Ligand-gated ion channels: new insights into neurological disorders and ligand recognition

D Lemoine, R Jiang, A Taly, T Chataigneau… - Chemical …, 2012 - ACS Publications
1. INTRODUCTION Ligand-gated ion channels (LGICs) mediate intercellular communication
by converting the binding of a neurotransmitter that is released from the presynaptic terminal …

GABAA receptors as molecular targets of general anesthetics: identification of binding sites provides clues to allosteric modulation

RW Olsen, GD Li - Canadian Journal of Anaesthesia, 2010 - pmc.ncbi.nlm.nih.gov
Purpose The purpose of this review is to summarize current knowledge of detailed
biochemical evidence for the role of γ-aminobutyric acid type A receptors (GABAA–Rs) in the …

Diazepam-bound GABAA receptor models identify new benzodiazepine binding-site ligands

L Richter, C De Graaf, W Sieghart, Z Varagic… - Nature chemical …, 2012 - nature.com
Benzodiazepines exert their anxiolytic, anticonvulsant, muscle-relaxant and sedative-
hypnotic properties by allosterically enhancing the action of GABA at GABAA receptors via …

Structural Requirements for Eszopiclone and Zolpidem Binding to the γ-Aminobutyric Acid Type-A (GABAA) Receptor Are Different

SM Hanson, EV Morlock, KA Satyshur… - Journal of medicinal …, 2008 - ACS Publications
The sleep-aids zolpidem and eszopiclone exert their effects by binding to and modulating γ-
aminobutyric acid type-A receptors (GABAARs), but little is known about the structural …

A Unified Model of the GABAA Receptor Comprising Agonist and Benzodiazepine Binding Sites

R Bergmann, K Kongsbak, PL Sørensen, T Sander… - PloS one, 2013 - journals.plos.org
We present a full-length α1β2γ2 GABA receptor model optimized for agonists and
benzodiazepine (BZD) allosteric modulators. We propose binding hypotheses for the …

The GABAA receptor α+ β− interface: a novel target for subtype selective drugs

J Ramerstorfer, R Furtmüller… - Journal of …, 2011 - Soc Neuroscience
GABAA receptors mediate the action of many clinically important drugs interacting with
different binding sites. For some potential binding sites, no interacting drugs have yet been …

Structure-based design, synthesis, and biochemical and pharmacological characterization of novel salvinorin A analogues as active state probes of the κ-opioid …

F Yan, RV Bikbulatov, V Mocanu, N Dicheva… - Biochemistry, 2009 - ACS Publications
Salvinorin A, the most potent naturally occurring hallucinogen, has attracted an increasing
amount of attention since the κ-opioid receptor (KOR) was identified as its principal …

Investigation of [3H]diazepam derivatives as allosteric modulators of GABAA receptor α1β2γ2 subtypes: combination of molecular docking/dynamic simulations …

R Djebaili, S Kenouche, I Daoud, N Melkemi… - Structural Chemistry, 2023 - Springer
In this paper, a data set of [3H] diazepam derivatives was analyzed using various
computational methods: molecular docking/dynamic simulations, and QSAR analysis. The …

Developmental toxicity of procymidone to larval zebrafish based on physiological and transcriptomic analysis

A Wu, Q Yu, H Lu, Z Lou, Y Zhao, T Luo, Z Fu… - … and Physiology Part C …, 2021 - Elsevier
As a broad-spectrum with low toxicity, procymidone (PCM), is widely used in agriculture and
frequently observed in aquatic system, which may cause some impacts on aquatic …

Synthesis, anticonvulsant screening, and molecular modeling studies of new arylalkylimidazole oxime ether derivatives

Z Özdemir, S Sari, A Karakurt… - Drug Development …, 2019 - Wiley Online Library
In this study, 15 new oxime ether derivatives were synthesized and their anticonvulsant
activities were screened in vivo. The compounds were synthesized by the reaction of various …