Ebastine - CAS 90729-43-4
Catalog number:
90729-43-4
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C32H39NO2
Molecular Weight:
469.66
COA:
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Targets:
Histamine Receptor
Description:
Ebastine is a nonsedating type histamine H1-receptor antagonist.
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Purity:
>98%
MSDS:
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1.Determination of Some Non-sedating Antihistamines via Their Native Fluorescence and Derivation of Some Quantitative Fluorescence Intensity - Structure Relationships.
El-Kommos ME1, El-Gizawy SM1, Atia NN1, Hosny NM2. J Fluoresc. 2015 Nov;25(6):1695-709. doi: 10.1007/s10895-015-1656-4. Epub 2015 Oct 6.
A validated simple, novel, and rapid spectrofluorimetric method was developed for the determination of some non-sedating antihistamines (NSAs); namely cetirizine (CTZ), ebastine (EBS), fexofenadine (FXD), and loratadine (LOR). The method is based on measuring the native fluorescence of the cited drugs after protonation in acidic media and studying their quantitative fluorescence intensity - structure relationships. There was a linear relationship between the relative fluorescence intensity and the concentration of the investigated drug. Under the optimal conditions, the linear ranges of calibration curves for the determination of the studied NSAs were 0.10-2.0, 0.20-6.0, and 0.02-1.0 [Formula: see text] for (CTZ, FXD), (EBS), and (LOR); respectively. The factors affecting the protonation of the studied drugs were carefully studied and optimized. The method was validated according to ICH guidelines. The suggested method is applicable for the determination of the four investigated drugs in bulk and pharmaceutical dosage forms with excellent recoveries (97.
2.360 degree perspective on allergic rhinitis management in Italy: a survey of GPs, pharmacists and patients.
Canonica GW1, Triggiani M2, Senna G3. Clin Mol Allergy. 2015 Nov 2;13:25. doi: 10.1186/s12948-015-0029-5. eCollection 2015.
BACKGROUND: General practitioners (GPs), community pharmacists and allergic rhinitis (AR) patients in Italy were surveyed in order to gain insight from all three perspectives into the diagnosis, management and burden of AR in Italy.
3.A new marmoset P450 4F12 enzyme expressed in small intestines and livers efficiently metabolizes an anti-histaminic drug ebastine.
Uehara S1, Uno Y2, Yuki Y1, Inoue T3, Sasaki E3, Yamazaki H4. Drug Metab Dispos. 2016 Apr 4. pii: dmd.116.070367. [Epub ahead of print]
Common marmosets (Callithrix jacchus) are attracting attention as animal models in preclinical studies for drug development. However, cytochrome P450s (P450s), major drug-metabolizing enzymes, have not been fully identified and characterized in marmosets. In this study, based on the four novel P450 4F genes found on the marmoset genome, we successfully isolated P450 4F2, 4F3B, 4F11, and 4F12 cDNAs in marmoset livers. Deduced amino acid sequences of the four marmoset P450 4F forms exhibited high sequence identities (87-93%) to the human and cynomolgus monkey P450 4F homologues. Marmoset P450 4F3B and 4F11 mRNAs were predominantly expressed in livers, whereas marmoset P450 4F2 and 4F12 mRNAs were highly expressed in small intestines and livers. Four marmoset P450 4F proteins heterologously expressed in Escherichia coli catalyzed the ω-hydroxylation of leukotriene B4. Additionally, marmoset P450 4F12 effectively catalyzed the hydroxylation of anti-allergy drug ebastine, a human P450 2J/4F probe substrate.
4.A comparison of the intrasubject variation in drug exposure between generic and brand-name drugs: a retrospective analysis of replicate design trials.
Yu Y1,2, Teerenstra S2,3, Neef C1,4, Burger D5, Maliepaard M2. Br J Clin Pharmacol. 2016 Apr;81(4):667-78. doi: 10.1111/bcp.12828. Epub 2016 Jan 15.
AIMS: The aim of the present study was to investigate whether differences in total and peak drug exposure upon generic substitution are due to differences between formulations or to intrasubject pharmacokinetic variability of the active substance.
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CAS 90729-43-4 Ebastine

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