Results 81 to 90 of about 1,218,415 (224)

Signal detection and characterisation of a novel drug–drug interaction between methadone and a synthetic cannabinoid receptor agonist

British Journal of Pharmacology, EarlyView.
Background and Purpose Little is known about how synthetic cannabinoid receptor agonist (SCRA) co‐use with other psychoactive substances may exacerbate risk of death. This study aimed to characterise the polypharmacy of deaths where SCRAs were detected at post‐mortem, investigate the cardiotoxicity of SCRAs and probe their inhibition of human ether‐a ...
Kirsten L. Rock, Louise M. Hesketh, Hongwei Cheng, Shuoqi Chen, Simon Hudson, Graeme Henderson, Jules C. Hancox, Michael J. Shattock, Michael J. Curtis, Caroline S. Copeland   +9 more
wiley   +1 more source

Selective excitatory effects of γ‐glutamyl‐glycine, a glutathione metabolite, on GluN1 NMDA and mGlu5 receptors impacting synaptic plasticity

British Journal of Pharmacology, EarlyView.
Background and Purpose Gamma‐glutamyl dipeptides are essentially produced after glutathione (GSH) degradation. While several γ‐glutamyl dipeptides have been detected in different organs and body fluids, their biological activity remains elusive. This is the case for γ‐Glutamyl‐Glycine (γ‐Glu‐Gly) which has been found in different brain areas.
Sandro Andreu, Victoria Gizzi, Ugo Pasco, Fatiha Sebih, Yattou Zitouni, Pablo Jimenez, Valérie Rolland, Alain Chavanieu, Sébastien Estaran, Matthieu Rousset, Thierry Cens, Guillaume Cazals, Pierre Charnet, Janique Guiramand, Catherine Cohen‐Solal, Claudine Ménard, Marie‐Céleste de Jésus Ferreira, Nathalie Chevallier, Sonia Cantel, Michel Vignes, Julien Roussel   +20 more
wiley   +1 more source

Methyl 4‐O‐Demethylbarbatate Destabilises HIF‐1α and Enhances Temozolomide Sensitivity in Glioma Cells

Cell Proliferation, EarlyView.
The lichen‐derived metabolite methyl 4‐O‐demethylbarbatate (Me‐4‐O‐DBA) suppresses glioma stemness, motility, and metabolic plasticity through inhibition of HIF‐1α signaling and synergistically enhances temozolomide activity, highlighting a potential strategy to target stemness‐driven therapeutic resistance in glioma.
Rui Zhou, Mücahit Varlı, Rundong Liu, Jieun Yu, Hyung‐Ho Ha, Jae‐Seoun Hur, Sang Kyum Kim, Hahyun Park, Hangun Kim   +8 more
wiley   +1 more source

Caenorhabditis elegans as an in vivo model system for human inherited primary arrhythmia syndromes

The Journal of Physiology, EarlyView.
Abstract figure legend Most genes involved in inherited primary arrhythmia syndromes (IPAS) are conserved in Caenorhabditis elegans, where genetic manipulation enables functional characterization of variants, identification of regulatory proteins, and in vivo drug testing.
Antoine Delinière, Thomas Boulin, Maëlle Jospin, Alexandre Janin, Gilles Millat, Philippe Chevalier, Olga Andrini   +6 more
wiley   +1 more source

Characterization of the novel mutant A78T-HERG from a long QT syndrome type 2 patient: Instability of the mutant protein and stabilization by heat shock factor 1

Journal of Arrhythmia, 2016
Background: The human ether-a-go-go-related gene (HERG) encodes the α-subunit of rapidly activating delayed-rectifier potassium channels. Mutations in this gene cause long QT syndrome type 2 (LQT2).
Takehito Kondo, Ichiro Hisatome, Shouichi Yoshimura, Endang Mahati, Tomomi Notsu, Peili Li, Kazuhiko Iitsuka, Masaru Kato, Kazuyoshi Ogura, Junichiro Miake, Takeshi Aiba, Wataru Shimizu, Yasutaka Kurata, Shinji Sakata, Naoe Nakasone, Haruaki Ninomiya, Akira Nakai, Katsumi Higaki, Yasushi Kawata, Yasuaki Shirayoshi, Akio Yoshida, Kazuhiro Yamamoto   +21 more
doaj   +1 more source

Voltage‐gated potassium channels mediate thyroid hormone control of skeletal muscle excitability

The Journal of Physiology, EarlyView.
Abstract figure legend Thyroid hormone (TH)‐dependent remodelling of potassium (K+) channel networks regulates skeletal muscle (SkM) excitability. Triiodothyronine (T3), locally generated from thyroxine (T4) by type 2 deiodinase (D2), binds thyroid hormone receptors (TRα/β) and modulates transcription via thyroid response elements (TREs).
Annarita Nappi, Caterina Miro, Annunziata Gaetana Cicatiello, Ilaria Piccialli, Serena Sagliocchi, Lucia Acampora, Federica Restolfer, Rosa Sirica, Melania Murolo, Emery Di Cicco, Daniela Terracciano, Anna Pannaccione, Monica Dentice   +12 more
wiley   +1 more source

Advances in New Approach Methodologies at FDA's Division of Applied Regulatory Science

Clinical Pharmacology &Therapeutics, Volume 120, Issue 5, Page 1250-1254, November 2026.
New Approach Methodologies (NAMs) represent a paradigm shift in drug development and regulatory science, offering human‐relevant alternatives to traditional preclinical models. This mini‐review highlights recent advances in NAM development, validation, and regulatory application from FDA's Division of Applied Regulatory Science (DARS).
Ksenia Blinova, Kimberly Chiu, Anik Chaturbedi, Jahan Cooper, Tromondae K. Feaster, Paula L. Hyland, Lidiya Stavitskaya, Wendy W. Wu, Jeffry Florian, Rodney Rouse   +9 more
wiley   +1 more source

HERG Protein Plays a Role in Moxifloxacin-Induced Hypoglycemia

Journal of Diabetes Research, 2016
The purpose of this study was to investigate the effect of moxifloxacin on HERG channel protein and glucose metabolism. HERG expression was investigated using immunohistochemistry.
Hai-Yan Qiu, Sha-Sha Yuan, Fang-Yuan Yang, Ting-Ting Shi, Jin-Kui Yang   +4 more
doaj   +1 more source

In Silico Clinical Trials in Drug Development: Virtual Patients, Applications, and Regulatory Convergence

Clinical Pharmacology &Therapeutics, Volume 120, Issue 5, Page 1181-1194, November 2026.
Conventional clinical trials remain the benchmark for evaluating therapeutic safety and efficacy, yet they are constrained by escalating costs, withdrawal over the extended follow‐up periods, recruitment difficulties, ethical limits, and a restricted ability to characterize heterogeneous populations.
Maximilian Balmus, Sheng‐Ya Wang, Edward W. G. Ashton, Rosie K. Barrows, Molly Monks, Yuzhang Ge, Arthur Lefebvre, Steven A. Niederer   +7 more
wiley   +1 more source

Validation of a [3H]Astemizole Binding Assay in HEK293 Cells Expressing HERG K+ Channels

Journal of Pharmacological Sciences, 2004
A radioligand binding assay for the HERG (human ether-a-go-go-related gene) K+ channel was developed to identify compounds which may have inhibitory activity and potential cardiotoxicity.
Peter J.S. Chiu, Karen F. Marcoe, Sidney E. Bounds, Chun-Hsiung Lin, Jin-Jye Feng, Atsui Lin, Fong-Chi Cheng, William J. Crumb, Richard Mitchell   +8 more
doaj   +1 more source