sclerosis
Infusion Reaction
Providence Health & Services February 5, 2020 Phase 3
NCT02037126 Active
Recruiting
Drug: Diphenhydramine
Drug: Psilocybin
Cocaine-Related Disorders University of Alabama at
Birmingham
May 2015 Phase 2
NCT04741139 Active
Recruiting
Drug: Acetaminophen and
Diphenhydramine Only Product
Immune Thrombocytopenia Baylor College of Medicine September 2, 2021 Phase 1
NCT04109885 Active
Recruiting
Drug: Paracervical injection
Drug: prochlorperazine
and diphenhydramine.
(Standard Treatment)
Pain Management
Emergency Department
Christian Fromm, MD September 15, 2020 Phase 2
NCT04805073 Recruiting Drug: Promethazine
Drug: Placebo
Pruritus
Pregnancy Related
University of Florida August 9, 2021 Phase 4
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