Home Neuronal Signaling Histamine Receptor antagonist Chlorpheniramine Maleate

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Chlorpheniramine Maleate Histamine Receptor antagonist

Cat.No.S1816

Chlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is an histamine H1 receptor antagonist with IC50 of 12 nM.
Chlorpheniramine Maleate Histamine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 390.86

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Quality Control

Batch: S181601 DMSO]78 mg/mL]false]Water]78 mg/mL]false]Ethanol]78 mg/mL]false Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 78 mg/mL

Ethanol : 78 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 390.86 Formula

C16H19ClN2.C4H4O4

 Storage (From the date of receipt)
CAS No. 113-92-8 Download SDF Storage of Stock Solutions

Synonyms NCI-C55265 Smiles CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2.C(=CC(=O)O)C(=O)O

Mechanism of Action

Targets/IC50/Ki
Histamine H1 receptor
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. 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. 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. 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.
Kinase Assay
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.
In vivo
Oral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg. 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. 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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17846138/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19443731/
  • [6] https://pubmed.ncbi.nlm.nih.gov/12826242/

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