Ebastine-d5 (CAS 1216953-13-7)
QUICK LINKS
A nonsedating type histamine H1-receptor antagonist. Ebastine-d5 serves as an internal standard for quantifying ebastine via GC- or LC-MS. Ebastine, a potent second-generation histamine H1 receptor antagonist (IC50 = 45 nM), remains isolated from the brain due to its inability to cross the blood-brain barrier. It extensively undergoes first-pass metabolism by hepatic cytochrome P450 3A4, transforming into its active carboxylic acid metabolite, carebastine, responsible for most of its pharmacological effects. Ebastine, at a concentration of 10 μM, exhibits inhibition of T cell proliferation and the production of Th2-type pro-inflammatory cytokines by macrophages. The synthesis of Ebastine-d5 involves a multi-step process, primarily centered on the deuteration of the starting material, which can be accomplished through various methods, replacing five hydrogen atoms with deuterium atoms.
Ebastine-d5 (CAS 1216953-13-7) References
- Method development and validation for simultaneous determination of ebastine and its active metabolite carebastine in human plasma by liquid chromatography-tandem mass spectrometry and its application to a clinical pharmacokinetic study in healthy Chinese volunteers. | Phiri, M., et al. 2020. Biomed Chromatogr. 34: e4904. PMID: 32449558
- A 'Dilute and Shoot' Liquid Chromatography-Mass Spectrometry Method for Multiclass Drug Analysis in Pre-Cut Dried Blood Spots. | Mainero Rocca, L., et al. 2021. Int J Environ Res Public Health. 18: PMID: 33809736
- Direct multiclass desorption electrospray ionization-tandem mass spectrometry method for the analysis of sleep inducers and ototoxic drugs in dried blood spots. | Mainero Rocca, L., et al. 2022. Rapid Commun Mass Spectrom. 36: e9265. PMID: 35128730
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Ebastine-d5, 1 mg | sc-218295 | 1 mg | $302.00 |