Art. -Nr.: HY-B0303

Diphenhydramine

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

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

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Reinheit: 99.85%
CAS. Nr.: 58-73-1
Formel: C₁₇H₂₁NO
Molecular Weight:255.35

Speicherung:

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

Diphenhydramine Chemical Structure

CAS. Nr.: 58-73-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen :

Alle iGluR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	41 μM 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]
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	>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]
MDCK	IC₅₀	24 μM Compound: Diphenhydramine	TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells	[PMID: 11758759]
MDCK	IC₅₀	32 μM Compound: Diphenhydramine	TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells	[PMID: 11758759]
Ventricular myocyte	IC₅₀	228 μM 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]
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]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 58-73-1
Appearance Liquid (Density: 1.024±0.06 g/cm³)
Molecular Weight 255.35
Formel C₁₇H₂₁NO
Color Colorless to light yellow
SMILES

CN(C)CCOC(C1=CC=CC=C1)C2=CC=CC=C2
Structure Classification
- Alkaloids
- Other Alkaloids
Initial Source
- Endogenous metabolite
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (9)

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Journal Impact Factor

Acta Pharmacol Sin

Desloratadine ameliorates paclitaxel-induced peripheral neuropathy and hypersensitivity reactions in mice. [Abstract]

2024 Oct;45(10):2061-2076. PMID: 38789495
Chemosphere

Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]

2019 Jun:225:378-387. PMID: 30884299
Cell Rep

Curative islet and hematopoietic cell transplantation in diabetic mice without toxic bone marrow conditioning. [Abstract]

2022 Nov 8;41(6):111615. PMID: 36351397
Am J Physiol Cell Physiol

Redox-sensitive GPCR signaling drives Gq-dependent Ca²⁺ mobilization and cytokine production in human bronchial epithelial cells. [Abstract]

2026 Jun 18. PMID: 42314770
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Pharm Res

Profiling Interactions Between Bicyclol and SLC/ABC Transporters: Advancing Clinical Safety and Efficacy in Combination Therapy. [Abstract]

2025 Oct 27. PMID: 41145746
Pharmacol Res Perspect

Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats. [Abstract]

2021 Oct;9(5):e00879. PMID: 34628723
Res Sq

2026 Mar 10.
bioRxiv

Curing autoimmune diabetes with islet and hematopoietic cell transplantation after CD117 antibody-based conditioning. [Abstract]

2025 Sep 10:2025.09.05.673576. PMID: 40964321

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	3.9162 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

Keywords

Diphenhydramine

9 Cited Publications

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Diphenhydramine

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Publications Citing Use of MedChemExpress (MCE) Diphenhydramine

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Diphenhydramine Related Classifications

HY-B0303 Related Classifications