Chlorpheniramine maleate

SKU: orb1308217

Description

Chlorpheniramine maleate (NCI-C55265) is a classical histamine H1 receptor antagonist. It is widely utilized in research to study allergic mechanisms, such as rhinitis and urticaria, and its pharmacological effects are characterized in both in vitro binding assays and in vivo models of hypersensitivity.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 113-92-8
• MW: 390.87
• Purity: 99.98% (May vary between batches)
• Formula: C₂₀H₂₃ClN₂O₄
• SMILES: OC(=O)\C=C/C(O)=O.CN(C)CCC(C1=CC=C(Cl)C=C1)C1=NC=CC=C1
• Target: Histamine Receptor
• Solubility: H2O:50 mg/mL (127.92 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.23 mM);DMSO:100 mg/mL (255.84 mM)

Bioactivity

• Target IC50:
  H1 receptor:12 nM
• In Vivo:
  Chlorpheniramine inhibits the binding of [3H] mepyramine to guinea pig cortical histamine H1 receptors (IC50=8.8 nM). It reduces ornithine decarboxylase mRNA translation in MCF-7, MDA-MB 231, and Ehrlich cells at a concentration of 250 μM, subsequently inhibiting cell proliferation. Chlorpheniramine displays antimalarial activity against Chloroquine-Sensitive (CQS) Plasmodium falciparum strain D6 (IC50=61.2uM) and Multidrug-Resistant (MDR) strain Dd2 (IC50=3.9uM). Furthermore, it exhibits cytotoxicity in mouse splenic lymphocytes induced by Concanavalin A (IC50=33.4 μM).
• In Vitro:
  Oral administration of Chlorpheniramine (10 mg/kg) can suppress short-term scratching in BALB/c mice experiencing albumin-induced allergic skin irritation and ICR mice injected with histamine subcutaneously. Furthermore, in guinea pigs induced with histamine (ED50=0.17 mg/kg), oral intake of Chlorpheniramine prevents mortality. In rats, a dosage of Chlorpheniramine (20 mg/kg) is capable of blocking the histamine or cholinergic mechanisms that induce rapid eye movement (REM) sleep.
• Cell Research:
  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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HistamineReceptor, Histamine Receptor, Inhibitor, H1 receptor, NCI-C55265, NCI-C-55265, NCI-C 55265, inhibit, Chlorpheniramine maleate, Chlorpheniramine Maleate, Chlorphenamine, Chlorphenamine maleate, Chlorphenamine Maleate, Chlorpheniramine

Compound Identifiers

PubChem CID

5281068