Rupatadine - CAS 158876-82-5
Catalog number: 158876-82-5
Category: Inhibitor
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Molecular Formula:
C26H26ClN3
Molecular Weight:
415.96
COA:
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Targets:
5-HT Receptor
Description:
Rupatadine, with the potential to treat allergic rhinitis and urticaria, is a potent and long-lasting dual antagonist of PAF/H1. in vitro: Without affecting contraction induced by ACh, it competitively inhibited histamine-induced guinea pig ileum contract
Appearance:
White solid powder
Synonyms:
8-chloro-11-[1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene]-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridine Rupatadine 158876-82-5 Alergoliber Pafinur Rinialer Rupax Rupafin UNII-2AE8M83G3E CHEMBL91397
Solubility:
Soluble in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -98℃ for long term (months to years).
MSDS:
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Shelf Life:
2 years
Quantity:
Grams-Kilos
Boiling Point:
586.4±50.0 °C | Condition: Press: 760 Torr
Melting Point:
136-137 °C | Condition: Solv: toluene
Density:
1.233g/cm3
InChIKey:
WUZYKBABMWJHDL-UHFFFAOYSA-N
InChI:
1S/C26H26ClN3/c1-18-13-19(16-28-15-18)17-30-11-8-20(9-12-30)25-24-7-6-23(27)14-22(24)5-4-21-3-2-10-29-26(21)25/h2-3,6-7,10,13-16H,4-5,8-9,11-12,17H2,1H3
Canonical SMILES:
CC1=CC(=CN=C1)CN2CCC(=C3C4=C(CCC5=C3N=CC=C5)C=C(C=C4)Cl)CC2
1.Olopatadine hydrochloride and rupatadine fumarate in seasonal allergic rhinitis: A comparative study of efficacy and safety.
Maiti R1, Jaida J, Rahman J, Gaddam R, Palani A. J Pharmacol Pharmacother. 2011 Oct;2(4):270-6. doi: 10.4103/0976-500X.85958.
OBJECTIVE: To compare the efficacy and safety of olopatadine and rupatadine in seasonal allergic rhinitis (SAR).
2.Rupatadine for the treatment of urticaria.
Nettis E1, Delle Donne P, Di Leo E, Calogiuri GF, Ferrannini A, Vacca A. Expert Opin Pharmacother. 2013 Sep;14(13):1807-13. doi: 10.1517/14656566.2013.813481. Epub 2013 Jun 28.
INTRODUCTION: 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. Rupatadine does not present the side effects of first-generation H1-antihistamines, such as somnolence, fatigue, headache, impaired memory and learning, sedation, increased appetite, dry mouth, dry eyes, visual disturbances, constipation, urinary retention and erectile dysfunction.
3.Lack of effects between rupatadine 10 mg and placebo on actual driving performance of healthy volunteers.
Vuurman E1, Theunissen E, van Oers A, van Leeuwen C, Jolles J. Hum Psychopharmacol. 2007 Jul;22(5):289-97.
INTRODUCTION: Rupatadine fumarate is a potent, selective, histamine H(1)-receptor antagonist and PAF inhibitor with demonstrated efficacy for the relief of allergic rhinitis. Rupatadine does not easily cross the blood-brain barrier and is believed to be non-sedating at therapeutic doses. Consequently, rupatadine should show no impairment on car driving.
4.Fixed drug eruption against rupatadine fumarate.
Fidan V1, Fidan T. J Craniofac Surg. 2011 Sep;22(5):1682-3. doi: 10.1097/SCS.0b013e31822e5c76.
Second generation of antihistaminics have better therapeutic efficacy and more predictable pharmacological responses at lower doses than older compounds. However, new compounds have a reduced adverse reaction profile; clinicians can also encounter some unexpected adverse effects of these newer compounds. We report the first case of fixed drug eruption of rupatadine fumarate, which was confirmed by oral provocation test.
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Chemical Structure

CAS 158876-82-5 Rupatadine

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