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琥珀酸多西拉敏 /Doxylamine succinate {[allProObj[0].p_purity_real_show]}

货号：A665536 同义名： 多西拉敏琥珀酸盐 / Doxylamine (succinate);NSC 74772

Doxylamine Succinate Salt is an antihistamine which inhibits histamine H1 receptors. It can be used as a short-term sedative and anticholinergic agent.

Doxylamine succinate 化学结构 CAS号：562-10-7
Doxylamine succinate 化学结构
CAS号：562-10-7
Doxylamine succinate 3D分子结构
CAS号：562-10-7
Doxylamine succinate 化学结构 CAS号：562-10-7
Doxylamine succinate 3D分子结构 CAS号：562-10-7
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Doxylamine succinate 纯度/质量文件 产品仅供科研

货号：A665536 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 H1 receptor ↓ H2 receptor ↓ H3 receptor ↓ H4 receptor ↓ Histamine receptor ↓ 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine ✔ 97%
Loratadine +

B(0)AT2, IC50: 4 μM

 		98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

 		98%
Doxylamine succinate ✔ 99%
Ebastine ✔ 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

 		98%
Meclizine dihydrochloride ✔ 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

 		99%
Diphenhydramine HCl ✔ 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

 		++

H2 receptor, pKi: 7.2

 		99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

 		99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

 		98%
Pemirolast potassium ✔ 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

 		98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

 		98%
Brompheniramine maleate ✔ 98%
Carbinoxamine maleate salt ✔ 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

 		98%
Ketotifen fumarate salt ✔ 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

 		PAFR 98%
Famotidine ✔ 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

 		98%
Lafutidine ✔ 99%
Cimetidine ✔ 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

 		AChE 98%
Ranitidine ✔ 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		98%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 98%
Levodropropizine ✔ 97%
Cyproheptadine hydrochloride ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin hydrochloride ✔ 99+%
Buclizine 2HCl ✔ 97%
Latrepirdine 2HCl ✔ GluR 98%
Cetirizine 2HCl ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Doxylamine succinate 生物活性

靶点

  • H1 receptor
描述 Doxylamine succinate is a commonly used antihistamine for respiratory allergies including allergic rhinitis as well as for the management of insomnia. Delirium, seizures, and coma are among the central adverse effects that are rare[3]. High-fat, high-calorie food intake does not affect the kinetics of doxylamine in healthy subjects[4]. Mean maximum observed plasma concentration (Cmax) and area under the concentration-time curve from time zero to time t (AUCt ) of doxylamine hydrogen succinate 12.5 mg and 25 mg tablets increased linearly and dose-dependently [12.5 mg: mean Cmax 61.94 ng/mL, coefficient of variation (CV) 23.2%; mean AUCt 817.33 ng·h/mL, CV 27.4%; and 25 mg: mean Cmax 124.91 ng/mL, CV 18.7%; mean AUCt 1630.85 ng·h/mL, CV 22.8%]. Doxylamine hydrogen succinate was safe and well tolerated[5]. Doxylamine succinate (DA) was formerly used as an antinauseant during pregnancy, showed no substantial mutagenicity in mouse embryos following transplacental exposure[6].

Doxylamine succinate 参考文献

[1]Somashekar BS, Nagana Gowda GA, et al. Differential protonation and dynamic structure of doxylamine succinate in solution using 1H and 13C NMR. Magn Reson Chem. 2004 Jul;42(7):636-40.

[2]Bookstaff RC, Murphy VA, et al. Effects of doxylamine succinate on thyroid hormone balance and enzyme induction in mice. Toxicol Appl Pharmacol. 1996 Dec;141(2):584-94.

[3]Derinöz-Güleryüz O. Doxylamine succinate overdose: Slurred speech and visual hallucination. Turk J Pediatr. 2018;60(4):439-442

[4]Videla S, Lahjou M, Guibord P, Xu Z, Tolrà C, Encina G, Sicard E, Sans A. Food effects on the pharmacokinetics of doxylamine hydrogen succinate 25 mg film-coated tablets: a single-dose, randomized, two-period crossover study in healthy volunteers. Drugs R D. 2012 Dec 1;12(4):217-25

[5]Videla S, Cebrecos J, Lahjou M, Wagner F, Guibord P, Xu Z, Cabot A, Encabo M, Encina G, Sicard E, Sans A. Pharmacokinetic dose proportionality between two strengths (12.5 mg and 25 mg) of doxylamine hydrogen succinate film-coated tablets in fasting state: a single-dose, randomized, two-period crossover study in healthy volunteers. Drugs R D. 2013 Jun;13(2):129-35

[6]Müller L, Korte A, Madle S. Mutagenicity testing of doxylamine succinate, an antinauseant drug. Toxicol Lett. 1989 Oct;49(1):79-86

Doxylamine succinate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.87mL

2.57mL

1.29mL

25.74mL

5.15mL

2.57mL

Doxylamine succinate 技术信息

CAS号562-10-7
分子式C21H28N2O5
分子量 388.457
别名 多西拉敏琥珀酸盐 ;Doxylamine (succinate);NSC 74772;562-10-7;A-H Injection;Evigoa D;Unisom;Decapryn
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

DMSO: 105 mg/mL(270.3 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(128.71 mM)，配合低频超声助溶
动物实验配方

Tags: Doxylamine succinate | Doxylamine (succinate);NSC 74772;562-10-7;A-H Injection;Evigoa D;Unisom;Decapryn | 多西拉敏琥珀酸盐 | Histamine Receptor | AmBeed-信号通路专用抑制剂 | Doxylamine succinate 纯度/质量文件 | Doxylamine succinate 亚型比较 | Doxylamine succinate 生物活性 | Doxylamine succinate 参考文献 | Doxylamine succinate 实验方案 | Doxylamine succinate 技术信息

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