Home Neuronal Signaling Histamine Receptor antagonist Diphenhydramine HCl For research use only.

Diphenhydramine HCl

Diphenhydramine HCl is a first-generation histamine H1 receptor antagonist, used in various allergic conditions such as rhinitis, urticaria and conjunctivitis.

Diphenhydramine HCl Chemical Structure

Diphenhydramine HCl Chemical Structure

CAS No. 147-24-0

Purity & Quality Control

Diphenhydramine HCl Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

Biological Activity

Description Diphenhydramine HCl is a first-generation histamine H1 receptor antagonist, used in various allergic conditions such as rhinitis, urticaria and conjunctivitis.
Targets
Histamine H1 receptor [1]
In vitro
In vitro Diphenhydramine blocks tetrodotoxin-sensitive (TTX-S) and tetrodotoxin-resistant (TTX-R) sodium currents with K(d) values of 48 mM and 86 mM, respectively, at a holding potential of -80 mV. Diphenhydramine shifts the conductance-voltage curve for TTX-S sodium currents in the depolarizing direction but has little effect on that for TTX-R sodium currents. Diphenhydramine causes a shift of the steady-state inactivation curve for both types of sodium currents in the hyperpolarizing direction. Diphenhydramine produces a profound use-dependent block when the cells are repeatedly stimulated with high-frequency depolarizing pulses. [1] Diphenhydramine induces apoptosis in a dose- and time-dependent manner in both CCRF-CEM and Jurkat cell lines, whereas Cimetidine fails to induce significant effects at similar concentrations. Diphenhydramine-induced apoptosis is evaluated in terms of morphology, flow cytometry, and the release of cytochrome c to the cytosol. Diphenhydramine inhibits cell proliferation without inducing apoptosis in human peripheral blood mononuclear cells. [2] Diphenhydramine (500 nM) significantly reduces the baseline firing of the periaqueductal gray neurons without a significant effect on the frequency of postsynaptic potentials. Diphenhydramine at high concentration inhibits periaqueductal gray neurons, but at low concentrations it has no effect on the baseline-firing rate and it blocks the response to neurotensin and tomedial preoptic nucleus stimulation. [3]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05759481 Recruiting
Post-operative Nausea and Vomiting
Milton S. Hershey Medical Center
 February 1 2024 Phase 2
NCT05674721 Completed
Pain
HALEON
 January 5 2023 Phase 1
NCT05219604 Terminated
Central Nervous System Effects of Diphenhydramine|Pharmacokinetics of Diphenhydramine
Dent Neuroscience Research Center
 March 15 2022 Phase 4
NCT05244460 Recruiting
Cannabis Hyperemesis Syndrome
Mercy Health Ohio|Lake Erie College of Osteopathic Medicine
 December 2 2021 Phase 3

Chemical Information & Solubility

Molecular Weight 291.82 Formula

C17H21NO.HCl
CAS No. 147-24-0 SDF Download Diphenhydramine HCl SDF
Smiles CN(C)CCOC(C1=CC=CC=C1)C2=CC=CC=C2.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 58 mg/mL ( (198.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 58 mg/mL

Ethanol : 58 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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