Home Neuronal Signaling Histamine Receptor inhibitor Rupatadine Fumarate

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Rupatadine Fumarate Histamine Receptor inhibitor

Cat.No.S3052

Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.
Rupatadine Fumarate Histamine Receptor inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 532.03

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Quality Control

Batch: S305201 Ethanol]13 mg/mL]false]DMSO]9 mg/mL]false]Water]Insoluble]false Purity: 99.69%
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  • NMR
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99.69

Solubility

In vitro
Batch:

Ethanol : 13 mg/mL

DMSO : 9 mg/mL (16.91 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 532.03 Formula

C26H26ClN3.C4H4O4

 Storage (From the date of receipt)
CAS No. 182349-12-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC(=CN=C1)CN2CCC(=C3C4=C(CCC5=C3N=CC=C5)C=C(C=C4)Cl)CC2.C(=CC(=O)O)C(=O)O

Mechanism of Action

Targets/IC50/Ki
Histamine H1 receptor
102 nM(Ki)
PAFR
550 nM(Ki)
In vitro
Rupatadine inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors. 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). It 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 acid-induced platelet aggregation. In another study, it is reported rupatadine and loratadine shows similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibits inhibitory effect against TNF-α.
Kinase Assay
[3H]-Pyrilamine binding to histamine (H1) receptors in guinea pig cerebellum membranes.
Antagonists are incubated with guinea pig cerebellum membranes (0.6 mg/ml) and [3H]-pyrilamine (1.2 nM) in 0.5 ml 50 mM PBS, pH 7.5, for 30 min at 25 ℃. The incubation is ended by the addition of 5 ml of ice-cold PBS containing 2 μM pyrilamine and the collection of membranes on Whatman GF/B filters. Then the filters are washed with 3 × 5 ml of ice-cold PBS plus 2 μM pyrilamine and transferred to counting vials. The radioactivity retained by each filter is measured by liquid scintillation counting in 3 ml of HiSafe 3. Specific binding is determined from the difference between the [3H]-pyrilamine bound in the absence and in the presence of a large molar excess (10 μM) of unlabeled promethazine.
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 = 113 and 9.6 μg/kg i.v.). Moreover, it 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's duration of action is long, as assessed by the histamine- and PAF-induced increase in vascular permeability test in dogs (42 and 34% inhibition at 26 h after 1 mg/kg p.o.). Rupatadine at a dose of 100 mg/kg p.o. neither modifies spontaneous motor activity nor prolongs barbiturate-sleeping time in mice, which indicates a lack of sedative effects.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/23120659/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01605487 Completed
Cold Contact Urticaria
Charite University Berlin Germany|Hospital del Mar
 June 2012 Phase 2
NCT00199251 Terminated
Urticaria
J. Uriach and Company
 April 2004 Phase 3

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