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The diversity of AMPA receptor inhibition mechanisms among amidine-containing compounds.
Front Pharmacol
October 2024
Laboratory for the Research of the Mechanisms of Regulation and Compensation of Nervous System Excitability Pathologies, I.M. Sechenov Institute of Evolutionary Physiology and Biochemistry RAS, Saint Petersburg, Russia.
Amidine-containing compounds are primarily known as antiprotozoal agents (pentamidine, diminazene, furamidine) or as serine protease inhibitors (nafamostat, sepimostat, camostat, gabexate). DAPI is widely recognized as a fluorescent DNA stain. Recently, it has been shown that these compounds also act as NMDA receptor inhibitors.
View Article and Find Full Text PDFGLP-1-directed NMDA receptor antagonism for obesity treatment.
Nature
May 2024
Novo Nordisk Foundation Center for Basic Metabolic Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
The N-methyl-D-aspartate (NMDA) receptor is a glutamate-activated cation channel that is critical to many processes in the brain. Genome-wide association studies suggest that glutamatergic neurotransmission and NMDA receptor-mediated synaptic plasticity are important for body weight homeostasis. Here we report the engineering and preclinical development of a bimodal molecule that integrates NMDA receptor antagonism with glucagon-like peptide-1 (GLP-1) receptor agonism to effectively reverse obesity, hyperglycaemia and dyslipidaemia in rodent models of metabolic disease.
View Article and Find Full Text PDFChanges in Serotonin Modulation of Glutamate Currents in Pyramidal Offspring Cells of Rats Treated With 5-MT during Gestation.
Brain Sci
April 2020
Instituto de Fisiología Benemérita Universidad Autónoma de Puebla, Puebla C.P.72570, Mexico.
Changes in stimuli and feeding in pregnant mothers alter the behavior of offspring. Since behavior is mediated by brain activity, it is expected that postnatal changes occur at the level of currents, receptors or soma and dendrites structure and modulation. In this work, we explore at the mechanism level the effects on Sprague-Dawley rat offspring following the administration of serotonin (5-HT) agonist 5-methoxytryptamine (5-MT).
View Article and Find Full Text PDFMechanism of modulation of AMPA receptors by TARP-γ8.
J Gen Physiol
January 2020
Center for Membrane Biology, Department of Biochemistry and Molecular Biology, University of Texas Health Science Center at Houston, Houston, TX.
Fast excitatory synaptic transmission in the mammalian central nervous system is mediated by glutamate-activated α-amino-5-methyl-3-hydroxy-4-isoxazole propionate (AMPA) receptors. In neurons, AMPA receptors coassemble with transmembrane AMPA receptor regulatory proteins (TARPs). Assembly with TARP γ8 alters the biophysical properties of the receptor, producing resensitization currents in the continued presence of glutamate.
View Article and Find Full Text PDFGlutamate-activated BK channel complexes formed with NMDA receptors.
Proc Natl Acad Sci U S A
September 2018
Department of Anesthesiology and Perioperative Medicine, The University of Texas MD Anderson Cancer Center, Houston, TX 77030;
The large-conductance calcium- and voltage-activated K (BK) channel has a requirement of high intracellular free Ca concentrations for its activation in neurons under physiological conditions. The Ca sources for BK channel activation are not well understood. In this study, we showed by coimmunopurification and colocalization analyses that BK channels form complexes with NMDA receptors (NMDARs) in both rodent brains and a heterologous expression system.
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