Diphenhydramine HCl

Catalog No.S1866

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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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
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02960555 Recruiting Myeloma M.D. Anderson Cancer Center|Sanofi February 8, 2017 Phase 2
NCT02240407 Not yet recruiting Pompe Disease University of Florida April 2017 Phase 1
NCT02935699 Not yet recruiting Acute Urticaria JDP Therapeutics, Inc. December 2016 Phase 3
NCT02648490 Recruiting Solid Tumour Henlix, Inc September 2016 Phase 1
NCT02867800 Recruiting Sickle Cell Disease|Graft Versus Host Disease Monica Bhatia|Columbia University July 2016 Phase 1
NCT02711826 Recruiting Kidney Transplant|Adult Living Donor Kidney Transplant Recipients|Renal Transplant|Living Kidney Donor National Institute of Allergy and Infectious Diseases (NIAID)|Clinical Trials in Organ Transplantation May 2016 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID