Diphenhydramine HCl

For research use only.

Catalog No.S1866

3 publications

Diphenhydramine HCl  Chemical Structure

Molecular Weight(MW): 291.82

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

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10mM (1mL in DMSO) USD 130 In stock
USD 97 In stock
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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

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]

Protocol

Solubility (25°C)

In vitro DMSO 58 mg/mL (198.75 mM)
Water 58 mg/mL (198.75 mM)
Ethanol 58 mg/mL (198.75 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 291.82
Formula

C17H21NO.HCl

CAS No. 147-24-0
Storage powder
in solvent
Synonyms N/A
Smiles Cl.CN(C)CCOC(C1=CC=CC=C1)C2=CC=CC=C2

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02509312 Unknown status Drug: Ketorolac|Drug: Epidural Morphine|Drug: Hydromorphone Analgesia Obstetrical University Hospitals Cleveland Medical Center May 2016 Phase 4
NCT01071057 Completed Drug: Naloxone|Drug: Saline/Morphine Pruritus University of British Columbia December 2010 Phase 2|Phase 3
NCT01289938 Terminated Drug: Diphenhydramine|Drug: Metoclopramide Drug Metabolism Poor CYP2D6-RELATED Matthias Schwab|University Hospital Tuebingen July 2009 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID