Diphenhydramine

Name: Diphenhydramine
Brand: MedChemExpress
SKU: HY-B0303
Rating: 5.0 (5 reviews)

Cat. No.: HY-B0303 Purity: 99.08%: FAQs
Data Sheet SDS COA Handling Instructions

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Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .

For research use only. We do not sell to patients.

Diphenhydramine Chemical Structure

CAS No. : 58-73-1

Size	Price	Stock	Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Liquid
250 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Diphenhydramine:

Diphenhydramine hydrochloride In-stock
Diphenhydramine hydrochloride (Standard) Get quote
Diphenhydramine (Standard) Get quote

5 Publications Citing Use of MCE Diphenhydramine

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AMPA Receptor NMDA Receptor Kainate Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) ^[1]^[2]^[3].

IC₅₀ & Target

H₁ Receptor

NMDA Receptor

24.6 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 500 μM Compound: Table 1, R42C1	Inhibition of ORAl1/2/3 in HEK293 cells assessed as inhibition of Cd2+ influx after 10 mins by FLIPR assay in presence of thapsigargin Inhibition of ORAl1/2/3 in HEK293 cells assessed as inhibition of Cd2+ influx after 10 mins by FLIPR assay in presence of thapsigargin	[PMID: 23602525]
HEK293	IC₅₀	> 500 μM Compound: Table 1, R42C1	Inhibition of ORAl1/2/3 in HEK293 cells assessed as inhibition of Ca2+ influx after 10 mins by FLIPR assay in presence of thapsigargin Inhibition of ORAl1/2/3 in HEK293 cells assessed as inhibition of Ca2+ influx after 10 mins by FLIPR assay in presence of thapsigargin	[PMID: 23602525]
HEK293	IC₅₀	41000 nM Compound: Diphenhydramine	Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA	[PMID: 21300721]
Ventricular myocyte	IC₅₀	228 μM Compound: Diphenhydramine	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Ventricular myocyte	IC₅₀	228000 nM Compound: Diphenhydramine	Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes	[PMID: 21300721]

In Vitro

Diphenhydramine (1-300 μM, 30 s) can block NMDA-activated membrane currents. This property can be responsible for or add to its sedative, analgesic and memory related effects^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	Human TsA cells
Concentration:	1-300 μM
Incubation Time:	10-30 s
Result:	Did not discriminate between different GluN2 receptor subunits. The IC₅₀ value of Diphenhydramine against GluN1/GluN2B was 24.6 µM. The IC₅₀ values of Diphenhydramine against GluN1/GluN2A and GluN1_A652C/GluN2A were 24.4 µM and 89.6 µM, respectively, indicating that the receptor modification reduces sensitivity for diphenhydramine. The inhibitory potency of Diphenhydramine did not be overcome with increasing NMDA concentrations. The inhibitory potency of Diphenhydramine did not increase with increasing agonist concentration.

In Vivo

Diphenhydramine (0-10 mg/kg, i.v. and p.o.) has better oral bioavailability when used in combination with Dimenhydrinate (HY-B1215)sup>[3].
Diphenhydramine (20 mg/kg, i.p.) can improve the kidney injury induced by Cisplatin (CDDP) (HY-17394) in mice, and does not affect the anti-tumor efficacy of Cisplatin^[4].

Pharmacokinetic parameters for diphenhydramine after single oral or intravenous administration of diphenhydramine HCl (5 mg/kg) to six healthy dogs by using a noncompartmental model with first-order elimination^[3]

Route	Dose (mg/kg)	AUC_last (ng·h/mL)	C₀ (ng/Ml)	CL (Ml/h/kg)	T_1/2 (h)	K_el (1/h)	MRT (h)	V_{ss_obs} (mL/kg)	C_max (ng/mL)	T_max (h)	V_z (mL/kg)	F (%)
i.v.	5	391.20	266.10	2833.04	1.89	0.45	2.47	6582.36	/	/	/	/
p.o.	5	153.80	/	/	4.98	0.59	6.97	/	35.80	1.30	180157.36	7.75

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	healthy, fasted mixed-breed dogs^[3]
Dosage:	1/5/10 mg/kg
Administration:	i.v., p.o.
Result:	Oral absorption of diphenhydramine was approximately three times greater with a longer half-life when it was administered as the combination product Dimenhydrinate (HY-B1215).

Clinical Trial

Molecular Weight

255.35

Formula

C₁₇H₂₁NO

CAS No.

58-73-1

Appearance

Liquid (Density: 1.024±0.06 g/cm³)

Color

Colorless to light yellow

SMILES

CN(C)CCOC(C1=CC=CC=C1)C2=CC=CC=C2

Structure Classification

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (391.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.9162 mL	19.5810 mL	39.1619 mL
5 mM	0.7832 mL	3.9162 mL	7.8324 mL
10 mM	0.3916 mL	1.9581 mL	3.9162 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.79 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.08%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (248 KB) HNMR (227 KB) LCMS (84 KB)

Handling Instructions (2659 KB)

References

[1]. Jason P Berninger, et al. Effects of the antihistamine diphenhydramine on selected aquatic organisms. Environ Toxicol Chem. 2011 Sep;30(9):2065-72. [Content Brief]

[2]. Föhr KJ, et al. Open channel block of NMDA receptors by diphenhydramine. Neuropharmacology. 2015 Dec;99:459-70. [Content Brief]

[3]. Ehling S, et al. Diphenhydramine pharmacokinetics after oral and intravenous administration of diphenhydramine and oral administration of dimenhydrinate to healthy dogs, and pharmacodynamic effect on histamine-induced wheal formation: a pilot study. Vet Dermatol. 2019 Apr;30(2):91-e24. [Content Brief]

[4]. Hamano H, et al. Diphenhydramine may be a preventive medicine against cisplatin-induced kidney toxicity. Kidney Int. 2021 Apr;99(4):885-899. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.9162 mL	19.5810 mL	39.1619 mL	97.9048 mL
	5 mM	0.7832 mL	3.9162 mL	7.8324 mL	19.5810 mL
	10 mM	0.3916 mL	1.9581 mL	3.9162 mL	9.7905 mL
	15 mM	0.2611 mL	1.3054 mL	2.6108 mL	6.5270 mL
	20 mM	0.1958 mL	0.9790 mL	1.9581 mL	4.8952 mL
	25 mM	0.1566 mL	0.7832 mL	1.5665 mL	3.9162 mL
	30 mM	0.1305 mL	0.6527 mL	1.3054 mL	3.2635 mL
	40 mM	0.0979 mL	0.4895 mL	0.9790 mL	2.4476 mL
	50 mM	0.0783 mL	0.3916 mL	0.7832 mL	1.9581 mL
	60 mM	0.0653 mL	0.3263 mL	0.6527 mL	1.6317 mL
	80 mM	0.0490 mL	0.2448 mL	0.4895 mL	1.2238 mL
	100 mM	0.0392 mL	0.1958 mL	0.3916 mL	0.9790 mL