Ebastinum

Ebastinum - Names and Identifiers

Name	Ebastine
Synonyms	Ebastel Kestine Ebastine Ebastina RP 64305 LAS W-090 Ebastinum UNII-TQD7Q784P1 Ebastinum [Latin] Ebastina [Spanish] 4'-tert-Butyl-4-(4-(diphenylmethoxy)piperidino)butyrophenone 4-Diphenylmethoxy-1-(3-(4-tert-butylbenzoyl)propyl)piperidine 1-(4-tert-butylphenyl)-4-[4-(diphenylmethoxy)piperidin-1-yl]butan-1-one 1-(4-(1,1-Dimethylethyl)phenyl)-4-(4-(diphenylmethoxy)-1-piperidinyl)-1-butanone 1-Butanone, 1-(4-(1,1-dimethylethyl)phenyl)-4-(4-(diphenylmethoxy)-1-piperidinyl)-
CAS	90729-43-4
InChI	InChI=1/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

Ebastinum - Physico-chemical Properties

Molecular Formula	C32H39NO2
Molar Mass	469.67
Density	1.09g/cm³
Melting Point	80-82℃
Boling Point	596.3°C at 760 mmHg
Flash Point	314.5°C
Solubility	Slightly soluble in chloroform, methanol.
Vapor Presure	3.47E-14mmHg at 25°C
Appearance	solid
Color	white
pKa	8.19±0.10(Predicted)
Storage Condition	2-8°C
Refractive Index	1.59
Physical and Chemical Properties	White crystalline powder.
Use	Used as an anti-amine drugTherapeutic category : Anti-allergic agent

Ebastinum - Risk and Safety

WGK Germany	3
RTECS	EL8140000

Ebastinum - Introduction

Antihistamines

Antihistamines are a class of drugs that can compete with histamine for histamine receptors on cells, so that histamine cannot bind to the receptor, thereby producing antihistamines. According to different types of histamine receptors, antihistamines can be divided into two types: H1 receptor blockers and H2 receptor blockers. H1 receptor blockers are commonly referred to as antihistamines in the past, which can antagonize histamine's vasodilation and smooth muscle contraction effects, helps relieve or eliminate allergic symptoms caused by endogenous histamine release. Mainly used to prevent and treat skin and mucous membrane allergic diseases, motion sickness and vomiting.
Ebastine and cetirizine hydrochloride, loratadine, levocetirizine, and mizolastine are currently commonly used anti-H1 receptor antihistamines without sedation, which are anti-allergic drugs. It is characterized by no sedative effect or little sedative effect on the central nervous system, and the antihistamine effect is stronger, which can significantly inhibit the red halo and wind mass caused by histamine, and does not affect the release of histamine by mast cells.
This product takes effect 1~4 hours after oral administration, and the peak time of blood drug concentration is 3~6 hours. It can pass through the blood-brain barrier, and it is converted into the active form of Carestine (carebastine) in the body. After one po ebastine in healthy adult volunteers, Tmax is about 3~6 h and 3~5 times/d to reach a stable state. Cmax after a single dose of 10 mg is approximately 0.1mg/L. Taking it at the same time as food can increase its bioavailability. PPB is about 98%. Vd is about 90~140 L. The terminal T1/2 is 13~16h, which is mainly excreted from urine.
Clinical treatment of various allergic diseases, such as chronic idiopathic urticaria, seasonal, perennial allergic rhinitis, skin pruritus. Adults are treated with chronic urticaria or allergic rhinitis, po,10 mg,qd; The dosage for children is 5 mg,qd. High-dose ebastine 20 mg,qd is only used in adults with more severe allergic diseases, and it will achieve better curative effect when taken in the morning.
The most common adverse reactions were drowsiness, headache, and dry mouth. Most patients had mild to moderate reactions, which did not affect continued medication. Other rare adverse reactions include fatigue, nausea, vomiting, hyperappetite, diarrhea, constipation and restlessness. For more than 1 year, the most common adverse reactions were headache and gastrointestinal disorders.

Biological activity

Ebastine is a powerful H1 histidine receptor (H1-histamine receptor) antagonist, which is used to treat allergic diseases.

Target
Target Value
Histamine H1 receptor

In vitro studies

In guinea pig ventricular myocytes, the concentration of Ebastine inhibits I(Kr) in a voltage-independent manner when it approximates the concentration found in plasma under certain conditions (Kd = 0.14 μM, the maximum inhibition is 74%), which is more effective than slow Delayed rectified potassium current (I(Ks)) (Kd = 0.8 μM, the maximum inhibition is 60%). Ebastine also inhibited hERG to express IKr of Xenopus laevis oocytes with a Kd value of 0.3 μM and a maximum inhibition rate of 46% at 3 μM. Ebastine has a slight effect on the transient potassium current in rats at a concentration of less than 100 nM. In human nasal polyp cells, Ebastine inhibited anti-IgE-induced prostaglandin D2(PGD2) and leukotriene C4/D4 release, IC30 was 2.57 μM and 9.6 μM, respectively, and inhibited cytokine release. Ebastine is a new histamine H1 receptor antagonist, which has the characteristics of fast onset (rapid absorption) and long duration (slow elimination), at least partly through the formation of an acidic metabolite (carebastine), which makes it a more effective antihistamine. Ebastine have minimal activity against acetylcholine (upper secretion and visual regulation have no effect like atropine), and their ability to penetrate the blood-brain barrier (without the adverse effects of sedation) is not strong. Even under high dose conditions, Ebastine has no effect on the central nervous system and cardiovascular system, and has no interaction with other potential concomitant drugs. Compared with the H2 receptor, Ebastine shows selectivity to histamine H1, has moderate activity against other potential allergic phenomena, such as leukotriene C4 and platelet activating factor, and is a potent antigen for allergic reactions produced by appropriate sensitized tissue or animal contact.

Chemical properties

ebastine fumarate (Ebastine Fumarate):C32H39NO2?C4H4O4. Crystallized from ethanol, melting point 197-198 ℃. Acute toxicity LD50 rodents (mg/kg):500 intraperitoneal injection;>4000 oral administration.
Use

Its antihistamine activity is competitive at low concentrations and non-competitive at high concentrations. For allergic diseases, including allergic rhinitis in children, year-round rhinitis in adults, seasonal rhinitis, hay fever and chronic urticaria.

Uses

used as anti-blocking amine drug Therapeutic category : Anti-allergic agent

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

Last Update：2024-04-10 22:29:15

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Product Name: Ebastine Request for quotation
CAS: 90729-43-4
Tel: 0086-551-65418684
Email: sales@tnjchem.com
　　　　 info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840

Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog

Shanghai Yuanye Bio-Technology Co., Ltd.

Spot supply

Wechat: 18301782025

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Ebastinum

Ebastinum

Ebastine

CAS: 90729-43-4

Molecular Formula: C32H39NO2

Ebastinum - Names and Identifiers

Ebastinum - Physico-chemical Properties

Ebastinum - Risk and Safety

Ebastinum - Introduction

Supplier List

Ebastinum Request for Quotation

Ebastine

CAS: 90729-43-4

Molecular Formula: C32H39NO2

Ebastinum - Names and Identifiers

Ebastinum - Physico-chemical Properties

Ebastinum - Risk and Safety

Ebastinum - Introduction

Supplier List

Ebastinum