Pheniramine (Prophenpyridamine; Tripoton) maleate 是第一代组胺H1受体拮抗剂，作用于中枢神经系统 (CNS) ，产生镇静、助眠的作用。Pheniramine maleate 也是安全、有效的局部麻醉剂，并有止痒作用。
| 生物活性 | Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generationhistamine H1 receptorantagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cellsapoptosis. Pheniramine maleate is also a safe and effective local anesthetic, with antipruritic effects[1][2][3][4]. |
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体外研究
(In Vitro) | Pheniramine maleate inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time and prolong antihistaminic effects[1].
Pheniramine maleate regulates cellular Ca2+transmembrane action, and inhibits Ca2+influx into BC3H-1 cells by inhibiting histamine with an IC50value of 1.01 mM[2].
Pheniramine maleate (0.5, 1.0 mM; 24 h) induces cell apoptosis in human T-cell acute lymphoblastic leukemia cell lines[3].
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[3].
Cell Viability Assay[3] | 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[3] | 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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体内研究
(In Vivo) | Pheniramine maleate (1.75 μM; i.t.) exerts local anesthesia effect and results spinal block in rats[4].
| Animal Model: | Sprague–Dawley rats (300-350 g; male)[4] | | 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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| 中文名称 | 马来酸非利拉明 （右氯苯那敏EP杂质A 马来酸盐） |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : ≥ 38 mg/mL(106.62 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.8057 mL | 14.0284 mL | 28.0568 mL | | 5 mM | 0.5611 mL | 2.8057 mL | 5.6114 mL | | 10 mM | 0.2806 mL | 1.4028 mL | 2.8057 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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