Results 111 to 120 of about 1,218,415 (224)

Preclinical and Toxicology Studies of LPM7100328, a Novel Oral GnRH Antagonist

Pharmacology Research &Perspectives, Volume 14, Issue 5, October 2026.
ABSTRACT LPM7100328 is a novel oral GnRH antagonist being developed for the prevention of premature luteinizing hormone (LH) surges in women undergoing controlled ovarian stimulation. The studies presented herein reported assessment of safety in favor of human clinical trials.
Yao Wang, Junxian Zhao, Fangxia Zou, Wanglin Jiang, Jianzhao Zhang, Pengfei Yu, Liang Ye, Xiaolin Sun, Chunmei Li, Jingwei Tian   +9 more
wiley   +1 more source

Molecular basis of cardiac arrhythmias: genetics of natural variants and electrophysiological investigation of mutant proteins [PDF]

, 2010
Channelopathies are diseases caused by deranged functioning of ion channel subunits or the proteins that regulate them. Long QT and Brugada syndrome are included in this group.
Detta, Nicola
core  

Implementation of the In Vitro Seizure Liability Assay (iLAseizure) in Drug Discovery and Development: Mechanism of Action Case Studies

Pharmacology Research &Perspectives, Volume 14, Issue 5, October 2026.
ABSTRACT Central nervous system (CNS) liabilities remain a significant cause of attrition during small molecule drug development. We previously developed the in vitro seizure liability assay (iLAseizure), a new approach methodology (NAM) comprising a human induced pluripotent stem cell neuron microelectrode array (MEA) assay coupled with a panel of ...
Kimberly Rockley, Ruth Roberts, Hannah Jennings, Karen Jones, Magali‐Anne Maizières, Michael Morton   +5 more
wiley   +1 more source

Application of an Open‐Source Modular Framework for Pharmacokinetic, Pharmacodynamic, and Safety Simulations to Anti‐Tuberculosis Drugs

CPT: Pharmacometrics &Systems Pharmacology, Volume 15, Issue 10, October 2026.
ABSTRACT Tuberculosis (TB) treatment requires long‐term multidrug regimens where dosing, efficacy, and safety optimization remain challenging. This tutorial establishes an integrated, open‐source, modular framework connecting high‐throughput PBPK (HT‐PBPK) simulations, mechanistic PBPK models, pharmacodynamic endpoints, and safety predictions for anti ...
Marco Siccardi, Nina Nauwelaerts, Raphaëlle Lesage, Diane Lefaudeux, Vanessa Baier, Venetia Karamitsou, Cleo Demeester, Miao‐Chan Huang, Alexander Kulesza, Stephan Schaller   +9 more
wiley   +1 more source

Chlorine Position Governs the Multitarget Bioactivity of Phenylhydrazines: In Vitro Antioxidant, Anti‐Inflammatory, Anti‐Tyrosinase and Antibacterial Evaluation Supported by DFT and Molecular Docking

ChemistrySelect, Volume 11, Issue 37, 6 October 2026.
Positional chlorination emerges as a key determinant of multitarget activity in phenylhydrazines. The para‐chloro derivative H3 shows the strongest anti‐inflammatory response, notable antibacterial activity, favorable ADMET behavior, and high COX‐2 affinity. DFT descriptors and molecular docking rationalize these substitution‐dependent effects, linking
L. Aouachria, S. Issadi, H. Debab, I. Selatnia, A.G. Soliman, K. Metwally, O. M. A. Khamaysa, Han‐seung Lee, Hassane Lgaz   +8 more
wiley   +1 more source

Rosemary metabolite carnosic acid opens Kv1.1 via its voltage sensor and corrects Kv1.1‐linked episodic ataxia in mice

British Journal of Pharmacology, Volume 183, Issue 20, Page 6179-6198, October 2026.
Background and Purpose Episodic ataxia type 1 (EA1) is an autosomal dominant neurological disorder caused primarily by loss‐of‐function mutations in the voltage‐gated potassium channel Kv1.1 (KCNA1). Small molecules that restore Kv1.1 activity hold promise as targeted therapies for EA1, yet current pharmacological strategies remain limited ...
Rían W. Manville, Ryan F. Yoshimura, Hanh A. Nguyen, Ruiming Zhao, Derk J. Hogenkamp, Steve A. N. Goldstein, Geoffrey W. Abbott   +6 more
wiley   +1 more source

Comprehensive in vitro profiling of traditional and emerging stimulants at monoamine transporters and the 5‐HT2A receptor

British Journal of Pharmacology, Volume 183, Issue 19, Page 5871-5894, October 2026.
A pharmacological profiling of 58 synthetic stimulants of various classes at dopamine, norepinephrine, and serotonin transporters and the 5‐HT2A receptor, most showing distinct class‐dependent profiles, with some indicating a high abuse potential. Background and Purpose New psychoactive substances (NPSs) often emerge on the illicit drug market with ...
Darta Stalberga, Robert Kronstrand, Bianca Schranz, Nick van Zijl, Sebastian Karlman, Soma Aref, Tobias Rautio, Svante Vikingsson, Mattias Persson, Henrik Green   +9 more
wiley   +1 more source

A Multi‐Scale Computational Framework for Anti‐Persister Tuberculosis Drug Discovery

Chemical Biology &Drug Design, Volume 108, Issue 4, October 2026.
This review presents an integrated QSAR–scaffold design–docking–MD framework for discovering anti‐persister tuberculosis agents active in dormant granuloma‐like conditions. By targeting Mtb bioenergetics and prioritising dual NDH‐2/cytochrome bd oxidase inhibition, the workflow advances rational design of candidates with higher resistance barriers ...
Said Moshawih, Anguraj Moulishankar, Chee Yan Choo, Khang Wen Goh, Chrismawan Ardianto, Azam Che Idris, Long Chiau Ming   +6 more
wiley   +1 more source

Cell-Based hERG Channel Inhibition Assay in High-Throughput Format. [PDF]

Methods Mol Biol, 2022
Zhao J, Xia M.
europepmc   +1 more source

Computer Simulations of Structure–Activity Relationships for hERG Channel Blockers

, 2016
The hERG potassium channel is of major pharmaceutical importance, and its blockade by various compounds, potentially causing serious cardiac side effects, is a major problem in drug development.
Göran Wallin (2036587), Johan Åqvist (553577), Henrik Keränen (2183596), Bert L. de Groot (131967), Anna Stary-Weinzinger (194187), Lars Boukharta (553575)   +5 more
core   +1 more source