Journal ArticleDOI
Histamine Potentiates N-Methyl-d-aspartate Receptors by Interacting with an Allosteric Site Distinct from the Polyamine Binding Site
Aude Burban,Raphaël Faucard,Vincent Armand,Cecile Bayard,Vladimir Vorobjev,Jean-Michel Arrang +5 more
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TLDR
The histamine-induced potentiation of NMDARs occurs in the brain under normal conditions, and histamine does not bind to the polyamine site, but to a distinct entity, the so-called histamine site of the N MDAR.Abstract:
Histamine potentiates activation of native and recombinant N-methyl-d-aspartate receptors (NMDARs), but its mechanisms of action and physiological functions in the brain remain controversial. Using four different models, we have further investigated the histamine-induced potentiation of various NMDAR-mediated responses. In single cultured hippocampal neurons, histamine potentiated NMDA currents. It also potentiated the NMDA-induced increase in intracellular calcium in the absence, as well as with saturating concentrations, of exogenous d-serine, indicating both glycine-dependent and glycine-independent components of its effect. In rat hippocampal synaptosomes, histamine strongly potentiated NMDA-induced [(3)H]noradrenaline release. The profile of this response contained several signatures of the histamine-mediated effect at neuronal or recombinant NMDARs. It was NR2B-selective, being sensitive to micromolar concentrations of ifenprodil. It was reproduced by tele-methylhistamine, the metabolite of histamine in brain, and it was antagonized by impromidine, an antagonist/inverse agonist of histamine on NMDA currents. Up to now, histamine was generally considered to interact with the polyamine site of the NMDAR. However, spermine did not enhance NMDA-induced [(3)H]noradrenaline release from synaptosomes, and the potentiation of the same response by tele-methylhistamine was not antagonized by the polyamine antagonist arcaine. In hippocampal membranes, like spermine, tele-methylhistamine enhanced [(3)H]dl-(E)-2-amino-4-propyl-5-phosphono-3-pentenoic acid (CGP39653) binding to the glutamate site. In contrast, spermine increased nonequilibrium [(3)H]5H-dibenzo[a,d]cyclohepten-5,10-imine (dizocilpine maleate; MK-801) binding, and suppressed [(3)H]ifenprodil binding, whereas histamine and tele-methylhistamine had no effect. In conclusion, the histamine-induced potentiation of NMDARs occurs in the brain under normal conditions. Histamine does not bind to the polyamine site, but to a distinct entity, the so-called histamine site of the NMDAR.read more
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Journal ArticleDOI
Glutamate Receptor Ion Channels: Structure, Regulation, and Function
Stephen F. Traynelis,Lonnie P. Wollmuth,Chris J. McBain,Frank S. Menniti,Katie M. Vance,Kevin K. Ogden,Kasper B. Hansen,Hongjie Yuan,Scott J. Myers,Raymond Dingledine +9 more
TL;DR: This review discusses International Union of Basic and Clinical Pharmacology glutamate receptor nomenclature, structure, assembly, accessory subunits, interacting proteins, gene expression and translation, post-translational modifications, agonist and antagonist pharmacology, allosteric modulation, mechanisms of gating and permeation, roles in normal physiological function, as well as the potential therapeutic use of pharmacological agents acting at glutamate receptors.
Journal ArticleDOI
Pharmacology of Acute PainNMDA receptor subunits: Function and pharmacology
P. Paoletti,J. Neyton +1 more
TL;DR: Given the growing body of evidence that diverse brain disorders implicate different NMDAR subtypes, such as NR2B in pain or NR3A in white matter injury, there is a growing interest in exploiting the pharmacological heterogeneity of N MDARs for the development of novel NMD AR subtype-selective compounds.
Journal ArticleDOI
Norepinephrine ignites local hotspots of neuronal excitation: How arousal amplifies selectivity in perception and memory.
TL;DR: GANE not only reconciles apparently contradictory findings in the emotion-cognition literature but also extends previous influential theories of LC neuromodulation by proposing specific mechanisms for how LC-NE activity increases neural gain.
Journal ArticleDOI
Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels.
Kasper B. Hansen,Lonnie P. Wollmuth,Derek Bowie,Hiro Furukawa,Frank S. Menniti,Alexander I. Sobolevsky,Geoffrey T. Swanson,Sharon A. Swanger,Ingo H. Greger,Terunaga Nakagawa,Chris J. McBain,Vasanthi Jayaraman,Chian-Ming Low,Mark L. Dell’Acqua,Jeffrey S. Diamond,Chad R. Camp,Riley E. Perszyk,Hongjie Yuan,Stephen F. Traynelis +18 more
TL;DR: In this paper, the authors review insights from more than 3 decades of iGluR studies with an emphasis on the progress that has occurred in the past decade, covering structure, function, pharmacology, roles in neurophysiology, and therapeutic implications for all classes of receptors assembled from the subunits encoded by the 18 ionotropic glutamate receptor genes.
Journal ArticleDOI
Modulation of behavior by the histaminergic system: Lessons from HDC-, H3R- and H4R-deficient mice
TL;DR: This review summarizes current knowledge on possible central H4R functions and discusses the clinical relevance of H3R- and HDC-deficient mice, e.g. the role of HDC in Tourette's syndrome.
References
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Journal Article
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Journal ArticleDOI
The physiology of brain histamine.
TL;DR: The central histamine system is involved in many central nervous system functions: arousal; anxiety; activation of the sympathetic nervous system; the stress-related release of hormones from the pituitary and of central aminergic neurotransmitters; antinociception; water retention and suppression of eating.
Journal Article
Ifenprodil discriminates subtypes of the N-methyl-D-aspartate receptor: selectivity and mechanisms at recombinant heteromeric receptors.
TL;DR: In this article, the effects of the atypical N-methyl-D-aspartate (NMDA) receptor antagonist ifenprodil were investigated by voltage-clamp recording of Xenopus oocytes expressing heteromeric NMDA receptors from cloned NR1 and NR2 subunit RNAs.
Journal ArticleDOI
NMDA receptor subunits: function and pharmacology
Pierre Paoletti,Jacques Neyton +1 more
TL;DR: Given the growing body of evidence that diverse brain disorders implicate different NMDAR subtypes, such as NR2B in pain or NR3A in white matter injury, there is a growing interest in exploiting the pharmacological heterogeneity of N MDARs for the development of novel NMD AR subtype-selective compounds.
Journal ArticleDOI
Cooperative modulation of [3H]MK-801 binding to the N-methyl-D-aspartate receptor-ion channel complex by L-glutamate, glycine, and polyamines.
Richard W. Ransom,Nancy L. Stec +1 more
TL;DR: High concentrations of l‐glutamate, glycine, or spermidine produced concentration‐dependent increases in specific [3H]MK‐801 binding due to a reduction in the Kd of the radioligand.