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Gabaergic sedative prospection of sclareol-linalool co-treatment: An antagonistic intervention through in vivo and in silico studies.
Neurosci Lett
January 2025
Department of Biological Chemistry, Regional University of Cariri, Crato 63105-000, Brazil. Electronic address:
Sleep disturbance causes many health problems in humans worldwide. This study evaluated the effects and possible mechanisms of sclareol (SCL) and/or linalool (LIN) through in vivo and in silico studies. For this, young chicks SCL (5, 10, and 20 mg/kg) and/or LIN (50 mg/kg) were orally administered thirty minutes before to the thiopental sodium (TS)-induced chicks with or without the standard drug diazepam (DZP: 3 mg/kg).
View Article and Find Full Text PDFSynergistic polytherapy for the broad-spectrum treatment of chemically-induced seizures in rats.
Toxicol Appl Pharmacol
December 2024
Department of CBRN Protection, TNO Defence, Safety and Security, Lange Kleiweg 137, 2288 GJ Rijswijk, the Netherlands.
Chemically-induced seizures, as a result of exposure to a neurotoxic compound, present a serious health concern. Compounds can elicit seizure activity through disruption of neuronal signaling by neurotransmitters, either by mimicking, modulating or antagonizing their action at the receptor or interfering with their metabolism. Benzodiazepines, such as diazepam and midazolam, and barbiturates are the mainstay of treatment of seizures.
View Article and Find Full Text PDFSynthesis and Psychotropic Properties of Novel Condensed Triazines for Drug Discovery.
Pharmaceuticals (Basel)
June 2024
Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Sciences of Republic of Armenia, Ave. Azatutyan 26, Yerevan 0014, Armenia.
The exploration of heterocyclic compounds and their fused analogs, featuring key pharmacophore fragments like pyridine, thiophene, pyrimidine, and triazine rings, is pivotal in medicinal chemistry. These compounds possess a wide array of biological activities, making them an intriguing area of study. The quest for new neurotropic drugs among derivatives of these heterocycles with pharmacophore groups remains a significant research challenge.
View Article and Find Full Text PDFSclareol antagonizes the sedative effect of diazepam in thiopental sodium-induced sleeping animals: In vivo and in silico studies.
Biomed Pharmacother
July 2024
Department of Pharmacy, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, Bangladesh; Pharmacy Discipline, Khulna University, Khulna 9208, Bangladesh; BioLuster Research Center, Gopalganj, Dhaka 8100, Bangladesh.
Background: Sclareol (SCL), a labdane diterpene compound found in Salvia sclarea L., exhibited therapeutic effects. This study investigated the potential interaction between SCL and diazepam (DZP) in modulating sedation in the thiopental sodium-induced sleeping animal model, supported by in-silico molecular docking analysis.
View Article and Find Full Text PDFSynthesis, evaluation of biological activity and SAR of new thioalkyl derivatives of pyridine.
Bioorg Chem
July 2024
Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Sciences of Republic of Armenia, Ave. Azatutyan 26, Yerevan 0014, Armenia.
Article Synopsis
- Pyridine derivatives are important in medicinal chemistry due to their ability to bind biological targets, prompting research to create new thioalkyl derivatives for potential drug development.
- The synthesis of these new compounds utilized classical organic chemistry methods, and various biological tests were conducted to analyze their neurotropic and psychotropic effects, including anticonvulsant and sedative activities.
- Results showed that several synthesized derivatives had high gastro-intestinal absorption, low toxicity, and significant psychotropic effects, with some compounds demonstrating anxiolytic activity up to four times greater than diazepam.
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