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: 147-24-0

Selleck's Diphenhydramine HCl has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.59%
99.59

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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 Not yet recruiting Post-operative Nausea and Vomiting Milton S. Hershey Medical Center January 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 lnformation & 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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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