ArticleScientific reports2016
Zolpidem is a potent stoichiometry-selective modulator of α1β3 GABAA receptors: evidence of a novel benzodiazepine site in the α1-α1 interface.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 38 citations in OpenAlex.
- Effects of zolpidem on sleep parameters in patients with cirrhosis and sleep disturbances: A randomized, placebo-controlled trial.Clinical and molecular hepatology · 2019Trial
- 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
- Probes for the heterogeneity of muscimol binding sites in rat brain.Frontiers in pharmacology · 2024Article
- GABA signalling in human pancreatic islets.Frontiers in endocrinology · 2023Review
- Structural and dynamic mechanisms of GABANature communications · 2022Article
- High-Dose Benzodiazepines Positively Modulate GABAInternational journal of molecular sciences · 2021Article
- The efficacy of γ-aminobutyric acid type A receptor (GABAToxicology and applied pharmacology · 2021Article
- Electrophysiology of ionotropic GABA receptors.Cellular and molecular life sciences : CMLS · 2021Review
- GABAFrontiers in neuroscience · 2021Article
- Eszopiclone and Zolpidem Produce Opposite Effects on Hippocampal Ripple Density.Frontiers in pharmacology · 2021Article
- Flumazenil-Insensitive Benzodiazepine Effects in Recombinant αβ and Neuronal GABABrain sciences · 2020Article
- Sleep Disturbances After General Anesthesia: Current Perspectives.Frontiers in neurology · 2020Review
- Construction of a Fluorescent Screening System of Allosteric Modulators for the GABAACS central science · 2019Article
- Concatenated γ-aminobutyric acid type A receptors revisited: Finding order in chaos.The Journal of general physiology · 2019Article
- Functional genomics of epilepsy-associated mutations in the GABAThe Journal of biological chemistry · 2019Article
- Cell surface expression of homomeric GABAThe Journal of biological chemistry · 2018Article
- Molecular tools for GABAScientific reports · 2017Article
- Reducing GABAScientific reports · 2016Article
- Article
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6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Zolpidem is not a typical GABAA receptor hypnotic. Unlike benzodiazepines, zolpidem modulates tonic GABA currents in the rat dorsal motor nucleus of the vagus, exhibits residual effects in mice lacking the benzodiazepine binding site, and improves speech, cognitive and motor function in human patients with severe brain injury. The receptor by which zolpidem mediates these effects is not known. In this study we evaluated binary α1β3 GABAA receptors in either the 3α1:2β3 or 2α1:3β3 subunit stoichiometry, which differ by the existence of either an α1-α1 interface, or a β3-β3 interface, respectively. Both receptor stoichiometries are readily expressed in Xenopus oocytes, distinguished from each other by using GABA, zolpidem, diazepam and Zn(2+). At the 3α1:2β3 receptor, clinically relevant concentrations of zolpidem enhanced GABA in a flumazenil-sensitive manner. The efficacy of diazepam was significantly lower compared to zolpidem. No modulation by either zolpidem or diazepam was detected at the 2α1:3β3 receptor, indicating that the binding site for zolpidem is at the α1-α1 interface, a site mimicking the classical α1-γ2 benzodiazepine site. Activating α1β3 (3α1:2β3) receptors may, in part, mediate the physiological effects of zolpidem observed under distinct physiological and clinical conditions, constituting a potentially attractive drug target.
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