Could NAPQI Contribute to Paracetamol Analgesia? Redox Modulation of Kv7 Ion Channels
ABSTRACT Paracetamol (acetaminophen, APAP) is one of the most widely used analgesic and antipyretic drugs worldwide, yet its mechanism of action remains incompletely understood. While several pathways have been proposed, including cyclooxygenase inhibition and endocannabinoid modulation via AM404, none fully account for its pharmacological profile. The
Sara M‐Alicante +6 more
wiley +1 more source
Medications That Regulate Pregnane X Receptor: A Systematic Review of Current Evidence
PRISMA 2020 flow diagram of study selection for this systematic review of medications that regulate the pregnane X receptor (PXR), from 12 236 records screened to 101 included studies. ABSTRACT The pregnane X receptor (PXR) gene encodes a ligand‐activated protein involved with the metabolism and excretion of drugs, toxins, and other xenobiotics.
Petra Czarniak +4 more
wiley +1 more source
ABSTRACT Malaria remains a major global health challenge, with an urgent need for new therapies to combat the evolving resistance to anti‐malarial treatments. Physiologically‐based pharmacokinetic (PBPK) modeling offers a promising approach to accurately predict PK, optimize dosing strategies, reduce development time and cost, and de‐risk the ...
Junjie Ding +3 more
wiley +1 more source
Mitochondria‐Targeting Moieties Based on N‐Tethered Pyridinium Cations
Pyridinium cations were benchmarked as mitochondria‐targeting moieties in a panel of N‐tethered fluorescent‐, bioactive‐, and inert‐cargo conjugates. 3,5‐Diphenylpyridinium (DPPy+) is a competent triphenylphosphonium (TPP+) surrogate, combining high mitochondria‐targeting efficiency with lower intrinsic effects on mitochondrial function.
Ivan Džajić +27 more
wiley +2 more sources
DDIapp—A Web‐Based Application for Static Drug–Drug Interaction Assessment
ABSTRACT In this work we describe the development of a web‐based application for static drug–drug interaction (DDI) risk assessment in accordance with the International Council for Harmonization (ICH) M12 guidance. The app was built using the Shiny for Python framework and it employs a modular mathematical modeling structure that incorporates models ...
Hirotaka Watase +5 more
wiley +1 more source
Cytochrome P450-Mediated Metabolism of Antimycobacterial <i>N</i>α-Aroyl-<i>N</i>-aryl-phenylalanine Amides. [PDF]
Doering J +13 more
europepmc +1 more source
Safety Evaluation of an Aqueous Root and Leaf Extract of Ashwagandha ( Withania somnifera )
Sensoril, an aqueous root and leaf extract of ashwagandha showed no evidence of mutagenicity in the in vitro Ames assay, was negative in the in vitro micronucleus, in vivo mammalian bone marrow chromosome aberration assays, and was well tolerated in the rat at up to 4000 mg/kg BW/day when administered orally for a period of 90 days. The data from these
Mukesh Summan +2 more
wiley +1 more source
Cross-Species Hepatic Metabolism of the Antileishmanial Chalcone NAT22 Generates Metabolites with Predicted Enhanced Affinity for the Parasite Target cTXNPx. [PDF]
Barreto ARR +11 more
europepmc +1 more source
This work highlights the satisfactory pharmacokinetic profile of two benzenesulfonylpiperazine lead candidates, followed by in vivo assessment in a murine model of visceral leishmaniasis. This assessment identified compound 2 as moderately active at a lower dose, but its efficacy increased at higher doses, though with concerns regarding safety.
Thibault Joseph William Jacques Dit Lapierre +13 more
wiley +1 more source
Stereoselective Biotransformation: Transfer of Learning to Advance Drug Metabolism and Biocatalysis. [PDF]
Okunlola GA, Aleku GA.
europepmc +1 more source

