ArticleJournal of medicinal chemistry2008
Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different.
Article in Journal of medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers.
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Who cites it
53 citing papers in PubMed, 201 citations in OpenAlex.
- Characterisation of the contribution of the GABA-benzodiazepine α1 receptor subtype to [(11)C]Ro15-4513 PET images.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2012Trial
- Zolpidem restores sleep and decreases amyloid in a mouse model.Alzheimer's & dementia : the journal of the Alzheimer's Association · 2026Article
- Exploring the role of zolpidem in alleviating cognitive and motor impairments in chronic cerebral hypoperfusion: a rat model study with in vivo and in silico insights.Experimental animals · 2026Article
- Abrogation of aberrant glycolytic interactions eliminates senescent cells and alleviates aging-related dysfunctions.Signal transduction and targeted therapy · 2025Article
- Prediction of the therapeutic mechanism of Sugemule-4 in insomnia treatment using network pharmacology and molecular docking.Medicine · 2025Article
- Effects of Chronic Administration of a Standardized Rice Bran Supplement on Sleep Architecture and Profiles in Mice: A Comparative Study with a Hypnotic Drug Zolpidem.Journal of microbiology and biotechnology · 2025Article
- Synergistic effects of combined hypnotic drugs on sleep in mice.Frontiers in pharmacology · 2025Article
- Magnetic nanocatalyst for microwave-assisted synthesis of Benzo[4,5]imidazo[1,2-Frontiers in chemistry · 2025Article
- Greener and whiter analytical method development and validation for determining the presence of zolpidem tartrate infused in apple juice using RP-HPLCRSC advances · 2024Article
- Synthesis of imidazo[1,2-Beilstein journal of organic chemistry · 2023Article
- Pharmacological modulation of chloride channels as a therapeutic strategy for neurological disorders.Frontiers in physiology · 2023Review
- In Silico Screening of Novel α1-GABAInternational journal of molecular sciences · 2021Article
- Regulation of GABATrends in neurosciences · 2021Review
- Eszopiclone and Zolpidem Produce Opposite Effects on Hippocampal Ripple Density.Frontiers in pharmacology · 2021Article
- Synthesis and anticancer activity of bis(2-arylimidazo[1,2-Beilstein journal of organic chemistry · 2020Article
- Aroyl and acyl cyanides as orthogonal protecting groups or as building blocks for the synthesis of heterocycles.Molecular diversity · 2019Review
- Novel imidazo[1,2-a]pyridine inhibits AKT/mTOR pathway and induces cell cycle arrest and apoptosis in melanoma and cervical cancer cells.Oncology letters · 2019Article
- IRSC advances · 2019Article
- The role of loops B and C in determining the potentiation of GABAPharmacology research & perspectives · 2018Article
- Agonists of the γ-aminobutyric acid type B (GABABioorganic & medicinal chemistry letters · 2018Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The sleep-aids zolpidem and eszopiclone exert their effects by binding to and modulating gamma-aminobutyric acid type-A receptors (GABA(A)Rs), but little is known about the structural requirements for their actions. We made 24 cysteine mutations in the benzodiazepine (BZD) binding site of alpha(1)beta(2)gamma(2) GABA(A)Rs and measured zolpidem, eszopiclone, and BZD-site antagonist binding. Mutations in gamma(2)loop D and alpha(1)loops A and B altered the affinity of all ligands tested, indicating that these loops are important for BZD pocket structural integrity. In contrast, gamma(2)loop E and alpha(1)loop C mutations differentially affected ligand affinity, suggesting that these loops are important for ligand selectivity. In agreement with our mutagenesis data, eszopiclone docking yielded a single model stabilized by several hydrogen bonds. Zolpidem docking yielded three equally populated orientations with few polar interactions, suggesting that unlike eszopiclone, zolpidem relies more on shape recognition of the binding pocket than on specific residue interactions and may explain why zolpidem is highly alpha(1)- and gamma(2)-subunit selective.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.