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Merck
CN

E9531

Ebastine

≥98% (HPLC), Histamine H1 receptor antagonist, solid

Synonym(s):

1-[4-(1,1-Dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone

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About This Item

Empirical Formula (Hill Notation):
C32H39NO2
CAS Number:
90729-43-4
Molecular Weight:
469.66
UNSPSC Code:
12352200
PubChem Substance ID:
329799086
NACRES:
NA.77
MDL number:
MFCD00865661

Key Documents

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Product Name

Ebastine, ≥98% (HPLC), solid

SMILES string

CC(C)(C)c1ccc(cc1)C(=O)CCCN2CCC(CC2)OC(c3ccccc3)c4ccccc4

InChI key

MJJALKDDGIKVBE-UHFFFAOYSA-N

InChI

1S/C32H39NO2/c1-32(2,3)28-18-16-25(17-19-28)30(34)15-10-22-33-23-20-29(21-24-33)35-31(26-11-6-4-7-12-26)27-13-8-5-9-14-27/h4-9,11-14,16-19,29,31H,10,15,20-24H2,1-3H3

assay

≥98% (HPLC)

form

solid

color

white

solubility

DMSO: >10 mg/mL
H2O: insoluble

storage temp.

room temp

Quality Level

100

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Application

Ebastine has been used as a cationic amphiphilic drug (CAD) in sensitizing cancerous cells to chemotherapy and revert multidrug resistance.

Biochem/physiol Actions

Ebastine is a non-sedating histamine H1 receptor antagonist, which inhibits allergen-induced bronchospasm in conscious guinea pigs. Unlike other compounds in this category, ebastine does not prolong the QT interval at up to five times the recommended therapeutic dose.
Ebastine is a non-sedating histamine H1 receptor antagonist.

Features and Benefits

This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

General description

Ebastine is metabolised by cytochrome P450 3A (CYP3A4) to carebastine. It is used to treat allergic rhinitis and chronic idiopathic urticaria.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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Certificates of Analysis (COA)

Lot/Batch Number
0000382372
0000382372
0000194393
0000194393
0000066037

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Ji-Hong Shon et al.
Journal of clinical pharmacology, 50(2), 195-204 (2009-10-21)
The present study was performed to elucidate the effects of itraconazole and rifampin on the pharmacokinetics and pharmacodynamics of ebastine, a nonsedative H1 receptor antagonist. In a 3-way crossover sequential design with 2-week washouts, 10 healthy participants were pretreated with
Piperidine-Based Drug Discovery (2017)
Alexander H Schmidt et al.
Journal of pharmaceutical and biomedical analysis, 78-79, 65-74 (2013-03-05)
A stability-indicating ultra high performance liquid chromatographic (UHPLC) method has been developed for purity testing of ebastine and its pharmaceutical formulations. Successful chromatographic separation of the API from impurities was achieved on a Waters Acquity UPLC BEH C18, 50 mm
Yong Ju Jang et al.
Auris, nasus, larynx, 39(2), 175-179 (2011-05-17)
Maxillary sinus hypoplasia (MSH) is a radiologically detectable abnormality of the maxillary sinus that can be associated with sinusitis. Symptomatic MSH patients with a patent ostiomeatal complex (MSHPO) constitute a particular therapeutic challenge. Ostiomeatal unit CT scans of 1293 patients
M Magerl et al.
Clinical and experimental dermatology, 34(5), e137-e140 (2009-03-28)
In dermographic urticaria (DU), shearing forces on the skin result in weals and itching. Second-generation antihistamines are recommended as the first-line treatment, but to date only a few have ever been tested for this condition. The objective of this pilot
View All Related Papers

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