 Home > Encyclopedia > Ebastine

Ebastine

Ebastine structure

CAS No:
90729-43-4
Formula:
C32H39NO2
Chemical Name:
Ebastine
Synonyms:
1-Butanone,1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-;1-[4-(1,1-Dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone;Ebastine;Ebastin;LAS-W 090;Ebastel;RP 64305;Bastel;Kestine;Erostin
Categories:
Active Pharmaceutical Ingredients > Antiallergic Drugs

Description

Ebastine(LAS-W 090;RP64305) is a long-acting and selective H1-histamine receptor antagonist.Target: Histamine H1 ReceptorEbastine is a H1 antihistamine with low potential for causing drowsiness. Ebastine (10 mg orally) causes brain histamine H1-receptor occupation of approximately 10%, consistent with its lower incidence of sedative effect, whereas (+)-chlorpheniramine occupied about 50% of brain H1-receptors even at a low but sedative dose of 2 mg; occupancy of (+)-chlorpheniramine was

Ebastine is an organic molecular entity.|Ebastine is under investigation for the treatment of Irritable Bowel Syndrome (IBS). Ebastine has been investigated for the treatment of Urticaria.

Ebastine Basic Attributes

Molecular Weight：

469.66

Exact Mass：

469.66

EC Number：

1806241-263-5

UNII：

TQD7Q784P1

DSSTox ID：

DTXSID6046472

ATC Code：

R06AX22|R - Respiratory system

Characteristics

PSA：

29.5

XLogP3：

7.2

Appearance：

white

Density：

1.1±0.1 g/cm3

Melting Point：

80-82°C

Boiling Point：

596.3°C at 760 mmHg

Flash Point：

314.5±30.1 °C

Refractive Index：

1.590

Water Solubility：

Slightly soluble in chloroform, methanol.

Storage Conditions：

room temp

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

RTECS Number：

EL8140000

Precautionary statement(s)：

P273, P501

Hazard Statements：

H413

GHS Classification：

H413 (97.5%): May cause long lasting harmful effects to aquatic life [Hazardous to the aquatic environment, long-term hazard]|P273, and P501|Aggregated GHS information provided by 40 companies from 2 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)

Metabolism/Metabolites：

Ebastine has known human metabolites that include 4-(4-tert-butylphenyl)-4-oxobutanal and Deslakylebastine.

MeSH Entry Terms：

4-diphenylmethoxy-1-(3-(4-tert-butylbenzoyl)propyl)piperidine

Ebastine Use and Manufacturing

Methods of Manufacturing

Alkylation of 4-piperidinol with compound (I) yields compound (II). Then use benzhydryl bromide for alkylation to obtain ebastine.

Uses

A nonsedating type histamine H1-receptor antagonist. Its antihistamine activity is competitive at low concentrations and non-competitive at high concentrations. It is used for allergic diseases, including allergic rhinitis in children, perennial rhinitis in adults, seasonal rhinitis, hay fever and chronic urticaria. Used as an anti-histamine

Computed Properties

Molecular Weight:469.7
XLogP3:7.2
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:10
Exact Mass:469.298079487
Monoisotopic Mass:469.298079487
Topological Polar Surface Area:29.5
Heavy Atom Count:35
Complexity:594
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Ebastine is a histamine H1 receptor antagonist. This product is metabolized to carbastine in the body, which has a selective antagonistic effect on histamine H1 receptors and can inhibit the release of histamine. Its H1 receptor antagonism and anticholinergic effects on the central nervous system are very weak.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Ebastine Tablets
Ingredients	Main ingredient: Ebastine.
Indication	Erythromycin can increase the plasma concentration of carbastine, a metabolite of this product, by 2 times.

Ebastine Tablets
Ingredients	The main ingredient of this product is Ebastine. Its chemical name is: 4'-tert-butyl-4[4-(diphenylmethoxy)piperidinyl]propylphenyl ketone.
Indication	Erythromycin can increase the plasma concentration of carbastine, a metabolite of this product, by 2 times.
Specifications	10mg
Manufacturer	Hangzhou Qianyuan Baoling Pharmaceutical Co., Ltd.

Ebastine Tablets
Ingredients	Main ingredient: Ebastine.
Indication	Erythromycin can increase the plasma concentration of carbastine, a metabolite of this product, by 2 times.
Specifications	10mg
Manufacturer	Jiangsu Lianhuan Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

Polaris AI Pharma Corp.

South Korea
Active
China CHINO PHARMA Ltd

China
Active
Jiangsu Sinobiopharma Co., Ltd.

China
Active

See More Registered Holders

Recommended Suppliers of Ebastine

Hangzhou Dawn Ray Pharmaceutical Co.,Ltd Contact Supplier

CN
5 YRS

Business licensed Certified factory

Manufactory Supplier of D-Biotin,Tobramycin base,L(-)-Carnitine base,Polymyxin B sulfate USP,Kanamycin sulfate monohydrate,Finasteride 99% USP

Ebastine China manufacture 98%min

CAS No.: 90729-43-4

Inquiry
HANGZHOU LEAP CHEM CO., LTD. Contact Supplier

CN
5 YRS

Business licensed

Trader Supplier of Intermediates,Building blocks,API,Silicones,Peptides,Lab chemicals,Biochemicals,Pharmaceuticals,Screening Compounds,Food Additives

Ebastine

CAS No.: 90729-43-4

Content: 99.00%

Inquiry
Shandong Airuike Chemical Co., Ltd. Contact Supplier

CN
3 YRS

Business licensed

Trader Supplier of api,Intermediates,Organic Chemistry,Inorganic Chemistry,Daily Chemicals,Cosmetic Raw Materals,CATALYST AND AUXILIARY,FLAVORS AND FRAGRANCES,Chemical Pesticides,ADDITIVE

Ebastine CAS 90729-43-4

CAS No.: 90729-43-4

Grade: Pharmaceutical Grade

Content: 99%

Inquiry
Hubei KDG Web Science&Technology Co.,Ltd Contact Supplier

CN
2 YRS

Business licensed

Trader Supplier of Peptide,API,HCG,Amino Acids,Plant Extract,Vitamin

High Quality Competitive Price Ebastine CAS 90729-43-4

CAS No.: 90729-43-4

Grade: Pharmaceutical Grade

Content: 99%

Inquiry