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E9531

Ebastine

Name: Ebastine
Brand: SIGMA

≥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

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

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Product Name

Ebastine, ≥98% (HPLC), solid

Quality Level

100

assay

≥98% (HPLC)

form

solid

color

white

solubility

DMSO: >10 mg/mL, H₂O: insoluble

storage temp.

room temp

SMILES string

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

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

InChI key

MJJALKDDGIKVBE-UHFFFAOYSA-N

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Related Categories

Bioactive Small Molecules

General description

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

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 H₁receptor 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.

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

0000536028

0000382372

0000194393

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Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.

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

Histamine H(1) antagonist treatment with pyrilamine reduces nicotine self-administration in rats.

Edward D Levin et al.

European journal of pharmacology, 650(1), 256-260 (2010-10-19)

Nicotine has been definitively shown to be critically involved in the neural bases of tobacco addiction. However, nicotine releases a wide variety of neurotransmitters. Nicotine-induced dopamine release has been shown to play a key role in facilitating nicotine self-administration. Other

Myocardial pharmacokinetics of ebastine, a substrate for cytochrome P450 2J, in rat isolated heart.

W Kang et al.

British journal of pharmacology, 163(8), 1733-1739 (2011-03-18)

It is well established that cytochrome P450 2J (CYP2J) enzymes are expressed preferentially in the heart, and that ebastine is a substrate for CYP2J, but it is not known whether ebastine is metabolized in myocardium. Therefore, we investigated its pharmacokinetics

Maxillary sinus hypoplasia with a patent ostiomeatal complex: A therapeutic dilemma.

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

Piperidine-Based Drug Discovery (2017)

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Global Trade Item Number

SKU	GTIN
E9531-10MG	04061832071992
E9531-50MG	04061832072005

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