AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPsychiatry and PsychologyPhenomena and Processes
Kainic AcidExcitatory Amino Acid AgonistsSeizuresReceptors, Kainic AcidStatus EpilepticusHippocampusConvulsantsFlurothylN-MethylaspartateNeuronsNeurotoxinsKindling, NeurologicPentylenetetrazoleRats, Sprague-DawleyMedulla OblongataEpilepsy, Temporal LobeReceptors, NeurotransmitterQuinolinic AcidsNitrergic NeuronsIbotenic AcidEpilepsyalpha-MethyltyrosineMossy Fibers, HippocampalReceptors, GlutamateGlutamatesPyrrolidinesVestibular NucleiNerve DegenerationGliosisGlutamic AcidBrainNeuroprotective AgentsQuisqualic AcidPeriaqueductal GrayRats, Wistaralpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic AcidQuinolinic AcidRats, Inbred StrainsDisease Models, AnimalAnticonvulsantsExcitatory Amino AcidsCell DeathNystagmus, PhysiologicReceptors, N-Methyl-D-AspartateMicroinjectionsHyperprolactinemiaInjections, IntraventricularProtein BindingElectroencephalographyDentate GyrusPonsPilocarpineExcitatory Amino Acid AntagonistsCorpus StriatumBehavior, Animal6-Cyano-7-nitroquinoxaline-2,3-dioneAstrocytesNADPH DehydrogenaseQuinoxalinesLimbic System
SeizuresReceptorNeuronalInjectionStatus epilepticusEpilepsyAMPANeuronsAminoReceptorsHippocampusNeurotoxicityExcitatory neurotransmitterProteinsAffinityAspartateOkadaicLigandsExtracellularCholinergicLigandSpecifically bindIonsBrainCompoundsSelectivityMethodsRegulationMembraneCellExhibitSiteFigureDomainTargetEffects
Seizures4
  • Mice homozygous for a conditional allele activated in the brain exhibit reduced fertility, infrequent spontaneous seizures, increased susceptibility to kainic acid-induced seizures and lethality, and increased neuronal excitation. (jax.org)
  • Using immunocytochemistry and ELISA, we investigated the production of interleukin (IL)-1β in the rat hippocampus after focal application of kainic acid inducing electroencephalographic (EEG) seizures and CA3 neuronal cell loss. (jneurosci.org)
  • Ramifications of progesterone against kainic acid-induced seizures may also be sex-specific: in females, progesterone provides anticonvulsant results while in men the effect is certainly proconvulsant (Nicoletti et al. (nos-nop.org)
  • We investigated the two exclusively ketogenic amino acids, L-leucine and L-lysine, and found that only L-leucine potently protects mice when administered prior to the onset of seizures induced by kainic acid injection, but not by inducing ketosis. (johnshopkins.edu)
Receptor14
  • Isomer-specific binding affinity is a result of steric effects between (R)-Willardiine and the binding site on the receptor. (wikipedia.org)
  • Binding causes a conformational change that opens the receptor and allows for positively charged ions, Na+ and/or Ca2+ to enter the cell** (Figure 3). (wikipedia.org)
  • When both the ligand and ion bind, the receptor undergoes a conformational change and the ion channel opens. (wikipedia.org)
  • 100 microM) the receptor binding of tritiated AMPA, kainic acid, or (RS)-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid, the latter being a competitive NMDA antagonist. (ku.dk)
  • Receptor dimerization and autophosphorylation attracts proteins containing Src homology 2 (SH2) or phosphotyrosine binding (PTB) domains including adaptor proteins like FRS2 and GRB2. (springer.com)
  • Truncation of the amitriptyline binding motif on TrkA, but not the corresponding region on TrkB, abolished the receptor homo- and heterodimerization. (drugdiscoveryopinion.com)
  • Amitriptyline was found to bind to a motif in the first leucine-rich motif of the extracellular domain of the TrkA receptor with a Kd of 3 µM, which approximates to the brain concentration achieved when used to treat depression or neuropathic pain. (drugdiscoveryopinion.com)
  • Allosteric modulators of sigma-1 receptor (Sig1R) are described as compounds that can increase the activity of some Sig1R ligands that compete with (+)-pentazocine, one of the classic prototypical ligands that binds to the orthosteric Sig1R binding site. (frontiersin.org)
  • Loss of striatal serotonin synaptic receptor binding induced by kainic. (erowid.org)
  • His Glutamate receptor research includes themes of Amino acid, Glutamic acid, Neurotransmitter, Biophysics and Dopamine. (research.com)
  • His Glutamic acid study combines topics in areas such as Free nerve ending, Calcium metabolism, Mammalian brain, Receptor and Aspartate binding. (research.com)
  • The various areas that Frode Fonnum examines in his Glutamate receptor study include Amino acid, Glutamine, Neurotransmitter, Neuroscience and Metabolism. (research.com)
  • The glutamate receptor agonist kainic acid [21] and the cholinergic agonist pilocarpine [22] are commonly used in SE models. (jle.com)
  • Title: Neurosteroid Binding Sites on the GABA(A) Receptor Complex as Novel Targets for Therapeutics to Reduce Alcohol Abuse and Dependence. (aablocks.com)
Neuronal4
  • There was a statistically significant correlation between the ratio of lesioned to control activity for membrane‐bound COMT and the neuronal marker enzyme glutamate decarboxylase. (psu.edu)
  • On the contrary, knockdown of Sprouty proteins increases proliferation of activated astrocytes and, consequently, reduces secondary brain damage in neuronal lesion models such as kainic acid-induced epilepsy or endothelin-induced ischemia. (springer.com)
  • In mice, amitriptyline was further shown to suppress neuronal apoptosis caused by the neuroexitotoxin, kainic acid, in a TrkA-dependent manner. (drugdiscoveryopinion.com)
  • In a screen of candidate neuronal receptors, D-leucine failed to compete for binding by cognate ligands, potentially suggesting a novel target. (johnshopkins.edu)
Injection4
  • Abstract: The cellular localization of the two forms of catechol‐O‐methyltransferase (COMT) was investigated by measuring their activities in rat striatum following unilateral stereotaxic injection of kainic acid, which causes degeneration of striatal neurons followed by proliferation of astroglial cells. (psu.edu)
  • More recently we have demonstrated that C/EBPβ regulates the expression of several genes involved in inflammatory processes and brain injury [ 14 ] and mice lacking C/EBPβ showed a reduced inflammatory response after kainic acid injection and exhibited a dramatic reduction in pyramidal cell loss in the CA1 and CA3 subfields of the hippocampus [ 15 ]. (biomedcentral.com)
  • Neuroprotection was not limited to models of demyelination, but was also observed in another mouse model of axonal damage (that is, kainic acid injection) and detected in cultured neurons after knockdown of Xpo1, the gene encoding CRM1. (nih.gov)
  • To answer this question, we have analyzed longitudinal variations of FC patterns in the hippocampus in a mouse model of medial temporal lobe epilepsy (MTLE), induced by intra- hippocampal injection of kainic acid (KA), which resembles main features of human MTLE. (jesuscortes.info)
Status epilepticus2
Epilepsy1
  • reduction of cbzr binding was consistently over and above loss of hippocampal volume indicating that atrophy is not the sole determinant of cbzr loss in mesial temporal lobe epilepsy . (brain-knowledge-engine.org)
AMPA7
  • Willardiine analogs have been developed that have different binding affinities for the AMPA and kainate receptors. (wikipedia.org)
  • Willardiine naturally exists as two isomers: (S)-Willardiine (R)-Willardiine Only the (S) isomer has binding affinity for the AMPA and kainate receptors. (wikipedia.org)
  • AMPA receptors are tetrameric transmembrane proteins with distinct amino terminal, ligand binding, and transmembrane domains (Figure 2). (wikipedia.org)
  • However, unlike AMPA receptors, external ions also bind to kainate receptors at the ion binding pocket on the extracellular domain. (wikipedia.org)
  • lt;div class="textblock">We have previously shown that (RS)-2-amino-2-(5-tert-butyl-3-hydroxyisoxazol-4-yl)acetic acid (ATAA) is an antagonist at N-methyl-D-aspartic acid (NMDA) and (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptors. (ku.dk)
  • RS)-2-Amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid (Bu-HIBO, 6) has previously been shown to be an agonist at (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptors and an inhibitor of CaCl2-dependent [3H]-(S)-glutamic acid binding (J. Med. (ku.dk)
  • To elucidate the pharmacological significance of this latter binding affinity, which is also shown by quisqualic acid (3) but not by AMPA, we have now resolved Bu-HIBO via diastereomeric salt formation using the diprotected Bu-HIBO derivative 11 and the enantiomers of 1-phenylethylamine (PEA). (ku.dk)
Neurons1
  • These results indicate that the K m membrane‐bound catechol‐O‐methyltransferase may be localized predominantly in neurons, whereas the high‐K m soluble enzyme is found in glial cells. (psu.edu)
Amino7
  • The seedlings of these plants contain enzymes capable of complex chemical substitutions that result in the formation of free amino acids (See: #Synthesis). (wikipedia.org)
  • Willardiine was first discovered in 1959 by R. Gmelin, when he isolated several free, non-protein amino acids from Acacia willardiana (another name for Mariosousa willardiana) when he was studying how these families of plants synthesize uracilyalanines. (wikipedia.org)
  • The family of willardiine compounds (see: #Analogs) all have a uracil or substituted uracil as the primary amino acid side chain. (wikipedia.org)
  • A potential antiseizure role of dietary protein or of individual amino acids in the ketogenic diet is understudied. (johnshopkins.edu)
  • We have studied the effects of excitatory amino acids on the expression of the c-fos and c-jun mRNA in rat C6 glioma cells. (kyobobook.co.kr)
  • His Choline acetyltransferase research is multidisciplinary, relying on both Glutamate decarboxylase, Acetylcholinesterase, Choline, Aromatic L-amino acid decarboxylase and Nucleus. (research.com)
  • A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. (edu.au)
Receptors4
  • These receptors are found at excitatory synapses and bind glutamate (the major excitatory neurotransmitter) and structurally similar ligands, such as willardiine. (wikipedia.org)
  • Willardiine binds to glutamate receptors at the glutamate binding site in the extracellular ligand binding domain (Figure 2). (wikipedia.org)
  • Many members of this class of receptors occur in the cytoplasm and are transported to the CELL NUCLEUS upon ligand-binding where they signal via DNA-binding and transcription regulation. (edu.au)
  • Cellular receptors that bind the human immunodeficiency virus that causes AIDS. (edu.au)
Hippocampus2
  • Domoic acid has been associated with necrosis of the glutamate-rich hippocampus and amygdala in autopsied cases. (medscape.com)
  • Le Gal La Salle G, Rougon G, Valin A. The embryonic form of neural cell surface molecule (E-NCAM) in the rat hippocampus and its reexpression on glial cells following kainic acid-induced standing epilepticus. (upstream.pk)
Neurotoxicity1
  • Frode Fonnum combines subjects such as Kainic acid and Neurotoxicity with his study of Endocrinology. (research.com)
Excitatory neurotransmitter1
  • Domoic acid (DA) is structurally similar to the excitatory neurotransmitter glutamate. (medscape.com)
Proteins6
  • CCAAT/enhancer-binding protein β (C/EBPβ), is a member of a family of transcription factors consisting of six structurally related basic leucine-zipper DNA-binding proteins. (biomedcentral.com)
  • Furthermore, both forskolin and PMA itself increased the phosphorylation of ERK (extracellular signal regulated kinase) and CREB (cyclicAMP responsible element binding protein) proteins. (kyobobook.co.kr)
  • Binding of a miRNA to a complementary sequence in a target mRNA is mediated by Argonaute proteins leading to degradation of the mRNA or translational inhibition, thereby lowering protein levels in cells [ 7 ]. (researchsquare.com)
  • Aijón, J. (1997) Calcium-binding proteins in the periglomerular region of typical and atypical olfactory glomeruli. (uv.es)
  • Cell surface proteins that bind gastrointestinal hormones with high affinity and trigger intracellular changes influencing the behavior of cells. (edu.au)
  • Cytoplasmic proteins that specifically bind glucocorticoids and mediate their cellular effects. (edu.au)
Affinity1
  • Sig1R is an endoplasmic reticulum membrane protein that, in addition to its promiscuous high-affinity ligand binding, has been shown to have chaperone activity. (frontiersin.org)
Aspartate1
Okadaic1
  • Okadaic acid binds to intestinal epithelial cells and increases their permeability. (medscape.com)
Ligands2
  • The binding of allosteric modulators to a target protein induces a conformational change in the protein structure and changes the activity of orthosteric ligands ( Figure 1 ). (frontiersin.org)
  • Thus, allosteric modulators of Sig1R are described as compounds that can increase the activity of Sig1R ligands that compete with [ 3 H](+)-pentazocine for binding to Sig1R. (frontiersin.org)
Extracellular1
  • They bind to extracellular signaling molecules that migrate through or are transported across the CELL MEMBRANE. (edu.au)
Cholinergic1
  • 3 H]Pirenzepine and (-)-[ 3 H]quinuclidinyl benzilate binding to rat cerebral cortical and cardiac muscarinic cholinergic sites. (arizona.edu)
Ligand1
Specifically bind1
  • Cell surface molecules on cells of the immune system that specifically bind surface molecules or messenger molecules and trigger changes in the behavior of cells. (edu.au)
Ions1
  • Using X-ray crystallography, we analyzed structures of the PA-Nter in complex with luteolin at 2.0 Å resolution and quambalarine B at 2.5 Å resolution, which clearly revealed the binding pose of these polyols coordinated to two manganese ions in the endonuclease active site. (bross-medical.com)
Brain5
  • Rivett, AJ , Francis, A & Roth, JA 1983, ' Distinct Cellular Localization of Membrane‐Bound and Soluble Forms of Catechol‐O‐Methyltransferase in Brain ', Journal of neurochemistry , vol. 40, no. 1, pp. 215-219. (psu.edu)
  • Previous studies from our laboratory indicated that C/EBPβ is implicated in inflammatory process and brain injury, since mice lacking this gene were less susceptible to kainic acid-induced injury. (biomedcentral.com)
  • Unexpectedly, the D-enantiomer of leucine, which is found in trace amounts in the brain, worked as well or better than L-leucine against both kainic acid and 6. (johnshopkins.edu)
  • Serotonin and Lysergic Acid Diethylamide Binding in Rat Brain Membran. (erowid.org)
  • Data from in vitro and animal studies suggest that among the sources of antioxidants, phytochemicals in berry fruits ( e.g. , anthocyanin and caffeic acid) have a beneficial role in brain aging and neurodegenerative disorders because of their anti-oxidative, anti-inflammatory, anti-viral and anti-proliferative properties (Youdim et al. (lww.com)
Compounds2
  • We examined a newly characterized class of compounds that target nucleo-cytoplasmic shuttling by binding to the catalytic groove of the nuclear export protein XPO1 (also known as CRM1, chromosome region maintenance protein 1). (nih.gov)
  • Docking analysis of low-energy poses of the most active compound (as well as their comparison to the binding of an inactive compound) revealed that these compounds reproduced similar binding components to a known PA endonuclease inhibitor and displayed similar binding pose and desired monodentate metal coordination, as was initially envisioned. (bross-medical.com)
Selectivity1
  • Title: High selectivity of the γ-aminobutyric acid transporter 2 (GAT-2, SLC6A13) revealed by structure-based approach. (aablocks.com)
Methods1
  • The toxins responsible for most shellfish poisonings are water-soluble, are heat and acid-stable, and are not inactivated by ordinary cooking methods. (medscape.com)
Regulation1
  • Allosteric regulation is the regulation of protein activity by binding an effector molecule at a site other than the orthosteric or active site of a protein ( Figure 1 ). (frontiersin.org)
Membrane1
  • Membrane‐bound COMT activity was decreased in the lesioned striatum, while soluble COMT activity was increased. (psu.edu)
Cell2
  • We studied measures of molecular signaling and cell death in a model of SE in mice of both sexes, including wild-type and TrkB Shc/Shc mutant mice in which a point mutation (Y515F) of TrkB prevents the binding of Shc to activated TrkB kinase. (jneurosci.org)
  • The mechanism of binding of neural cell adhesion molecules. (upstream.pk)
Exhibit1
  • All six members of this family exhibit a high sequence similarity in their C-terminal DNA binding domain and a more diverge regulatory N-terminus [ 1 , 2 ]. (biomedcentral.com)
Site1
  • The definition of allosteric Sig1R modulators might be artificial due to a lack of information on the orthosteric binding site for Sig1R. (frontiersin.org)
Figure1
  • Willardiine was isolated from Acacia Willardiana and characterized as 3-(1-uracyl)-L-alanine, based on elemental composition and stability in strong acid, which were used to deduce the organic structure of willardiine (Figure 1). (wikipedia.org)
Domain2
  • The binding of BDNF to the ectodomain of TrkB leads to phosphorylation of tyrosines 515 (Y515) and 816 (Y816) in the cytoplasmic domain of TrkB. (jneurosci.org)
  • In this review, the authors summarize the definition of FIRES, IL-1β-IL-1R1 signaling, the nucleotide-binding oligomerization domain the NLRP3 inflammasome, and IL-1 targeted therapy for FIRES. (annchildneurol.org)
Target1
  • It was envisioned that aromatic groups introduced to this scaffolds via metal-catalyzed N-arylation (Buchwald-Hartwig or Chan-Evans-Lam) would contribute to lipophilic binding to the target and one of the imidazoline nitrogen atoms would ensure non-chelating coordination to the prosthetic divalent metal ion. (bross-medical.com)
Effects1
  • The neuroprotective effects of berry fruits on neurodegenerative diseases are related to phytochemicals such as anthocyanin, caffeic acid, catechin, quercetin, kaempferol and tannin. (lww.com)