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Rupatadine Fumarate

CAS No. : 182349-12-8

MCE 站：Rupatadine Fumarate

产品活性：Rupatadine Fumarate (UR-12592 Fumarate) 富马酸盐是口服有效的、长效的，PAF/H1 受体的双抑制剂，K_i 值分别为 0.55 μM 和 0.1 μM。Rupatadine (UR-12592) Fumarate 可维持纤维化肺组织中的自噬通量。

研究领域：Immunology/Inflammation  |  GPCR/G Protein  |  Neuronal Signaling  |  Autophagy

作用靶点：Histamine Receptor  |  Autophagy

In Vitro: Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA₂ = 9.29 ± 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). Rupatadine also competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA₂ = 6.68 ± 0.08) and in human platelet-rich plasma (HPRP) (IC₅₀ ± 0.68 μM), while not affecting ADP- or arachidonic acidinduced platelet aggregation.
Rupatadine (0.1-30 μM) inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5 ± 3.5%.

In Vivo: Rupatadine blocks histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID₅₀ ± 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID₅₀ 5 113 and 9.6 mg/kg i.v.). Rupatadine also potently inhibits PAF-induced mortality in mice (ID₅₀ ± 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID₅₀ ± 1.6 and 0.66 mg/kg i.v.).
Rupatadine (6 mg/kg) promots the absorption of the lesions and decreased the density of lungs.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Neuronal Signaling Compound Library  |  FDA-Approved Drug Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  NMPA-Approved Drug Library  |  Orally Active Compound Library  |  Neurotransmitter Receptor Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Histamine  |  Clemastine fumarate  |  Amitriptyline hydrochloride  |  Astemizole  |  Fexofenadine hydrochloride  |  Osthole  |  Terfenadine  |  Famotidine  |  Diphenhydramine hydrochloride  |  Levocetirizine dihydrochloride  |  Perphenazine  |  Loratadine  |  Cimetidine  |  Chlorprothixene  |  Lodoxamide  |  Pitolisant hydrochloride  |  Desloratadine  |  Latrepirdine dihydrochloride  |  Mianserin hydrochloride  |  Mirtazapine  |  Ebastine  |  Azelastine hydrochloride  |  Ritanserin  |  Chlorpheniramine maleate  |  Mepyramine maleate  |  Cinnarizine  |  Ranitidine hydrochloride  |  Clemizole hydrochloride  |  Ketotifen fumarate

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