scholarly journals Toxicokinetics and analytical toxicology of the abused opioid U‐48800 — in vitro metabolism, metabolic stability, isozyme mapping, and plasma protein binding

2019 ◽  
Vol 11 (10) ◽  
pp. 1572-1580 ◽  
Author(s):  
Tanja M. Gampfer ◽  
Lilian H.J. Richter ◽  
Jan Schäper ◽  
Lea Wagmann ◽  
Markus R. Meyer
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Metabolic Stability ◽  
In Vitro Metabolism ◽  
Analytical Toxicology

Evaluation of oral pharmacokinetics, in vitro metabolism, blood partitioning and plasma protein binding of novel antidiabetic agent, S009-0629 in rats

2018 ◽  
Vol 79 (4) ◽  
pp. 173-183 ◽  
Author(s):  
Guru Raghavendra Valicherla ◽  
Kishan Shamjibhai Italiya ◽  
Chandra Prakash Gupta ◽  
Shachi Mishra ◽  
Mohammed Riyazuddin ◽  
...  
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
In Vitro Metabolism ◽  
Antidiabetic Agent ◽  
Oral Pharmacokinetics

scholarly journals Pharmacokinetic properties, in vitro metabolism and plasma protein binding of govaniadine an alkaloid isolated from Corydalis govaniana Wall

2016 ◽  
Vol 131 ◽  
pp. 464-472 ◽  
Author(s):  
Lucas M.M. Marques ◽  
Daniel R. Callejon ◽  
Larissa G. Pinto ◽  
Michel L. de Campos ◽  
Anderson R.M. de Oliveira ◽  
...  
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
In Vitro Metabolism ◽  
Pharmacokinetic Properties

Toxicokinetic Studies and Analytical Toxicology of the New Synthetic Opioids Cyclopentanoyl-Fentanyl and Tetrahydrofuranoyl-Fentanyl

2020 ◽  
Vol 44 (5) ◽  
pp. 449-460 ◽  
Author(s):  
Tanja M Gampfer ◽  
Lea Wagmann ◽  
Matthias J Richter ◽  
Svenja Fischmann ◽  
Folker Westphal ◽  
...  
Keyword(s):  
Protein Binding ◽  
Phase I ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
New Psychoactive Substances ◽  
Analytical Toxicology ◽  
Rat Urine ◽  
Analytical Strategy ◽  
Synthetic Opioids

Abstract The growing number of new synthetic opioids (NSO) on the new psychoactive substances (NPS) market bears new challenges in toxicology. As their toxicodynamics and particularly their toxicokinetics are usually unknown, impact on human health is not yet fully understood. Detection of the 2 NSO cyclopentanoyl-fentanyl (CP-F) and tetrahydrofuranoyl-fentanyl (THF-F) was first reported in 2016. Both were involved in several fatal intoxication cases, but no detailed information about their toxicological characteristics is available so far. The main purpose of this study was therefore to investigate the in vitro toxicokinetics and in vivo analytical toxicology of CP-F and THF-F by means of liquid chromatography high-resolution tandem mass spectrometry (LC-HRMS/MS). These studies included metabolic stability, phase I and II metabolism, isozyme mapping, plasma protein binding and detectability in LC-HRMS/MS standard urine screening approaches (SUSA) using rat urine samples. In total, 12 phase I metabolites of CP-F and 13 of THF-F were identified, among them 9 metabolites described for the first time. Overall, N-dealkylations, hydroxylations and dihydroxylations were the main metabolic reactions. The cytochrome P450 (CYP) isozymes mainly involved were CYP2D6 and CYP3A4, leading to elevated drug levels and intoxications in CYP2D6 poor metabolizers. CP-F showed a high plasma protein binding of 99%, which may increase the risk of toxicity by simultaneous intake of other highly bound drugs. Detectability studies showed that neither the parent compounds nor their metabolites were detectable in rat urine using LC-HRMS/MS SUSA. However, a more sophisticated analytical strategy was successfully applied and should be used for analytical confirmation of an intake of CP-F and/or THF-F.

scholarly journals Metabolism and plasma protein binding of 16 straight- and branched-chain parabens in in vitro liver and skin models

2020 ◽  
pp. 105051
Author(s):  
Cathy Lester ◽  
Nicola J. Hewitt ◽  
Ursula Müller-Vieira ◽  
Manuela Mayer ◽  
Corie Ellison ◽  
...  
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Branched Chain
Sign in / Sign up

Export Citation Format

Share Document