Glutamate receptor agonist kainic acid. Medical search. Frequent questions

Glutamate is produced by the cell's metabolic processes and there are four major classifications of glutamate receptors: NMDA receptors, AMPA receptors, kainate receptors, and the metabotropic glutamate receptors. (wikipedia.org)
Kainic acid induces seizures via activation of kainate receptors containing the GluK2 subunit and also through activation of AMPA receptors, for which it serves as a partial agonist. (wikipedia.org)
Glutamate receptors (GluRs) can be categorized as ionotropic or metabotropic and subcatergorized by their agonist preferences (NMDA, AMPA or Kainic acid). (labmal.com)
Tetrameric or pentameric combinations of different subunits contributes to the functional diversity of AMPA receptors. (labmal.com)
In general, AMPA receptors mediate fast synaptic current at most excitatory synapses, with stoichiometry characterized by subtype composition. (labmal.com)
Although subunit composition of AMPA receptors varies, they must contain at least one edited GluR2 subunit to be calcium impermeable. (labmal.com)
Relative calcium permeability in AMPA receptor channels may be significant in pathological neurotoxic damage and long term changes in nervous system responses. (labmal.com)
It is now clear that the AMPA subtype of ionotropic glutamate receptors (iGluRs) undergoes a rapid desensitization in response to activation by AMPA receptor agonists. (nih.gov)
This desensitization is inhibited by compounds such as aniracetam and cyclothiazide, which act at a distinct site on the AMPA receptor complex. (nih.gov)
In particular, cyclothiazide greatly potentiates AMPA receptor-mediated depolarizing responses in the hippocampus. (nih.gov)
Nevertheless, these data suggest a role for AMPA receptor-mediated enhancement of norepinephrine release as a mechanism of action for nootropic compounds such as 1-BCP. (nih.gov)
Selective GluR2 lacking AMPA receptor blocker. (abcam.com)
these effects were mediated in part via glutamatergic AMPA/kainate but not NMDA receptor signaling. (uky.edu)
The l-glutamate analogue 18, which showed high affinity as a displacer for kainate and AMPA binding, was also examined for agonist potency for CA1 pyramidal neurons of the rat hippocampal slice preparation. (umn.edu)
It rivaled AMPA as one of the most potent agonists for depolarizing pyramidal neurons in medium containing 2.4 mM Mg +2 ions in which kainate/AMPA receptors are active but NMDA receptors are inhibited (IC 50 = 1.1 μM). (umn.edu)
It was 1 order of magnitude less potent for depolarizing pyramidal neurons under conditions in which kainate/AMPA receptors were inhibited by 10 μM CNQX but NMDA receptors were active in 0.1 mM Mg -2 -containing medium (IC 50 = 10 μM). (umn.edu)
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)
In EAE, excitotoxicity and axonal damage appear to contribute to the pathology of the disease, since -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists of GluRs can ameliorate the neurological deficits associated with the progression of the disease [14]. (healthandwellnesssource.org)
This affect may in part be due to injury of OLs and OPCs which express GluRs of the AMPA and kainate classes and are also susceptible to glutamate-mediated excitotoxicity [15]. (healthandwellnesssource.org)
The α-amino-3-hydroxy-5-methyl-4-isoxazolopropionic acid receptor ( AMPA receptor ) is an ionic glutamate (iGluR) transmembrane receptor. (immune-system-research.com)
Besides, AMPA receptors are responsible for most of the rapid excitatory transmission in the central nervous system. (immune-system-research.com)
Now, we will introduce a selective noncompetitive AMPA receptor antagonist, CP-465022 . (immune-system-research.com)
At first, CP-465022 is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. (immune-system-research.com)
CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes. (immune-system-research.com)
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)
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)

Intrastriatal injections of quinolinic acid, an N -methyl-D-aspartate (NMDA) receptor agonist, selectively affect medium-sized GABA-ergic spiny projection neurons, sparing the striatal interneurons and closely mimicking the neuropathology seen in HD. (medscape.com)
Watkins et al (1990) Experiments with kainate and quisqualate agonists and antagonists in relation to the sub-classification of 'non-NMDA' receptors. (tocris.com)
[17] It inhibits receptor activity in the NMDA glutamate receptor subtypes. (mdwiki.org)

The developmental upregulation of Cx36 is induced by activation of group II metabotropic glutamate receptors (mGluRIIs). (jneurosci.org)

and the effects of EP3 receptor agonists and antagonists on OPC viability were examined. (healthandwellnesssource.org)
In the present study, we examined attenuating effect of serotonin (5-HT) receptor antagonists on the impairment of the time perception presented by daily scheduled feeding in old rats. (eurekamag.com)
Daily injections of 5-HT-2 receptor antagonists, mianserin or ritanserin, or a 5-HT-3 receptor antagonist, Y25130, at 1700 h for 6 consecutive days significantly and dose-dependently attenuated the impairment of mealtime-associated activity on the fasting day in old rats without affecting the food intake. (eurekamag.com)

Kainic acid is a direct agonist of the glutamic kainate receptors and large doses of concentrated solutions produce immediate neuronal death by overstimulating neurons to death. (wikipedia.org)
Thus, in large, concentrated doses kainic acid can be considered a neurotoxin, and in small doses of dilute solution kainic acid will chemically stimulate neurons. (wikipedia.org)
Also, infusion with kainic acid in the hippocampus of animals results in major damage of pyramidal neurons and subsequent seizure activity. (wikipedia.org)
show that synaptically released glutamate acting on mGluRIIs is also required for injury-induced upregulation of Cx36 in mature cortical neurons. (jneurosci.org)
Though glutamate is present in all neurons, only a few are glutamatergic, releasing glutamate as their neurotransmitter. (org.es)
Using immunocytochemical techniques, neurons containing glutamate are identified and labeled with a glutamate antibody. (org.es)
These neurons are believed to release GABA, not glutamate, as their neurotransmitter (Yazulla, 1986), suggesting the weak glutamate labeling reflects the pool of metabolic glutamate used in the synthesis of GABA. (org.es)
Glutamate incorporated into Muller cells is rapidly broken down into glutamine, which is then exported from glial cells and incorporated into surrounding neurons (Pow and Crook, 1996). (org.es)
Isoflurane acts as a positive allosteric modulator of the GABA A receptor in electrophysiology studies of neurons and recombinant receptors. (mdwiki.org)

Ionotropic glutamate antagonist. (abcam.com)
Although the exact pathogenesis of FIRES has not been elucidated, a functional deficiency in the endogenous interleukin-1 receptor antagonist has been implicated in a genetic predisposition to FIRES. (annchildneurol.org)
A crucial role of interleukin-1β (IL-1β) in FIRES has been demonstrated in case reports describing the effective clinical use of anakinra, a recombinant IL-1 receptor antagonist (IL-1Ra) [ 1 , 7 ]. (annchildneurol.org)

Kainic acid is an agonist for kainate receptors, a type of ionotropic glutamate receptor. (wikipedia.org)

More potent and possibly more selective than kainate at kainate receptors, as demonstrated in electrophysiological studies. (tocris.com)
A selective D1 dopamine receptor agonist used primarily as a research tool. (lookformedical.com)

Kainic acid is a potent neuroexcitatory amino acid agonist that acts by activating receptors for glutamate, the principal excitatory neurotransmitter in the central nervous system. (wikipedia.org)
Kainic acid is a potent central nervous system excitant that is used in epilepsy research to induce seizures in experimental animals, at a typical dose of 10-30 mg/kg in mice. (wikipedia.org)

Kainate receptors likely control a sodium channel that produces excitatory postsynaptic potentials (EPSPs) when glutamate binds. (wikipedia.org)
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)
Once released, the neurotransmitter diffuses across the cleft and binds to receptors on the postsynaptic cell, allowing the signal to propagate. (org.es)
Isoflurane likely binds to GABA , glutamate and glycine receptors, but has different effects on each receptor. (mdwiki.org)

AMPAR, together with other members of the ionic glutamate receptor (iGluR) family, N-methyl-D-aspartic acid receptors and kainic acid receptors (NMDARs and KARs), is a cationic permeable receptor tetramer. (immune-system-research.com)

A family of receptors (RECEPTORS, DOPAMINE) mediate its action. (lookformedical.com)
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. (lookformedical.com)
A dopamine D2/D3 receptor agonist. (lookformedical.com)

In 2019, Chekan et al were able to use bioinformatic tools to look for domoic acid gene homologs in the seaweed Digenea simplex. (wikipedia.org)
neuroscience research neurodegenerative agent modeling of epilepsy modeling of Alzheimer's disease Dihydrokainic acid Domoic acid Kainate receptor Carlson NR (2013). (wikipedia.org)
Domoic acid (Cat. (tocris.com)
Domoic acid is a kainate receptor agonist. (tocris.com)
Be the first to review Domoic acid and earn rewards! (tocris.com)
Have you used Domoic acid? (tocris.com)

Whereas NGF promotes neuronal survival, extracellular proNGF can induce apoptosis by binding to receptor complexes comprised of sortilin and the p75 neurotrophin receptor (p75 NTR ), leading to activation of the apoptotic enzyme caspase-3. (jneurosci.org)

Treatment of OPCs with an EP1/EP3 agonist 17 phenyl-trinor PGE2 reversed protection from a COX-2 inhibitor while inhibition of EP3 receptor protected OPCs from excitotoxicity. (healthandwellnesssource.org)

Intrastriatal injections of kainic acid, an agonist of a subtype of glutamate receptor, produce lesions similar to those seen in HD. (medscape.com)

In this study, the effects of 1-BCP on excitatory amino acid agonist-induced [3H]NE release in rat hippocampal slices were determined. (nih.gov)
Neuroactive glutamate is classified as an excitatory amino acid (EAA) because glutamate binding onto postsynaptic receptors typically stimulates, or depolarizes, the postsynaptic cells. (org.es)

Glutamate is incorporated into these cell types through a high affinity glutamate transporter located in the plasma membrane. (org.es)

Excitatory Amino Acids and Synaptic Plasticity. (tocris.com)
Neuroactive glutamate is stored in synaptic vesicles in presynaptic axon terminals (Fykse and Fonnum, 1996). (org.es)
Glutamate transporters maintain the concentration of glutamate within the synaptic cleft at low levels, preventing glutamate-induced cell death (Kanai et al. (org.es)

Additional behavioral data indicated that GLP-1R expressed specifically within the VTA can partially mediate the intake- and body weight-suppressive effects of systemically administered Ex-4, offering the intriguing possibility that this receptor population may be clinically relevant for food intake control. (uky.edu)

However, the notion that allosteric modulators of Sig1R are identified is an additional argument for the "receptor" view of Sig1R. (frontiersin.org)

Expression of MMP-7 (green) decreases and cell death (red) increases in rat hippocampal slices after kainic acid treatment (right). (jneurosci.org)

The syntheses of several novel N-(hydroxydioxocyclobutenyl)-containing analogues of γ-aminobutyric acid and l-glutamate were undertaken to test the hypothesis that derivatives of 3,4-dihydroxy-3-cyclobutene-1,2-dione (squaric acid), such as 3-amino-4-hydroxy-3-cyclobutene-1,2-dione, could serve as a replacement for the carboxylate moiety in neurochemically interesting molecules. (umn.edu)
Compound 18 did not induce sensitization of CA1 pyramidal cells to depolarization by phosphonate analogues of glutamate (the QUIS-effect). (umn.edu)

Excitotoxicity refers to the neurotoxic effect of excitatory amino acids in the presence of excessive activation of postsynaptic receptors. (medscape.com)
Some neuroactive compounds are amino acids, which also have metabolic functions in the presynaptic cell. (org.es)

Kainic acid is utilised in primary neuronal cell cultures and in the acute brain slice preparation to study the physiological effect of excitotoxicity and assess the neuroprotective capabilities of potential therapeutics. (wikipedia.org)
Excitotoxicity originates by massive release of the excitatory neurotransmitter glutamate. (nature.com)

2) Specific neurotransmitter receptors are localized on the postsynaptic cells, and (3) there exists a mechanism to stop neurotransmitter release and clear molecules from the cleft. (org.es)

In addition to inducing seizures, kainic acid is excitotoxic and epileptogenic. (wikipedia.org)
The EP3 receptor was identified as a candidate contributing to OPC excitotoxic death based on pharmacological evidence. (healthandwellnesssource.org)
2, 3] and [4] following induction of glutamate-receptor-mediated excitotoxic death. (healthandwellnesssource.org)
Using this analogy as a framework for the role of COX-2 in death of oligodendrocytes (OLs), we showed that COX-2 is induced in OLs and OPCs following glutamate receptor (GluR) activation and renders these cells more susceptible to excitotoxic death [8]. (healthandwellnesssource.org)
In this study, we examined whether prostanoids (PGs) such as PGE2 and their receptors contribute to excitotoxic death of OPCs. (healthandwellnesssource.org)

Neurotransmitter compounds can be small molecules, such as glutamate and glycine, or large peptides, such as vasoactive intestinal peptide (VIP). (org.es)

This has been supported by the results from double-labeling studies using antibodies to both GABA and glutamate: glutamate-positive amacrine cells also label with the GABA antibodies (Jojich and Pourcho, 1996, Yang, 1996). (org.es)
It is a cyclic derivative of the neurotransmitter GABA [9] and shares the same 2-oxo-pyrrolidone base structure with pyroglutamic acid . (cloudfront.net)

Chemical stimulation, while more complicated than electrical stimulation, has the distinct advantage of activating cell bodies, but not nearby axons, because only cell bodies and subsequent dendrites contain glutamate receptors. (wikipedia.org)
Therefore, chemical stimulation by kainic acid is more localized than electrical stimulation. (wikipedia.org)

This review discusses the similarities and differences between the morphology of astrocytes and astrocytoma cells, and the role that dysregulation in glutamate and calcium signaling plays in the aberrant morphology of astrocytoma cells. (mdpi.com)
Dysregulation of the interleukin-1β-interleukin-1 receptor 1 (IL-1β-IL-1R1) signaling pathway appears to be involved in the pathogenesis of FIRES. (annchildneurol.org)

Glucagon-like peptide-1 receptor (GLP-1R) activation in the ventral tegmental area (VTA) is physiologically relevant for the control of palatable food intake. (uky.edu)

Researchers identified a cluster containing genes identified as the kainic acid biosynthesis (kab) genes. (wikipedia.org)
To confirm production of kainic acid through the identified cluster, Chekan et al expressed the genes in Escherichia coli and validated the enzymatic functions of each proposed gene. (wikipedia.org)
D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES. (lookformedical.com)

Meanwhile, the number and subunit composition of AMPARs at the synapse determines the dynamics of rapid glutamate signaling. (immune-system-research.com)

This transporter selectively accumulates glutamate through a sodium-independent, ATP-dependent process (Naito and Ueda, 1983, Tabb and Ueda, 1991, Fykse and Fonnum, 1996), resulting in a high concentration of glutamate in each vesicle. (org.es)
Water-based solutions of sodium salts of naphthenic acids usually include an excessive alkali, resulting in a high pH value. (mdpi.com)
Bipolar electrodialysis can convert sodium naphthenates into naphthenic acids, but up to a pH of 6.5, the decrease in pH is due to the removal of alkali, which implies that some part of electricity is wasted. (mdpi.com)

Kainic acid is commonly injected into laboratory animal models to study the effects of experimental ablation. (wikipedia.org)
The glutamate receptor agonist kainic acid [21] and the cholinergic agonist pilocarpine [22] are commonly used in SE models. (jle.com)

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)
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)

Our results suggest that the blockade of 5-HT-2 and/or 5-HT-3 receptors attenuates impairment of the manifestation of mealtime-associated anticipatory activity related to temporal learning in old rats. (eurekamag.com)

Kainic acid, or kainate, is an acid that naturally occurs in some seaweed. (wikipedia.org)

Herein, we review possible mechanisms by which glutamate may act in facilitating the growth of projections in astrocytic cells. (mdpi.com)
Together, these data provide novel mechanisms by which GLP-1R agonists in the mesolimbic reward system control for palatable food intake. (uky.edu)

Metabolism of arachidonic acid through cyclooxygenase (COX) enzymes is known to be actively involved in the neuroinflammatory events leading to neuronal death after ischemia. (southampton.ac.uk)

Supply shortages beginning in 2000 have caused the cost of kainic acid to rise significantly. (wikipedia.org)

Perturbed homeostasis of the neurotransmitter glutamate is associated with astrocytoma tumor onset and progression, but the factors that govern this phenomenon are less known. (mdpi.com)
examined the role of PGE2 receptor signaling in EAE and identified a role for EP2 and EP4 in peripheral immune response and increase of bloodCbrain barrier permeability in the initiation and progression of monophasic EAE using global knockouts of PG receptors [13]. (healthandwellnesssource.org)

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AMPA27

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