The effect of the neuroprotective drug lubeluzole on cortical receptor binding was investigated in animals with photothrombotic ischemic lesions. Control animals were treated with the inactive stereoisomer of the drug. Lubeluzole was applied intravenously as a single bolus (0.31 mg/kg) followed by a 1-h infusion of 0.31 mg/kg. Lubeluzole selectively increased gamma-amino-butyric acid(A) (GABA(A)) receptor binding but had no significant and/or consistent effects on N-methyl-D-aspartate (NMDA), (+/-)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), and kainate receptors. Lubeluzole caused a significant up-regulation of GABA(A) receptor binding in the lesioned area as well as in unimpaired cortical areas of both hemispheres. This effect appeared in the hours following the lesion and peaked at 24 h. Our findings suggest that reduced cortical excitability brought about by increased binding capacities of GABA(A) receptors may contribute to the neuroprotective effect of lubeluzole.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0304-3940(00)01637-2 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Nuclear factor I-C regulates intramembranous bone formation via control of FGF signalling.
Heliyon
January 2025
Department of Oral Histology-Developmental Biology, School of Dentistry and Dental Research Institute, Seoul National University, Seoul, Republic of Korea.
Our previous studies indicate that NFI-C is essential for tooth root development and endochondral ossification. However, its exact role in calvarial intramembranous bone formation remains unclear. In this study, we demonstrate that the disruption of the gene leads to defects in intramembranous bone formation, characterized by decreased osteogenic proliferative activity and reduced osteoblast differentiation during postnatal osteogenesis.
View Article and Find Full Text PDFTranscript Changes of Placental Tissue in Gestational Diabetes Mellitus Based on Transcriptome Sequencing.
Diabetes Metab Syndr Obes
January 2025
Department of Obstetrics, The Affiliated Taian City Central Hospital of Qingdao University, Taian, People's Republic of China.
Purpose: This study aims to identify key genes that may be involved in the pathogenesis of gestational diabetes mellitus and to preliminarily elucidate the underlying mechanisms.
Methods: High-throughput transcriptome sequencing was employed to identify Differentially expressed genes (DEGs) in placental tissue samples of GDM and normal pregnant women. Functional and pathway analyses of these DEGs were conducted using bioinformatics databases.
analysis of the effect of HCV genotype-specific polymorphisms in Core, NS3, NS5A, and NS5B proteins on T-cell epitope processing and presentation.
Front Microbiol
January 2025
Department of Biomedical Sciences, Nazarbayev University School of Medicine, Astana, Kazakhstan.
Background: HCV genotypes are 30-35% polymorphic at the nucleotide level, while subtypes within the same genotype differ by nearly 20%. Although previous studies have shown the immune escape potential of several mutations within the HCV proteins, little is known about the effect of genotype/subtype-specific gene polymorphism on T-cell immunity. Therefore, this study employed several methods to examine the impact of genotype/subtype-specific polymorphisms in Core, NS3, NS5A, and NS5B sequences on T cell epitope processing and HLA-epitope interactions.
View Article and Find Full Text PDFSynthesis, antimicrobial evaluation, ADMET prediction, molecular docking and dynamics studies of pyridine and thiophene moiety-containing chalcones.
R Soc Open Sci
January 2025
Department of Chemistry, Jagannath University, Dhaka 1100, Bangladesh.
In this study, three pyridine- and four thiophene-containing chalcone derivatives were synthesized via Claisen-Schmidt condensation reaction, where five derivatives were new. Different spectral analyses (IR, H NMR, HRMS) clarified the structures and these proposed compounds were screened for antimicrobial activity by the agar disc diffusion technique. Compound was conspicuously active against most of the bacterial and fungal strains.
View Article and Find Full Text PDFDesign and Mechanism Study of 6c, a Novel Artesunate Derivatives, for Anti-Hepatocellular Carcinoma.
J Hepatocell Carcinoma
January 2025
Departments of Pharmacology, School of Pharmacy, Qingdao University Medical College, Shandong, People's Republic of China.
Objective: Artesunate can inhibit the proliferation of various tumor cells and has practical value in developing anti-tumor drugs. However, its biological activity against hepatocellular carcinoma is weak. The efficacy of its anti-tumor effect needs to be improved.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!