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Rupatadine Fumarate

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Chemical Structure| 182349-12-8 同义名 : UR-12592 Fumarate;Rupatadine (fumarate)
CAS号 : 182349-12-8
货号 : A160823
分子式 : C30H30ClN3O4
纯度 : 98%
分子量 : 532.03
MDL号 : MFCD00926499
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(56.39 mM)，配合低频超声，并水浴加热至45℃助溶，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
动物实验配方：
生物活性
靶点

  • H1 receptor

    Histamine H1 receptor, Ki:102 nM
描述 Rupatadine fumarate is a second-generation antihistamine provided with a potent, long-lasting and balanced in vivo dual platelet-activating factor (PAF) and histamine antagonist activity and it uniquely combines both activities at a high level of potency. Rupatadine has a rapid onset of action and a long-lasting effect, so a once-daily dosing is permitted, moreover is well tolerated by young adults and the elders[3]. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria[4]. New studies have demonstrated that rupatadine inhibits PAF effects in nasal airways and produces a greater reduction in nasal symptoms than levocetirizine[5]. Rupatadine 20 and 40 mg significantly reduced the development of chronic cold urticaria symptom without an increase in adverse effects[6]. Moreover, rupatadine significantly reduced endothelial permeability by dengue sera in vitro, and significantly inhibited the increased haematocrit in dengue-infected mice with dose-dependency[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.40mL

1.88mL

0.94mL

18.80mL

3.76mL

1.88mL
参考文献

[1]Queralt M, Brazis P, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60.

[2]Merlos M, Giral M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21.

[3]Nettis E, Delle Donne P, Di Leo E, Calogiuri GF, Ferrannini A, Vacca A. Rupatadine for the treatment of urticaria. Expert Opin Pharmacother. 2013 Sep;14(13):1807-13

[4]González-Núñez V, Bachert C, Mullol J. Rupatadine: global safety evaluation in allergic rhinitis and urticaria. Expert Opin Drug Saf. 2016 Oct;15(10):1439-48

[5]Mullol J, Bousquet J, Bachert C, Canonica GW, Giménez-Arnau A, Kowalski ML, Simons FE, Maurer M, Ryan D, Scadding G. Update on rupatadine in the management of allergic disorders. Allergy. 2015 Jan;70 Suppl 100:1-24

[6]Abajian M, Curto-Barredo L, Krause K, Santamaria E, Izquierdo I, Church MK, Maurer M, Giménez-Arnau A. Rupatadine 20 mg and 40 mg are Effective in Reducing the Symptoms of Chronic Cold Urticaria. Acta Derm Venereol. 2016 Jan;96(1):56-9

[7]Malavige GN, Wijewickrama A, Fernando S, Jeewandara C, Ginneliya A, Samarasekara S, Madushanka P, Punchihewa C, Paranavitane S, Idampitiya D, Wanigatunga C, Dissanayake H, Prathapan S, Gomes L, Aman SAB, John AS, Ogg GS. A preliminary study on efficacy of rupatadine for the treatment of acute dengue infection. Sci Rep. 2018 Mar 1;8(1):3857