The Effects of Pregnenolone 16α-Carbonitrile Dosing on Digoxin Pharmacokinetics and Intestinal Absorption in the Rat [PDF]
The effect of Pgp induction in rats by pregnenolone 16α-carbonitrile (PCN) (3 days, 35 mg/kg/d, p.o.) on digoxin pharmacokinetics and intestinal transport has been assessed.
Anna-Lena Ungell +12 more
core +2 more sources
The pregnane X receptor: from bench to bedside [PDF]
The pregnane X receptor (PXR; NR1I2), a member of the nuclear receptor superfamily, regulates the expression of metabolic enzymes and transporters involved in the response of mammals to their chemical environment.To summarize the functions and clinical implications of PXR.In the current review, the clinical implications of PXR are discussed, and the ...
Xiaochao, Ma +2 more
openaire +2 more sources
Prenatal dexamethasone exposure (PDE) persistently upregulates hepatic CYP3A1/CYP2B1 in offspring via glucocorticoid receptor (GR) activation. In vivo and in vitro studies show GR promotes P300/CBP binding to the constitutive androstane receptor (CAR) promoter, sustaining histone acetylation (H3K9/K27ac) and enhancing CYP expression. The GR–CAR pathway
Xiaoxiang Sun +9 more
wiley +1 more source
Differential effects of clinically used derivatives and metabolites of artemisinin in the activation of constitutive androstane receptor isoforms [PDF]
BACKGROUND AND PURPOSE Widespread resistance to antimalarial drugs requires combination therapies with increasing risk of pharmacokinetic drugdrug interactions.
Alexander +51 more
core +1 more source
Prioritising research on endocrine disruption in the marine environment: a global perspective
ABSTRACT A healthy ocean is a crucial life support system that regulates the global climate, is a source of oxygen and supports major economic activities. A vast and understudied biodiversity from micro‐ to macro‐organisms is integral to ocean health.
Patricia I. S. Pinto +23 more
wiley +1 more source
ABSTRACT Sex plays a key role in shaping both anti‐cancer immunity and autoimmunity. Biological factors underlying sexual dimorphism have now been identified in multiple aspects of anti‐cancer immunity and autoimmunity. These factors include sex differences in hormone levels, chromosome complement, and expression of the long non‐coding RNA XIST.
Christian G. Bustillos +4 more
wiley +1 more source
Summary: Here, we describe an optimized protocol to identify specific nuclear receptor ligands. First, to rule out any compound interference with luciferase activity per se, we describe an in vitro assay assessing potential inhibition or activation of ...
Alexandre Berthier +2 more
doaj +1 more source
Functional constraints on the constitutive androstane receptor inferred from human sequence variation and cross-species comparisons [PDF]
Members of the NR1I subfamily of nuclear receptors play a role in the transcriptional activation of genes involved in drug metabolism and transport. NR1I3, the constitutive androstane receptor (CAR), mediates the induction of several genes involved in ...
Di Rienzo Anna +3 more
core +2 more sources
Efavirenz and CYP2C9 Genetic Polymorphisms Reduce CYP2C9 Activity in Healthy Participants
ABSTRACT Efavirenz's effects on cytochrome P450 2C9 (CYP2C9) activity have not been formally characterized in vivo. We conducted the first clinical drug–drug interaction (DDI) study to test the effect of chronic efavirenz dosing on CYP2C9 activity, using tolbutamide as a selective probe.
Jason D. Kim +4 more
wiley +1 more source
Pharmacological effect of one icv dose of Allopregnanolone in female rat: behavioural profile [PDF]
We have previously observed that intracerebroventricular allopregnanolone (ALLO) injection produced an anxiolytic effect and inhibited sexual receptivity when the test was performed in a separate manner. Also, ALLO reverts learning deficit in female rats
Cabrera Kreiker, Ricardo Jorge +5 more
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