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Doxylamine succinate

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Chemical Structure| 562-10-7 同义名 : 多西拉敏琥珀酸盐 ;Doxylamine (succinate);NSC 74772;562-10-7;A-H Injection;Evigoa D;Unisom;Decapryn
CAS号 : 562-10-7
货号 : A665536
分子式 : C21H28N2O5
纯度 : 99%
分子量 : 388.457
MDL号 : MFCD00056168
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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