Development of Potent Fluorescent Polyamine Toxins and Application in Labeling of Ionotropic Glutamate Receptors in Hippocampal Neurons

2013 ◽  
Vol 8 (9) ◽  
pp. 2033-2041 ◽  
Author(s):  
Niels G. Nørager ◽  
Christel B. Jensen ◽  
Mette Rathje ◽  
Jacob Andersen ◽  
Kenneth L. Madsen ◽  
...  
Keyword(s):  
Glutamate Receptors ◽  
Hippocampal Neurons ◽  
Ionotropic Glutamate Receptors ◽  
Polyamine Toxins

scholarly journals Illuminating Ionotropic Glutamate Receptors: Characterization of Fluorescent Antagonists Based on Polyamine Toxins

2013 ◽  
Vol 104 (2) ◽  
pp. 272a
Author(s):  
Christel B. Jensen ◽  
Niels G. Nørager ◽  
Anders S. Kristensen ◽  
Kristian Strømgaard
Keyword(s):  
Glutamate Receptors ◽  
Ionotropic Glutamate Receptors ◽  
Polyamine Toxins

scholarly journals Rapid, Activation-Induced Redistribution of Ionotropic Glutamate Receptors in Cultured Hippocampal Neurons

1999 ◽  
Vol 19 (4) ◽  
pp. 1263-1272 ◽  
Author(s):  
Dmitri V. Lissin ◽  
Reed C. Carroll ◽  
Roger A. Nicoll ◽  
Robert C. Malenka ◽  
Mark von Zastrow
Keyword(s):  
Glutamate Receptors ◽  
Hippocampal Neurons ◽  
Ionotropic Glutamate Receptors ◽  
Rapid Activation ◽  
Cultured Hippocampal Neurons

scholarly journals Cover Picture: Structure-Activity Relationship Study of Spider Polyamine Toxins as Inhibitors of Ionotropic Glutamate Receptors (ChemMedChem 12/2014)

ChemMedChem ◽  
2014 ◽  
Vol 9 (12) ◽  
pp. 2605-2605
Author(s):  
Xiao-Feng Xiong ◽  
Mette H. Poulsen ◽  
Rama A. Hussein ◽  
Niels G. Nørager ◽  
Kristian Strømgaard
Keyword(s):  
Glutamate Receptors ◽  
Structure Activity Relationship ◽  
Ionotropic Glutamate Receptors ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Study ◽  
Polyamine Toxins

Structure–Activity Relationship Studies of N-Methylated and N-Hydroxylated Spider Polyamine Toxins as Inhibitors of Ionotropic Glutamate Receptors

2014 ◽  
Vol 57 (11) ◽  
pp. 4940-4949 ◽  
Author(s):  
Niels G. Nørager ◽  
Mette H. Poulsen ◽  
Anna G. Jensen ◽  
Nanna S. Jeppesen ◽  
Anders S. Kristensen ◽  
...  
Keyword(s):  
Glutamate Receptors ◽  
Structure Activity Relationship ◽  
Ionotropic Glutamate Receptors ◽  
Activity Relationship ◽  
Structure Activity ◽  
Polyamine Toxins

General Synthesis of β-Alanine-Containing Spider Polyamine Toxins and Discovery of Nephila Polyamine Toxins 1 and 8 as Highly Potent Inhibitors of Ionotropic Glutamate Receptors

2012 ◽  
Vol 55 (22) ◽  
pp. 10297-10301 ◽  
Author(s):  
Simon Lucas ◽  
Mette H. Poulsen ◽  
Niels G. Nørager ◽  
Anne F. Barslund ◽  
Tinna B. Bach ◽  
...  
Keyword(s):  
Glutamate Receptors ◽  
Ionotropic Glutamate Receptors ◽  
General Synthesis ◽  
Polyamine Toxins

Structure-Activity Relationship Study of Spider Polyamine Toxins as Inhibitors of Ionotropic Glutamate Receptors

ChemMedChem ◽  
2014 ◽  
Vol 9 (12) ◽  
pp. 2661-2670 ◽  
Author(s):  
Xiao-Feng Xiong ◽  
Mette H. Poulsen ◽  
Rama A. Hussein ◽  
Niels G. Nørager ◽  
Kristian Strømgaard
Keyword(s):  
Glutamate Receptors ◽  
Structure Activity Relationship ◽  
Ionotropic Glutamate Receptors ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Study ◽  
Polyamine Toxins

Differential effects of chlorpromazine on ionotropic glutamate receptors in cultured rat hippocampal neurons

2001 ◽  
Vol 305 (1) ◽  
pp. 53-56 ◽  
Author(s):  
Ewa D. Żarnowska ◽  
Jerzy W. Mozrzymas
Keyword(s):  
Glutamate Receptors ◽  
Hippocampal Neurons ◽  
Ionotropic Glutamate Receptors ◽  
Differential Effects

Repeated brief episodes of hypoxia modulate the calcium responses of ionotropic glutamate receptors in hippocampal neurons

2011 ◽  
Vol 496 (1) ◽  
pp. 11-14 ◽  
Author(s):  
Marija V. Turovskaya ◽  
Egor A. Turovsky ◽  
Valery P. Zinchenko ◽  
Sergei G. Levin ◽  
Alina A. Shamsutdinova ◽  
...  
Keyword(s):  
Glutamate Receptors ◽  
Hippocampal Neurons ◽  
Ionotropic Glutamate Receptors

High Concentrations of Tranexamic Acid Inhibit Ionotropic Glutamate Receptors

2017 ◽  
Vol 127 (1) ◽  
pp. 89-97 ◽  
Author(s):  
Irene Lecker ◽  
Dian-Shi Wang ◽  
Kirusanthy Kaneshwaran ◽  
C. David Mazer ◽  
Beverley A. Orser
Keyword(s):  
Tranexamic Acid ◽  
Nmda Receptors ◽  
Glutamate Receptors ◽  
Hippocampal Neurons ◽  
Inhibitory Concentration ◽  
Cell Voltage ◽  
Kainate Receptors ◽  
Ionotropic Glutamate Receptors ◽  
Competitive Antagonist ◽  
Peripheral Tissues

Abstract Background The antifibrinolytic drug tranexamic acid is structurally similar to the amino acid glycine and may cause seizures and myoclonus by acting as a competitive antagonist of glycine receptors. Glycine is an obligatory co-agonist of the N-methyl-d-aspartate (NMDA) subtype of glutamate receptors. Thus, it is plausible that tranexamic acid inhibits NMDA receptors by acting as a competitive antagonist at the glycine binding site. The aim of this study was to determine whether tranexamic acid inhibits NMDA receptors, as well as α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid and kainate subtypes of ionotropic glutamate receptors. Methods Tranexamic acid modulation of NMDA, α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid, and kainate receptors was studied using whole cell voltage-clamp recordings of current from cultured mouse hippocampal neurons. Results Tranexamic acid rapidly and reversibly inhibited NMDA receptors (half maximal inhibitory concentration = 241 ± 45 mM, mean ± SD; 95% CI, 200 to 281; n = 5) and shifted the glycine concentration–response curve for NMDA-evoked current to the right. Tranexamic acid also inhibited α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (half maximal inhibitory concentration = 231 ± 91 mM; 95% CI, 148 to 314; n = 5 to 6) and kainate receptors (half maximal inhibitory concentration = 90 ± 24 mM; 95% CI, 68 to 112; n = 5). Conclusions Tranexamic acid inhibits NMDA receptors likely by reducing the binding of the co-agonist glycine and also inhibits α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid and kainate receptors. Receptor blockade occurs at high millimolar concentrations of tranexamic acid, similar to the concentrations that occur after topical application to peripheral tissues. Glutamate receptors in tissues including bone, heart, and nerves play various physiologic roles, and tranexamic acid inhibition of these receptors may contribute to adverse drug effects.

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