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Synthesis, Anticonvulsant, Antinociceptive Activity and Preliminary Safety Evaluations of Novel Hybrid Imidazolidine-2,4-dione Derivatives with Morpholine Moiety.
ChemMedChem
December 2024
Uniwersytet Jagielloński Collegium Medicum, Department of Medicinal Chemistry, POLAND.
This study aimed to design new hybrid compounds with imidazolidin-2,4-dione and morpholine rings as broad spectrum anticonvulsants. To achieve this goal, all compounds were evaluated in animal seizure models, namely the maximal electroshock (MES), the subcutaneous pentylenetetrazole (scPTZ), and selected in the 6 Hz (32 mA) tests. The most promising compound, 5-isopropyl-3-(morpholinomethyl)-5-phenylimidazolidine-2,4-dione (19), demonstrated broader anticonvulsant activity than phenytoin or levetiracetam, with ED50 of 26.
View Article and Find Full Text PDFThe fruit fly as a screening model for antiseizure medications.
Front Pharmacol
December 2024
Department of Epileptology and Neurology, RWTH Aachen University, Aachen, Germany.
Objective: Resistance to antiseizure medications (ASMs) is a major challenge in the treatment of patients with epilepsy. Despite numerous newly marketed ASMs, the proportion of drug-resistant people with epilepsy has not significantly decreased over the years. Therefore, novel and innovative seizure models for preclinical drug screening are highly desirable.
View Article and Find Full Text PDFThe impact of extract on pharmacokinetics of phenytoin in rats.
Nat Prod Res
December 2024
Faculty of Health Sciences, University of Beira Interior, Covilhã, Portugal.
Epilepsy patients are at a higher risk of developing overweight and obesity. Given the thermogenic properties of (Guarana), this study aimed to evaluate a potential pharmacokinetic interaction between extract and phenytoin in rats. Two pharmacokinetic studies were developed with and phenytoin: a coadministration and a pre-treatment study.
View Article and Find Full Text PDFEffectiveness of pharmacological therapies for fibromyalgia syndrome in adults: an overview of Cochrane Reviews.
Rheumatology (Oxford)
December 2024
Division of Preventive Medicine, Department of Medicine, University of Alberta, Edmonton AB, Canada.
Objectives: To summarise and evaluate Cochrane reviews of pharmacological therapies for adults with fibromyalgia syndrome (FMS) pain.
Methods: Systematic search of Cochrane Database of Systematic Reviews to May 2024. Generic quality assessment used AMSTAR-2 criteria, validity checks of potentially critical factors in evaluation of analgesic efficacy, and assessment of susceptibility of results to publication bias.
Effectiveness of pharmacological therapies for fibromyalgia syndrome in adults: an overview of Cochrane Reviews.
Rheumatology (Oxford)
December 2024
Division of Preventive Medicine, Department of Medicine, University of Alberta, Edmonton AB, Canada.
Objectives: To summarise and evaluate Cochrane reviews of pharmacological therapies for adults with fibromyalgia syndrome (FMS) pain.
Methods: Systematic search of Cochrane Database of Systematic Reviews to May 2024. Generic quality assessment used AMSTAR-2 criteria, validity checks of potentially critical factors in evaluation of analgesic efficacy, and assessment of susceptibility of results to publication bias.
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