Pheniramine maleate

SKU: orb1226542

Description

Pheniramine Maleate is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria.(In Vitro):Pheniramine maleate inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time and prolong antihistaminic effects.Pheniramine maleate regulates cellular Ca2+ transmembrane action, and inhibits Ca2+ influx into BC3H-1 cells by inhibiting histamine with an IC50 value of 1.01 mM.Pheniramine maleate (0.5, 1.0 mM; 24 h) induces cell apoptosis in human T-cell acute lymphoblastic leukemia cell lines.Pheniramine maleate (1 μM-1 mM; 12-48 h) inhibits cell proliferation in a time-dependent manner and shows inhibitory concentration IC50s of 550 μM (CCRF-CEM cells) and 420 μM (Jurkat cells), respectively.(In Vivo):Pheniramine maleate (1.75 μM; i.t.) exerts local anesthesia effect and results spinal block in rats.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 132-20-7
• MW: 356.42
• Purity: >98% (HPLC)
• Formula: C₁₆H₂₀N₂·C₄H₄O₄
• SMILES: CN(C)CCC(C1=CC=CC=C1)C2=CC=CC=N2.C(=C\C(=O)O)\C(=O)O
• Target: 5-HT Receptor
• Solubility: Ethanol: 71 mg/mL (199.2 mM); Water: 71 mg/mL (199.2 mM); DMSO: 71 mg/mL (199.2 mM)

Bioactivity

• In Vivo:
  Pheniramine maleate (1.75 μM; i. t.) exerts local anesthesia effect and results spinal block in rats. Animal model: Sprague–Dawley rats (300-350 g; male). Dosage: 0.30, 0.60, 0.90, 1.50, 1.75 μM. Administration: Intrathecal injection; one time. Result: Resulted the spinal block and displayed dose-dependent effect. Showed 100% blockades in motor function, proprioception, and nociception, with full recoveryduration of action about 41, 56, and 88 min, respectively, at 1.75 μM.
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• In Vitro:
  Pheniramine maleate inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time and prolong antihistaminic effects. Pheniramine maleate regulates cellular Ca2+ transmembrane action, and inhibits Ca2+ influx into BC3H-1 cells by inhibiting histamine with an IC50 value of 1.01 mM. Pheniramine maleate (0.5, 1.0 mM; 24 h) induces cell apoptosis in human T-cell acute lymphoblastic leukemia cell lines. Pheniramine maleate (1 μM-1 mM; 12-48 h) inhibits cell proliferation in a time-dependent manner and shows inhibitory concentration IC50s of 550 μM (CCRF-CEM cells) and 420 μM (Jurkat cells), respectively. They are for reference only. Cell Viability Assay Cell line: Human T-cell acute lymphoblastic leukemia cell lines: CCRF-CEM and Jurkat ALL. Concentration: 0.5, 1.0 mM Incubation time: 24 hours. Result: Induced cells apoptosis with chromatin condenses and marginalizes, and nuclear debris spreaded into the cytoplasm. Cell Viability Assay Cell line: Human T-cell acute lymphoblastic leukemia cell lines: CCRF-CEM and Jurkat ALL. Concentration: 1 μM-1 mM. Incubation time: 12, 24, 48 hours. Result: Inhibited cell proliferation and survival in a time- and dose-dependent manner.
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Storage & Handling

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

Quick Database Links

Gene Symbol

5-HT Receptor