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Effect of Lipopolysaccharide on the Duration of Zolpidem-Induced Loss of Righting Reflex in Mice.
Acta Med Okayama
June 2024
Department of Clinical Pharmacy, Okayama University, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences.
Zolpidem, a non-benzodiazepine hypnotic, is primarily used to treat insomnia. In a previous study, pior treatment with non-benzodiazepine receptor agonists was associated with inflammation. The present study aimed to clarify the association between the effects of zolpidem and inflammation in mice treated with lipopolysaccharide (LPS), a known model of inflammation.
View Article and Find Full Text PDFCase Report: High doses of Zolpidem and QT interval lengthening: Is there a relationship? A case series.
Front Psychiatry
October 2022
Unit of Addiction Medicine, Department of Internal Medicine, G.B. Rossi Hospital, Verona, Italy.
Zolpidem is indicated in cases of severe insomnia in adults and, as for BDZs, its assumption should be limited to short periods under close medical supervision. Since several drugs cause corrected QT interval (QTc) elongation, the authors investigated whether high daily doses of Zolpidem could cause QTc elongation. The study was conducted in the Addiction Medicine Unit of the G.
View Article and Find Full Text PDFAltered Behavioral Responses Show GABA Sensitivity in Muscleblind-Like 2-Deficient Mice: Implications for CNS Symptoms in Myotonic Dystrophy.
eNeuro
October 2022
Department of Cell Biology, Emory University School of Medicine, Atlanta, GA 30322
Considerable evidence from mouse models and human postmortem brain suggests loss of Muscleblind-like protein 2 (MBNL2) function in brain is a major driver of CNS symptoms in Myotonic dystrophy type 1 (DM1). Increased hypersomnia, fatigue, and surgical complications associated with general anesthesia suggest possible sensitivity to GABAergic inhibition in DM1. To test the hypothesis that MBNL2 depletion leads to behavioral sensitivity to GABA receptor (GABA-R) modulation, knock-out (KO) and wild-type (WT) littermates were treated with the anesthetic sevoflurane, the benzodiazepine diazepam, the imidazopyridine zolpidem, and the benzodiazepine rescue agent, flumazenil (Ro 15-1788), and assessed for various behavioral metrics.
View Article and Find Full Text PDFHigh-Dose Benzodiazepines Positively Modulate GABA Receptors via a Flumazenil-Insensitive Mechanism.
Int J Mol Sci
December 2021
State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Key Laboratory of Neuropsychopharmacology, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.
Benzodiazepines (BZDs) produce versatile pharmacological actions through positive modulation of GABA receptors (GABARs). A previous study has demonstrated that high concentrations of diazepam potentiate GABA currents on the αβγ and αβ GABARs in a flumazenil-insensitive manner. In this study, the high-concentration effects of BZDs and their sensitivity to flumazenil were determined on synaptic (αβγ, αβγ, αβγ) and extra-synaptic (αβδ) GABARs using the voltage-clamp electrophysiology technique.
View Article and Find Full Text PDFSynthesis of 4,6-diphenylpyrimidin-2-ol derivatives as new benzodiazepine receptor ligands.
Bioorg Chem
April 2021
Department of Pharmacology and Toxicology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran. Electronic address:
Benzodiazepines (BZDs) have been widely used in neurological disorders such as insomnia, anxiety, and epilepsy. The use of classical BZDs, e.g.
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