Results 71 to 80 of about 2,738,308 (324)

In Vitro Metabolism and In Vivo Pharmacokinetics Profiles of Hydroxy-α-Sanshool

open access: yesToxics
Hydroxy-α-sanshool (HAS) is the predominant active compound in Zanthoxylum bungeanum Maxim (ZBM). Our present work was aimed to explore the in vitro metabolism characteristics, and in vivo pharmacokinetic (PK) profile of HAS.
Jie Meng   +4 more
doaj   +1 more source

Intrinsic Clearance in Liver Microsomes.

open access: yes, 2016
Intrinsic Clearance in Liver Microsomes.
William DeMaio (3111543)   +8 more
core   +1 more source

Monitoring pharmacodynamic and molecular drug targets in liquid biopsy: Exploratory study in liver cancer with modelling of EGFR Receptor engagement

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Abstract Aim Liquid biopsy is minimally invasive (compared with tissue biopsy) and has previously been used to generate systems data regarding drug elimination via hepatic enzymes and transporters. This study extends quantitative assessment of systems parameters in liquid biopsy to pharmacodynamic (PD) and disease markers relevant to cancer development
Zubida M. Al‐Majdoub   +3 more
wiley   +1 more source

Analysis of in vitro and in vivo metabolism of zidovudine and gemfibrozil in trans‐chromosomic mouse line expressing human UGT2 enzymes

open access: yesPharmacology Research & Perspectives, 2022
UDP‐glucuronosyltransferases (UGTs) catalyze the conjugation of various substrates with sugars. Since the UGT2 family forms a large cluster spanning 1.5 Mb, transgenic mouse lines carrying the entire human UGT2 family have not been constructed because of
Kaoru Kobayashi   +9 more
doaj   +1 more source

The integrated Lei‐CNS PBPK‐PD model effectively predicts clozapine brain disposition and D2 receptor occupancy in humans

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Aim Clozapine, used for treatment‐resistant schizophrenia, has a narrow therapeutic window and highly variable plasma pharmacokinetics (PK), necessitating careful monitoring. Direct measurement of unbound brain PK in humans is unethical. To develop a physiologically based pharmacokinetic–pharmacodynamic (PBPK‐PD) model to predict clozapine brain ...
Mengxu Zhang   +3 more
wiley   +1 more source

Assay for the terminal enzyme of the stearoyl coenzyme A desaturase system using chick embryo liver microsomes

open access: yesJournal of Lipid Research, 1977
The NADH-dependent stearoyl CoA desaturase of hepatic microsomes (EC 1.14.99.5) is an enzyme system consisting of cytochrome b5 reductase (EC 1.6.2.2), cytochrome b5, and the terminal desaturase. We have developed a simple method for routine assay of the
V C Joshi, A C Wilson, S J Wakil
doaj   +1 more source

In vivo effect of dried chicory root (Cichorium intybus L.) on xenobiotica metabolising cytochrome P450 enzymes in porcine liver [PDF]

open access: yes, 2011
Cytochrome P450 (CYP) enzymes are widely studied for their involvement in metabolism of drugs and endogenous compounds. In porcine liver, CYP1A2,2Aand 2E1 are important for the metabolism of skatole.Feeding chicory roots to pigs is known to decrease the ...
Martin Krøyer Rasmussen   +7 more
core   +1 more source

Histamine and the mechanisms of nausea and vomiting: Translating the uncertain pharmacology of cyclizine

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Abstract Cyclizine is a long‐established, short‐acting drug, registered for preventing motion sickness, post‐operative nausea and vomiting (PONV) and ‘vomiting of known cause’. The latter is not defined but may include pregnancy and patients receiving palliative care, historically accepted without large, controlled trials.
Gareth J. Sanger, Paul L. R. Andrews
wiley   +1 more source

Activation of HMG-CoA reductase by microsomal phosphatase

open access: yesJournal of Lipid Research, 1983
HMG-CoA reductase activity can be modulated by a reversible phosphorylation-dephosphorylation with the phosphorylated form of the enzyme being inactive and the dephosphorylated form, active. Phosphatases from diverse sources, including cytosol, have been
K R Feingold   +4 more
doaj   +1 more source

The Korea Chemical Bank: Over 25 years of national chemical infrastructure alongside KRICT's 50‐year journey

open access: yesBulletin of the Korean Chemical Society, EarlyView.
This graphic abstract illustrates the role of the Korea Chemical Bank (KCB) as a central national hub that integrates government R&D, academic compound deposits, and industrial drug discovery throughout the latter half of KRICT's 50‐year history. Abstract Since its establishment in 2000 under the Korea Research Institute of Chemical Technology (KRICT),
Seul‐Gee Hwang   +18 more
wiley   +1 more source

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