Results 71 to 80 of about 42,461 (214)

Histone deacetylase inhibitors as venetoclax‐sensitising partners in acute myeloid leukaemia: Mechanisms, pharmacology and translational perspectives

British Journal of Pharmacology, EarlyView.
Abstract Venetoclax combined with hypomethylating agents has improved treatment for older or unfit patients with acute myeloid leukaemia (AML), but resistance and relapse remain common. This review analyses the rationale for combining venetoclax with inhibitors of histone deacetylase (HDAC).
Jaebok Lee, Marc Diederich
wiley   +1 more source

The Effect of Uridine Diphosphate‐Glucuronosyltransferase Inhibition on the Pharmacokinetics of Ecopipam and Its Metabolites

Clinical and Translational Science
Ecopipam, a selective dopamine D1 receptor antagonist in development for Tourette syndrome, is primarily converted by uridine diphosphate‐glucuronosyltransferase (UGT)1A9 to ecopipam glucuronide, with a minor metabolic pathway by cytochrome P450 3A4 ...
Virginia D. Schmith, Danielle Graden, Joy Schleyer, Stephen P. Wanaski   +3 more
doaj   +1 more source

A Review of Nonsteroidal Anti‐Inflammatory Drugs for Food‐Producing Animals With a Focus on Potential Applications for Farmed Finfish

Journal of Fish Diseases, EarlyView.
ABSTRACT In finfish aquaculture, there are several inflammatory diseases impacting productivity and animal welfare, however there are limited options available to veterinarians to treat inflammation and pain in fish. Nonsteroidal anti‐inflammatory drugs (NSAIDs) are widely used in terrestrial animals raised for human consumption to treat a range of ...
Chloe J. English, Christine Huynh, William Roy, James W. Wynne, Hamish Rodger   +4 more
wiley   +1 more source

Lipid-based nanosystem of edaravone: development, optimization, characterization and in vitro/in vivo evaluation

Drug Delivery, 2017
Edaravone (EDR) is a well-recognized lipophilic free radical scavenger for diseases including neurodegenerative disease, cardiovascular disease, and cancer. However, its oral use is restricted due to poor oral bioavailability (BA).
Ankit Parikh, Krishna Kathawala, Chun Chuan Tan, Sanjay Garg, Xin-Fu Zhou   +4 more
doaj   +1 more source

Divergent Expression and Metabolic Functions of Human Glucuronosyltransferases through Alternative Splicing

Cell Reports, 2016
Maintenance of cellular homeostasis and xenobiotic detoxification is mediated by 19 human UDP-glucuronosyltransferase enzymes (UGTs) encoded by ten genes that comprise the glucuronidation pathway.
Michèle Rouleau, Alan Tourancheau, Camille Girard-Bock, Lyne Villeneuve, Jonathan Vaucher, Anne-Marie Duperré, Yannick Audet-Delage, Isabelle Gilbert, Ion Popa, Arnaud Droit, Chantal Guillemette   +10 more
doaj   +1 more source

Influence of Tramadol on the Intravenous Pharmacokinetics of Dipyrone Active Metabolites in Dogs

Journal of Veterinary Pharmacology and Therapeutics, EarlyView.
ABSTRACT This study aimed to compare the pharmacokinetic profile of the active dipyrone metabolites 4‐methylaminoantipyrine (MAA) and 4‐aminoantipyrine (AA) administered alone and in combination with tramadol in dogs. Nine mixed‐breed dogs, weighing 15.33 ± 2.25 kg, participated in a two‐treatment crossover design: G1 received intravenous dipyrone (25 ...
Andressa Nunes Mouta, Kathryn Nóbrega Arcoverde, Robson dos Anjos Honorato, Naftáli Silva Fernandes, Caio Vinicius Almeida de Oliveira, Glícia Cavalcante Mesquita, Yanna Deysi Bandeira Passos, Gabriel Araújo‐Silva, Valéria Veras de Paula   +8 more
wiley   +1 more source

Characterization of the Pharmacokinetics and Physiological Effects of Tapentadol in Horses

Journal of Veterinary Pharmacology and Therapeutics, EarlyView.
ABSTRACT Tapentadol is a dual mechanism analgesic utilizing both μ‐opioid receptor (MOR) agonism and norepinephrine reuptake inhibition (NRI). This study evaluated the pharmacokinetics and pharmacodynamics of tapentadol as a potential analgesic with the goal of treating pain in horses.
Annabella D. Lynch, Khursheed R. Mama, Dan S. McKemie, Phillip H. Kass, Heather K. Knych   +4 more
wiley   +1 more source

Regioselective Glucuronidation of Diosmetin and Chrysoeriol by the Interplay of Glucuronidation and Transport in UGT1A9-Overexpressing HeLa Cells.

PLoS ONE, 2016
This study aimed to determine the reaction kinetics of the regioselective glucuronidation of diosmetin and chrysoeriol, two important methylated metabolites of luteolin, by human liver microsomes (HLMs) and uridine-5'-diphosphate glucuronosyltransferase (
Xuejun Zeng, Jian Shi, Min Zhao, Qingwei Chen, Liping Wang, Huangyu Jiang, Feifei Luo, Lijun Zhu, Linlin Lu, Xinchun Wang, Zhongqiu Liu   +10 more
doaj   +1 more source

(Poly)phenols: Mechanisms of action and efficacy of contemporary supplements for exercise recovery and performance

Experimental Physiology, EarlyView.
Abstract (Poly)phenols are a diverse group of bioactive chemical compounds present in a wide range of plant‐ and animal‐based foods. Several thousands of (poly)phenols exist; many have potent biological effects, most notably antioxidant, anti‐inflammatory and vasodilatory.
Glyn Howatson, Tom Clifford
wiley   +1 more source

Isoursodeoxycholic acid: metabolism and therapeutic effects in primary biliary cirrhosis1

Journal of Lipid Research, 2001
Significant amounts of ursodeoxycholic acid (UDCA) used for the treatment of patients with primary biliary cirrhosis (PBC) become epimerized at C-3 to isoUDCA. We investigated the metabolism of isoUDCA and a possible pharmacologic effect in five patients
Hanns-Ulrich Marschall, Ulrika Broomé, Curt Einarsson, Gunvor Alvelius, Hans Günther Thomas, Siegfried Matern   +5 more
doaj   +1 more source