Pheniramine Maleate|132-20-7|(马来酸非尼拉敏; Prophenpyridamine maleate; Tripoton maleate)-陌孚医药/Medlife

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Pheniramine Maleate (Synonyms: 马来酸非尼拉敏; Prophenpyridamine maleate; Tripoton maleate)

目录号: PC16552 纯度: ≥98%

CAS No. :132-20-7

商品编号	规格	价格	会员价	是否有货	数量
PC16552-50mg	50mg	¥411.60	请登录
PC16552-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

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中文名称	Pheniramine Maleate
中文别名	马来酸非尼拉敏;1-苯基-1-(2-吡啶基)-3-二甲氨基丙烷马来酸盐;马来酸-非尼拉敏;非尼拉敏马来酸盐;8-甲基壬醛;Pheniramine Maleate 非尼拉敏马来酸盐;马来酸苯吡胺;马来酸非利拉明 EP标准品;马来酸非尼拉敏 USP标准品;马来酸非尼拉敏原药;专利兰VF;马来酸非利拉明;马来酸溴苯那敏杂质C(EP) 标准品;马来酸右氯苯那敏杂质A;马来酸非尼拉敏(1-苯基-1-(2-吡啶基)-3-二甲氨基丙烷马来酸盐);非尼拉敏马来酸盐
英文名称	Pheniramine Maleate
英文别名	Pheniramine maleate;1-Phenyl-1-(2-pyridyl)-3-dimethylaminopropane maleate;Heniramine Maleate;Pheniramine (Maleate);PHENIRAMINE MALEATE SALT;(Z)-but-2-enedioic acid,N,N-dimethyl-3-phenyl-3-pyridin-2-ylpropan-1-amine;pm241;Fervex;ho11513;daneral;inhiston;Trimetose;205-051-4;Antolozine;avil-retard;trimetonmaleate;Naphcon a;Pheniramine hydrogen maleate;Prophenpyridamine maleate;PM 241;HO 11513;2-(alpha-(2-(Dimethylamino)ethyl)benzyl)pyridine, maleate;2-(alpha-(2-(Dimethylamino)ethyl)benzyl)pyridine, bimaleate;Phenyl(2-pyridyl)(beta-N,N-dimethylaminomethyl) methane maleate;1-(N,N-Dimethyl
Cas No.	132-20-7
分子式	C₂₀H₂₄N₂O₄
分子量	356.42
包装储存	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

性状

Solid

IC50 & Target[1][2]

H₁ Receptor

1.01 mM (IC₅₀)

体外研究(In Vitro)

Pheniramine maleate inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time and prolong antihistaminic effects.
Pheniramine maleate regulates cellular Ca transmembrane action, and inhibits Ca 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.

Medlife has not independently confirmed the accuracy of these methods. 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.

体内研究(In Vivo)

Pheniramine maleate (1.75 μM; i.t.) exerts local anesthesia effect and results spinal block in rats.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃，, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[1]. Sharma A, et al. Classic histamine H1 receptor antagonists: a critical review of their metabolic and pharmacokinetic fate from a birds eye view. Curr Drug Metab. 2003 Apr;4(2):105-29. [Information]

[2]. Brown RD, et al. Alpha 1-adrenergic and H1-histamine receptor control of intracellular Ca2+ in a muscle cell line: the influence of prior agonist exposure on receptor responsiveness. Mol Pharmacol. 1986 Jun;29(6):531-9. [Information]

[3]. Jangi SM, et al. Apoptosis of human T-cell acute lymphoblastic leukemia cells by diphenhydramine, an H1 histamine receptor antagonist. Oncol Res. 2004;14(7-8):363-72. [Information]

[4]. Hung CH, et al. Spinal anesthesia with diphenhydramine and pheniramine in rats. Eur J Pharmacol. 2011 Dec 30;673(1-3):20-4. [Information]

溶解度数据

体外研究:

H₂O : ≥ 38 mg/mL (106.62 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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