产品
编 号:F119624
分子式:C20H24N2O4
分子量:356.42
产品类型
结构图
CAS No: 132-20-7
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产品详情
生物活性:
Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local anesthetic, with antipruritic effects.
体内研究:
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.
体外研究:
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.