Preparation of phenylephrine 3-O-sulfate as the major in vivo metabolite of phenylephrine to facilitate its pharmacokinetic and metabolism studies.
Metabolite synthesis
Methods
Phenylephrine metabolism
Sulfation
Journal
Journal of pharmacological and toxicological methods
ISSN: 1873-488X
Titre abrégé: J Pharmacol Toxicol Methods
Pays: United States
ID NLM: 9206091
Informations de publication
Date de publication:
Historique:
received:
30
08
2018
revised:
21
11
2018
accepted:
24
11
2018
pubmed:
7
12
2018
medline:
20
3
2019
entrez:
4
12
2018
Statut:
ppublish
Résumé
The in vivo disposition and metabolism of phenylephrine have not been establishedby previous analytical methods and there is a lack of available standards for quantitating the metabolites. We pursued and compared the preparation of sulfation metabolites of phenylephrine and its ethyl analog etilefrine via chemical and bio-synthesis. Both sulfates were obtained in higher yield and purity through chemical syntheses compared to biosynthesis. A facile method for the production of phenylephrine 3-O-sulfate and etilefrine 3-O-sulfate was established. These compounds will be useful in the development of analytical assays for studying the pharmacokinetics of phenylephrine and its main route of metabolism in the presence of formulation changes and pharmacogenetic variation.
Identifiants
pubmed: 30502391
pii: S1056-8719(18)30702-0
doi: 10.1016/j.vascn.2018.11.009
pii:
doi:
Substances chimiques
Nasal Decongestants
0
Sulfates
0
Phenylephrine
1WS297W6MV
Etilefrine
ZB6F8MY53V
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
66-69Informations de copyright
Copyright © 2018 Elsevier Inc. All rights reserved.