GPCR large-amplitude dynamics by 19F-NMR of aprepitant bound to the neurokinin 1 receptor
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2122682119
Abstract: Significance G protein-coupled receptor (GPCR) structures determined by X-ray crystallography or cryo-electron microscopy include 28 receptors for which complexes with agonists and antagonists can be compared. In all these comparisons, an interatomic distance representing the… read more here.
Keywords: receptor gpcr; large amplitude; 19f nmr; aprepitant ... See more keywords
Simple Liquid Chromatography-Tandem Mass Spectrometry Method for Quantitation of Total and Free Aprepitant and its Active N-Dealkylated Metabolites in Human Plasma.
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DOI: 10.1097/ftd.0000000000000815
Abstract: BACKGROUND Aprepitant, an antiemetic selective neurokinin-1 receptor antagonist, is primarily metabolized to the active N-dealkylated (ND-AP) form and then converted to its carbonyl (ND-CAP) form in humans. This study developed simple liquid chromatography-tandem mass spectrometry… read more here.
Keywords: dealkylated metabolites; active dealkylated; aprepitant; total free ... See more keywords
Nanoparticle Engineering of Aprepitant Using Nano-by-Design (NbD) Approach
Sign Up to like & getrecommendations! Published in 2022 at "AAPS PharmSciTech"
DOI: 10.1208/s12249-022-02350-5
Abstract: The aim of this research was to develop a nanosuspension of aprepitant (APT) using the Nano-by-Design approach. A novel microfluidization technology was used for processing the formulation. A 32 full factorial design was used for… read more here.
Keywords: using nano; aprepitant; design; nano design ... See more keywords