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Journal ArticleDOI

Esterase Activities in the Blood, Liver and Intestine of Several Preclinical Species and Humans

Loren Berry, +2 more
- 31 Mar 2009 - 
- Vol. 3, Iss: 2, pp 70-77
TLDR
Substantial species differences in activity of these esterases were observed between the mouse, rat, dog monkey and human, and such species differences must be considered when using these preclinical species to optimize the pharmacokinetic properties of ester compounds intended for human use.
Abstract
Species and tissue differences in the activity of three major classes of esterases, carboxylesterase (CE), butyrylcholinesterase (BChE) and paraoxonase (PON), were studied. Substantial species differences in activity of these esterases were observed between the mouse, rat, dog monkey and human. Such species differences must be considered when using these preclinical species to optimize the pharmacokinetic properties of ester compounds intended for human use.

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Effective Application of Metabolite Profiling in Drug Design and Discovery

TL;DR: The value in structural elucidation is derived from its application to better design molecules, guide their clinical development and underwrite patient safety.
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Validation of an ultra-sensitive detection method for steroid esters in plasma for doping analysis using positive chemical ionization GC-MS/MS.

TL;DR: In this article, the sensitivity of gas chromatography coupled with a triple quadrupole with chemical ionization (GC-CI-MS/MS) was applied to detect trace levels of 10 testosterone and 2 nandrolone esters in plasma for in human doping analysis.
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Investigation into drug release from colon-specific azoreductase-activated steroid prodrugs using in-vitro models.

TL;DR: The aim of this study was to investigate drug release from a double steroid prodrug, OPN501, which incorporates a phenylpropionate linker, and its phenylacetate analogue, and to explain the divergent effects of the two compounds in anti‐inflammatory models.
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Esterase phenotyping in human liver in vitro: specificity of carboxylesterase inhibitors

TL;DR: The work was aimed at summarizing the selectivity of esterase inhibitors for carboxylesterases 1 and 2 in the human liver to clarify their suitability for ester enzyme phenotyping.
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Characterization of metabolites of GLS4 in humans using ultrahigh‐performance liquid chromatography/quadrupole time‐of‐flight mass spectrometry

TL;DR: The metabolites of GLS4 in humans were identified by the diagnostic ions of dihydropyrimidine and morpholine rings by comparing the accurate molecular masses, retention times and spectral patterns of the analytes with those of the parent drug.
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