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].
Rupatadine Fumarate/富马酸卢帕他定 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human umbilical vein endothelial cells (HUVEC)
500 ng/ml
1 hour
To evaluate the effects of Rupatadine on dengue sera-induced endothelial permeability. Results showed that Rupatadine significantly reduced the effects of acute dengue sera on the expression of tight junction protein ZO-1 and trans-endothelial electrical resistance (TEER) in HUVEC cells.
Sci Rep. 2018 Mar 1;8(1):3857
Ltk7 cells
0.01, 1 and 20 µM
4 minutes to 10 minutes
To study the blocking effects of Rupatadine on hKv1.5 channels, results showed that Rupatadine blocked hKv1.5 channels in a concentration-dependent manner (KD=2.4±0.7 μM) and slowed the deactivation of tail currents.
Br J Pharmacol. 1999 Nov;128(5):1071-81
HEK293T cells
6 nM
6 hours
Determination of Rupatadine's residence time at the H1R using [3H]levocetirizine competitive association experiments. Results indicated that Rupatadine has a residence time exceeding 300 min, at least 10-fold longer than desloratadine.
J Med Chem. 2019 Jul 25;62(14):6630-6644
TOV 112D
30 µM
72 hours
To evaluate the inhibitory effect of rupatadine on ovarian cancer cell proliferation. Results showed that rupatadine significantly inhibited the proliferation of TOV 112D cells.
Cells. 2021 Sep 7;10(9):2337
ES-2
30 µM
72 hours
To evaluate the inhibitory effect of rupatadine on ovarian cancer cell proliferation. Results showed that rupatadine significantly inhibited the proliferation of ES-2 cells.
Cells. 2021 Sep 7;10(9):2337
UWB1.289
30 µM
72 hours
To evaluate the inhibitory effect of rupatadine on ovarian cancer cell proliferation. Results showed that rupatadine significantly inhibited the proliferation of UWB1.289 cells.
Cells. 2021 Sep 7;10(9):2337
OVCAR-3
30 µM
72 hours
To evaluate the inhibitory effect of rupatadine on ovarian cancer cell proliferation. Results showed that rupatadine significantly inhibited the proliferation of OVCAR-3 cells.
Cells. 2021 Sep 7;10(9):2337
Rupatadine Fumarate/富马酸卢帕他定 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
DENV-2 infection model
Intraperitoneal
0.8 and 3 mg/kg
Administered 30 minutes post-infection, monitored for 24 hours
To assess the effect of Rupatadine in reducing vascular leak in a dengue-infected mouse model. Results demonstrated that Rupatadine significantly inhibited the increased haematocrit in dengue-infected mice, showing dose-dependency.
Sci Rep. 2018 Mar 1;8(1):3857
Apoe-/- female mice
Atherosclerosis model
Dietary administration
170 mg/kg diet
12 weeks
To evaluate the potential beneficial effects of Rupatadine on atherosclerosis development. Results showed that Rupatadine treatment led to an approximately 22% increase in aortic sinus plaque area and a significant increase in T lymphocyte numbers in the plaque and myocardial parenchyma surrounding the aortic sinus.
Thromb Haemost. 2022 May;122(5):853-856
Wistar rats
DEN-induced liver fibrosis model
Oral
4 mg/kg/day
Once daily for 4 weeks
To assess the potential therapeutic effect of Rupatadine in DEN-induced liver fibrosis and to explore its possible mechanistic actions. Results showed that RUP ameliorated changes in body weights, liver indices, liver function enzymes, and histopathological alterations induced by DEN. Additionally, RUP amended oxidative stress, inhibited PAF/NF-κB p65-induced inflammation, and prevented TGF-β1 elevation and HSCs activation. Moreover, RUP exerted significant anti-fibrotic and anti-angiogenic effects by suppressing Hh and HIF-1α/VEGF signaling pathways.
Inflammopharmacology. 2023 Apr;31(2):845-858
Wistar albino rats
Isoproterenol-induced heart failure model
Oral
4 mg/kg/day
Once daily for 14 days
To assess the possible protection afforded by rupatadine against isoproterenol-induced heart failure in rats and to explore the role of PI3k/Akt as a possible mechanistic pathway. Results showed that rupatadine significantly improved electrocardiographic and echocardiographic measurements, prevented the marked elevation of PAF and oxidative stress, and inhibited the production of Th17-promoting cytokines (IL-6, IL-23, and TGF-β).
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