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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Neuronal Signaling >Histamine Receptor Inhibitors >Rupatadine Fumarate

Rupatadine Fumarate

Rupatadine Fumarate Structure
  • ₹8400.2 - ₹33936.38
  • Product name: Rupatadine Fumarate
  • CAS: 182349-12-8
  • MF: C26H26ClN3.C4H4O4
  • MW: 532.03
  • EINECS:1592732-453-0
  • MDL Number:MFCD00926499
  • Synonyms:Rupafin FuMarate;Rupax FuMarate;5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]-, (2E)-2-butenedioate (1:1);RUPATADINE FUMARATE;8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene]-5h-benzo[5,6]cyclohepta[1,2-b]pyridine fumarate;Alergoliber FuMarate;Pafinur FuMarate;Rinialer FuMarate
2 prices
Selected condition:

Brand

  • Sigma-Aldrich(India)

Package

  • 10MG
  • 50MG
  • ManufacturerSigma-Aldrich(India)
  • Product numberSML2898
  • Product descriptionRupatadine fumarate ≥98% (HPLC)
  • Packaging50MG
  • Price₹33936.38
  • Updated2022-06-14
  • Buy
  • ManufacturerSigma-Aldrich(India)
  • Product numberSML2898
  • Product descriptionRupatadine fumarate ≥98% (HPLC)
  • Packaging10MG
  • Price₹8400.2
  • Updated2022-06-14
  • Buy
Manufacturer Product number Product description Packaging Price Updated Buy
Sigma-Aldrich(India) SML2898 Rupatadine fumarate ≥98% (HPLC) 50MG ₹33936.38 2022-06-14 Buy
Sigma-Aldrich(India) SML2898 Rupatadine fumarate ≥98% (HPLC) 10MG ₹8400.2 2022-06-14 Buy

Properties

Melting point :196-198°C
storage temp. :Sealed in dry,2-8°C
solubility :Methanol (Slightly, Heated)
form :Solid
color :White to Pale Brown

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning GHS hazard pictograms P264, P270, P301+P312, P330, P501
Precautionary statements:
P264 Wash hands thoroughly after handling.
P264 Wash skin thouroughly after handling.
P270 Do not eat, drink or smoke when using this product.
P301+P312 IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P501 Dispose of contents/container to..…

Description

Rupatadine fumarate, a novel antiallergic drug with a dual mechanism of action, was introduced in Spain as an oral treatment for perennial and seasonal rhinitis. Rupatadine acts as non-sedating histamine H1 receptor antagonist and plateletactivating factor (PAF) antagonist. Its Kiapp i values against [3H]WEB-2086 binding to rabbit platelet membrane PAF receptors and [3H]pyralimine binding to guinea pig cerebellum membrane H1 histamine receptors are 0.55 and 0.10 μM, respectively. It has a rapid onset of action, with patients experiencing relief of symptoms within 2 h, and its long duration of action (>24 h) permits once-daily dosing. Rupatidine is prepared in a 6-step convergent synthesis, with the key steps involving the Grignard reaction of a N-alkyl-4-chloropiperdine with a benzocycloheptapyridinone intermediate, followed by dehydration. Rupatadine is rapidly absorbed after oral administration. The time to reach maximum plasma concentration is 0.75–1 h and the mean half-life in healthy volunteers is ~6 h. It is extensively metabolized, mainly by CYP3A4, and the major elimination route for the drug is biliary excretion. In comparative clinical trials, rupatadine 10 mg once daily was as effective as certizine 10 mg in short-term studies (2–4 weeks duration), but provided a better profile of CNS side effects. In comparison with ebastine 10 mg and loratadine 10 mg, rupatadine showed a superior relief of rhinitis symptoms at the same dose. Rupatadine was well tolerated in clinical trials and, at the recommended daily dose of 10 mg, was free of the sedative effects associated with first-generation antihistamines. In addition, there were no significant differences in the overall incidence of adverse events in rupatidine-treated patients and those treated with placebo or standard reference products.

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