Chlorpheniramine Maleate

Catalog No.S1816 Synonyms: NCI-C55265

Chlorpheniramine Maleate Chemical Structure

Molecular Weight(MW): 390.86

Chlorpheniramine (Chlorpheniramine maleate, Chlorphenamine) is an histamine H1 receptor antagonist with IC50 of 12 nM.

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In DMSO USD 130 In stock
USD 97 In stock
USD 970 In stock
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Biological Activity

Description Chlorpheniramine (Chlorpheniramine maleate, Chlorphenamine) is an histamine H1 receptor antagonist with IC50 of 12 nM.
Targets
Histamine H1 receptor [1]
12 nM
In vitro

Chlorpheniramine inhibits the [3H]mepyramine binding to the histamine H1 receptor in guinea pig cortex with IC50 of 8.8 nM. [2] Chlorpheniramine inhibits the proliferation of MCF-7, MDA-MB 231, and Ehrlich cells in a dose-response manner, and significantly reduces the ornithine decarboxylase mRNA translation by 50%-70% at the 250 μM. [3] Chlorpheniramine displaces of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells with IC50 of 66 nM. Chlorpheniramine displays antimalarial activity against CQS strain (D6) and MDR strain (Dd2) of P. falciparum with IC50 of 61.2 uM and 3.9 uM, respectively. Chlorpheniramine displays cytotoxicity against the proliferation of concanavalin A-induced murine splenic lymphocytes with IC50 of 33.4 μM. [4] Chlorpheniramine treatment in human salivary gland cells more significantly inhibits the histamine-induced [Ca2+]i increase in a concentration-dependent manner with IC50 of 128 nM than that of carbachol-induced [Ca2+]i increase with an IC50 of 43.9 μM. [5]

In vivo Oral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg. [1] Oral administration of Chlorpheniramine (10 mg/kg) significantly inhibits short-duration scratching in BALB/c mice stimulated by ovalbumin active cutaneous anaphylaxis and in ICR mice subcutaneously injected with histamine, but not long-duration scratching seen in NC/Nga mice, in contrast to that of dexamethasone or tacrolimus. [6] Administration of Chlorpheniramine (20 mg/kg) significantly abolishes the increase in REM sleep in rats induced by immobilization stress due to the blockage of the histaminergic and cholinergic mechanisms generating REM sleep. [7]

Protocol

Kinase Assay:[1]
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H1-Antihistaminic Activity:

The segments (1 cm) of isolated ileum from guinea pigs are suspended in an organ bath containing Tyrode solution (ventilation, 32 °C). The contractile responses to histamine (0.54 μM) are measured with an isotonic transducer. A set concentration of Chlorpheniramine is added in the organ bath 5 minutes before the addition of histamine. IC50 value of Chlorpheniramine is calculated by the probit methond.
Cell Research:[3]
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  • Cell lines: MCF-7, MDA-MB 231, and Ehrlich
  • Concentrations: Dissolved in water, final concentrations ~500 μM
  • Incubation Time: 48 hours
  • Method: Cells are exposed to various concentrations of Chlorpheniramine for 48 hours. Cells are washed, detached, and counted with a Coulter counter for the determination of cell growth.
    (Only for Reference)
Animal Research:[6]
+ Expand
  • Animal Models: Male NC/Nga mice, male ICR mice and female BALB/c mice with atopic dermatitis
  • Formulation: Suspended in 1% (v/v) Tween 80
  • Dosages: 10 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.55 mM)
Water 78 mg/mL (199.55 mM)
Ethanol 78 mg/mL (199.55 mM)
In vivo Add solvents individually and in order:
Saline
20 mg/mL

* 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 390.86
Formula

C16H19ClN2.C4H4O4

CAS No. 113-92-8
Storage powder
Synonyms NCI-C55265

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02675374 Recruiting Hemodynamic Instability|Vasoplegic Syndrome University Hospital, Bordeaux June 2016 Phase 3
NCT02722083 Terminated Rhinitis, Allergic Bayer May 2016 Phase 2
NCT02583594 Active, not recruiting Progressive Multiple Sclerosis Genzyme, a Sanofi Company|Sanofi December 2015 Phase 1
NCT02441894 Completed Prostate Cancer Sanofi April 2015 Phase 4
NCT01529242 Recruiting Cutaneous Hypersensitivity EMS February 2014 Phase 3
NCT01529229 Completed Allergic Rhinitis EMS November 2013 Phase 3

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID