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编 号：F485183
分子式：C16H20N2
分子量：240.34
分子式：C16H20N2
分子量：240.34
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CAS No: 86-21-5
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生物活性：
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local anesthetic, with antipruritic effects.
体内研究：
Pheniramine (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 inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time andprolong antihistaminic effects.Pheniramine inhibits Ca2+ influx into BC3H-1 cells by inhibiting histamine with an IC50 value of 1.01 mM and regulates cellular Ca2+ transmembrane action.Pheniramine (0.5, 1.0 mM; 24 h) induces cell apoptosis in human T-cell acute lymphoblastic leukemia cell lines.Pheniramine (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.
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local anesthetic, with antipruritic effects.
体内研究：
Pheniramine (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 inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time andprolong antihistaminic effects.Pheniramine inhibits Ca2+ influx into BC3H-1 cells by inhibiting histamine with an IC50 value of 1.01 mM and regulates cellular Ca2+ transmembrane action.Pheniramine (0.5, 1.0 mM; 24 h) induces cell apoptosis in human T-cell acute lymphoblastic leukemia cell lines.Pheniramine (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.
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