Glutamate (Glu) is considered the most important excitatory amino acid neurotransmitter in the mammalian Central Nervous System. Zinc (Zn) is co-released with Glu during synaptic transmission and interacts with Glutamate receptors and transporters. We performed binding experiments using [H]MK-801 (NMDA), and [H]Fluorowillardine (AMPA) as ligands to study Zn-Glutamate interactions in rat cortical synaptic membranes. We also examined the effects of mercury and lead on NMDA or AMPA receptors. Zinc at 1 nM, significantly potentiates [H]MK-801 binding. Lead inhibits [H]MK-801 binding at micromolar concentrations. At millimolar concentrations, Hg also has a significant inhibitory effect. These effects are not reversed by Zn (1 nM). Zinc displaces the [H]FW binding curve to the right. Lead (nM) and Hg (μM) inhibit [H]FW binding. At certain concentrations, Zn reverses the effects of these metals on [H]FW binding. These specific interactions serve to clarify the role of Zn, Hg, and Pb in physiological and pathological conditions.
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http://dx.doi.org/10.1007/s11064-021-03407-w | DOI Listing |
Neurochem Res
December 2021
Department of Pharmacology and Toxicology, University of Puerto Rico School of Medicine, P.O. Box 365067, San Juan, 00936-5067, Puerto Rico.
Glutamate (Glu) is considered the most important excitatory amino acid neurotransmitter in the mammalian Central Nervous System. Zinc (Zn) is co-released with Glu during synaptic transmission and interacts with Glutamate receptors and transporters. We performed binding experiments using [H]MK-801 (NMDA), and [H]Fluorowillardine (AMPA) as ligands to study Zn-Glutamate interactions in rat cortical synaptic membranes.
View Article and Find Full Text PDFEvid Based Complement Alternat Med
July 2011
Department of Pharmacology and Toxicology, School of Medicine, University of Puerto Rico, Medical Sciences Campus, P.O. Box 365067, San Juan, 00936-5067 Puerto Rico, USA.
The effects of two valerian extracts (aqueous and hydroalcoholic) were investigated through [(3)H]Glutamate ([(3)H]Glu) and [(3)H]Fluorowillardine ([(3)H]FW) receptor binding assays using rat synaptic membranes in presence of different receptor ligands. In addition, the extract stability was monitored spectrophotometrically. Both extracts demonstrated interaction with ionotropic glutamate receptors (iGluRs).
View Article and Find Full Text PDFAnn N Y Acad Sci
August 2006
Department of Pharmacology and Toxicology, School of Medicine, University of Puerto Rico, Medical Sciences Campus, P.O. Box 365067, San Juan, Puerto Rico 00936-5067, USA.
Cocaine sensitization results in the development of increased locomotion and stereotypy. It is accompanied by changes in glutamatergic trasmission that appear to be region-specific. The purpose of this article was to determine the effect(s) of cocaine and prazosin plus cocaine treatments on ionotropic glutamate receptors in rat cerebral cortex (CTX) and prefrontal cortex (PFC).
View Article and Find Full Text PDFBr J Pharmacol
August 2001
MRC Centre for Synaptic Plasticity, Anatomy Department, School of Medical Sciences, University of Bristol, University Walk, Bristol, BS8 1TD, UK.
In addition to its role in hydrolyzing the neurotransmitter acetylcholine, the synaptically enriched enzyme acetylcholinesterase (AChE) has been reported to play an important role in the development and remodelling of neural processes and synapses. We have shown previously that AChE causes an increase in binding of the specific AMPA receptor ligand (S)-[(3)H]-5-fluorowillardiine ([(3)H]-FW) to rat brain membranes. In this study we have used quantitative autoradiography to investigate the regional distribution and age-dependence of AChE-evoked increases in the binding of [(3)H]-FW in rat brain.
View Article and Find Full Text PDFNeurosci Lett
September 2000
Department of Pharmacology, Faculty of Medicine, PO Box 13E, Monash University, 3800, Victoria, Australia.
Adenosine A(2a) receptor knockout mice (A(2a)R k/o) have been characterised as hypertensive, aggressive, anxious and hypoalgesic [12]. Thus, the present study was designed to investigate markers of glutamatergic transmission in specific brain nuclei associated with autonomic regulation. Visualisation of alpha-amino-3-hydroxy-5-methylisoxasole-4-propionic acid binding sites in the brains of A(2a)R k/o mice was achieved by utilising quantitative receptor autoradiography with (S)-[(3)H]-5-fluorowillardiine ([(3)H]FW:10 nM) on slide-mounted sections of mouse-brain.
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