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Diphenhydramine

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].

Product Specifications

CAS Number

58-73-1

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Bacterial; Endogenous Metabolite; Histamine Receptor; iGluR

Type

Reference compound

Related Pathways

Anti-infection; GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/diphenhydramine.html

Concentration

10mM

Purity

99.56

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C17H21NO

Molecular Weight

255.36

Precautions

H302, H315, H319, H335

References & Citations

[1]Jason P Berninger, et al. Effects of the antihistamine diphenhydramine on selected aquatic organisms. Environ Toxicol Chem. 2011 Sep;30 (9) :2065-72.|[2]Föhr KJ, et al. Open channel block of NMDA receptors by diphenhydramine. Neuropharmacology. 2015 Dec;99:459-70. |[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. |[4]Hamano H, et al. Diphenhydramine may be a preventive medicine against cisplatin-induced kidney toxicity. Kidney Int. 2021 Apr;99 (4) :885-899.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

H1 Receptor; NMDA Receptor

Citation 01

Acta Pharmacol Sin. 2024 Oct;45 (10) :2061-2076.|Pharm Res. 2025 Oct 27.|bioRxiv. 2025 Sep 10:2025.09.05.673576.|Cell Rep Methods. 2023 Oct 23;3 (10) :100599.|Cell Rep. 2022 Nov 8;41 (6) :111615.|Chemosphere. 2019 Jun:225:378-387.|Pharmacol Res Perspect. 2021 Oct;9 (5) :e00879.

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