Brompheniramine hydrogen maleate

SKU: orb1223488

Description

Brompheniramine maleate is a histamine H1 receptors antagonist. (In Vitro):Brompheniramine (0.1-100 μM) blocks hERG K+ channels expressed in CHO cells in a concentration-dependent manner with an IC50 of 0.90±0.14 μM, and reduced peak tail current amplitude measured at -60 mV (cells are depolarized for 2 s to +20 mV from a holding potential of -80 mV followed by a 3s repolarization back to -60 mV).Brompheniramine (1, 10 and 100 μM) significantly shortens the APD50 and depresses the plateau phase on the action potential in guinea pig papillary muscle, as well as slightly prolongs the APD90 in guinea pig papillary muscle at 10 and 100 μM.Brompheniramine (0.1-100 μM) inhibit the amplitude of the Ca2+ channel currents in rat ventricular myocytes by 14.1±1.1, 31.1±5.8, 38.0±3.8 and 90.2±3.7% at 0.1, 1, 10 and 100 μM, respectively.Brompheniramine blocks muscarinic cholinergic receptors in human chinese hamster ovary (CHO) cells.(In Vivo):Brompheniramine (0.3-3 μM; SC, single dosage) induces cutaneous analgesia in rats.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 980-71-2
• MW: 435.31
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₉BrN₂·C₄H₄O₄
• SMILES: CN(C)CCC(C1=CC=C(C=C1)Br)C2=CC=CC=N2.C(=C\C(=O)O)\C(=O)O
• Target: 5-HT Receptor
• Solubility: Ethanol: 18 mg/mL (41.34 mM); Water: 46 mg/mL warmed (105.67 mM); DMSO: 87 mg/mL (199.85 mM)

Bioactivity

• In Vivo:
  Brompheniramine (0.3-3 μM; SC, single dosage) induces cutaneous analgesia in rats. Animal model: Male Sprague-Dawley rats. Dosage: 0.3, 0.6, 1.1, 1.5 and 3.0 μM. Administration: SC, single dosage. Result: Provoked cutaneous analgesia in a dose-dependent manner, with an EC50 value of 0.66 μM, and induced prolonged analgesic duration.
• In Vitro:
  Brompheniramine (0.1-100 μM) blocks hERG K+ channels expressed in CHO cells in a concentration-dependent manner with an IC50 of 0.90±0.14 μM, and reduced peak tail current amplitude measured at -60 mV (cells are depolarized for 2 s to +20 mV from a holding potential of -80 mV followed by a 3s repolarization back to -60 mV). Brompheniramine (1, 10 and 100 μM) significantly shortens the APD50 and depresses the plateau phase on the action potential in guinea pig papillary muscle, as well as slightly prolongs the APD90 in guinea pig papillary muscle at 10 and 100 μM. Brompheniramine (0.1-100 μM) inhibit the amplitude of the Ca2+ channel currents in rat ventricular myocytes by 14.1±1.1, 31.1±5.8, 38.0±3.8 and 90.2±3.7% at 0.1, 1, 10 and 100 μM, respectively. Brompheniramine blocks muscarinic cholinergic receptors in human chinese hamster ovary (CHO) cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

(±)-Brompheniramine

Quick Database Links

Gene Symbol

5-HT Receptor