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Class of ionotropic glutamate receptors
Kainate receptors, or kainic acid receptors (KARs), are ionotropic receptors that respond to the neurotransmitter glutamate. They were first identified
Kainate_receptor
Chemical compound
than AMP receptors. In general, the function of kainate receptors is much less characterized than AMPA receptors. Interestingly, kainate receptors are expressed
Willardiine
Protein-coding gene in the species Homo sapiens
Glutamate ionotropic receptor kainate type subunit 2, also known as ionotropic glutamate receptor 6 or GluR6, is a protein that in humans is encoded by
GRIK2
Chemical compound
glutamate receptors: NMDA receptors, AMPA receptors, kainate receptors, and the metabotropic glutamate receptors. Kainic acid is an agonist for kainate receptors
Kainic_acid
Protein-coding gene in the species Homo sapiens
Glutamate receptor, ionotropic, kainate 1, also known as GRIK1, is a protein that in humans is encoded by the GRIK1 gene. This gene encodes one of the
GRIK1
Protein-coding gene in the species Homo sapiens
Glutamate receptor, ionotropic kainate 5 is a protein that in humans is encoded by the GRIK5 gene. This gene encodes a protein that belongs to the glutamate-gated
GRIK5
Neuron membrane protein
plasticity. They are activated by the drug kainate and are permeable to both sodium and potassium ions. Kainate receptors are expressed in a variety of brain
Glutamate_receptor
Ligand-gated ion channels
and sequence similarity: AMPA receptors, kainate receptors, NMDA receptors and delta receptors (see below). AMPA receptors are the main charge carriers
Ionotropic_glutamate_receptor
Spanish neuroscientist and research professor
Morales, M; Lerma, J (1995). "Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons". Neuron. 14 (1):
Juan_Lerma_Gómez
Amino acid
the micromolar range, including the AMPA and kainate receptors and, to a lesser extent, the NMDA receptor. It acts as an antagonist of the former two sites
Theanine
Protein-coding gene in the species Homo sapiens
GRIK4 (glutamate receptor, ionotropic, kainate 4) is a kainate receptor subtype belonging to the family of ligand-gated ion channels which is encoded by
GRIK4
Transmembrane protein family
Gouaux E (October 1998). "Structure of a glutamate-receptor ligand-binding core in complex with kainate". Nature. 395 (6705): 913–7. Bibcode:1998Natur.395
AMPA_receptor
Class of depressant drugs derived from barbituric acid
this receptor. In addition to this GABAergic effect, barbiturates also block AMPA and kainate receptors, subtypes of ionotropic glutamate receptor. Glutamate
Barbiturate
Protein-coding gene in the species Homo sapiens
Glutamate receptor, ionotropic kainate 3 is a protein that in humans is encoded by the GRIK3 gene. This gene encodes a protein that belongs to the ligand-gated
GRIK3
Chemical compound
NS102 is a kainate receptor antagonist. NS102 at Sigma-Aldrich Johansen, Tina H; Drejer, Joergen; Watjen, Frank; Nielsen, Elsebet O (1993). "A novel non-NMDA
NS102
Class of cell surface receptors coupled to G-protein-associated intracellular signaling
Notable exceptions include GABAA receptor, 5-HT3 serotonin receptor and glutamate receptors (NMDAR, AMPAR and kainate receptor), which are ion channels. Regulation
G_protein-coupled_receptor
Anion of glutamic acid in its role as a neurotransmitter
ionotropic glutamate receptors consist of AMPA receptors, NMDA receptors, and kainate receptors. The metabotropic glutamate receptors consist of eight different
Glutamate_(neurotransmitter)
Glutamate receptor and ion channel protein found in nerve cells
is one of three types of ionotropic glutamate receptors, the other two being AMPA and kainate receptors. Depending on its subunit composition, its ligands
NMDA_receptor
Chemical compound
the AMPA and kainate subtypes of the ionotropic glutamate receptor family, with selectivity for the GluR5 subtype of the kainate receptor. It has neuroprotective
Tezampanel
Class of anesthetics
NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the N-methyl-D-aspartate receptor (NMDAR). They are commonly
NMDA_receptor_antagonist
Barbiturate general anesthetic
acetylcholine receptor (nAChR), the 5-HT3 receptor, the glycine receptor and others. Surprisingly, while GABAA receptor currents are increased by barbiturates
Sodium_thiopental
Medication used to treat low blood sugar and high blood pressure
positive allosteric modulator of the ionotropic glutamate AMPA and kainate receptors. The elimination half-life of diazoxide has been reported to be 24
Diazoxide
Chemical compound
amygdaloid nucleus. It damages the neurons by activating AMPA and kainate receptors, causing an influx of calcium. Although calcium flowing into cells
Domoic_acid
Chemical compound
5-Fluorowillardiine is a selective agonist for the AMPA receptor, with only limited effects at the kainate receptor. It is an excitotoxic neurotoxin when used in
5-Fluorowillardiine
Chemical compound
quinoxalinedione series which acts as a competitive antagonist of the AMPA and kainate receptors and, as of 2015, is being investigated in clinical trials by Novartis
Selurampanel
Chemical compound
as a weak agonist of the glycine receptor and of both NMDA and non-NMDA (AMPA/kainate) ionotropic glutamate receptors. It has been proposed to be a potential
Proline
Chemical compound
modulator of the AMPA and kainate receptors, capable of reducing or essentially eliminating rapid desensitization of the former receptor, and potentiating AMPA-mediated
Cyclothiazide
Protein molecule receiving signals for a cell
In biochemistry and pharmacology, receptors are proteins that receive and transduce signals that may be integrated into biological systems. These signals
Receptor_(biochemistry)
Chemical compound
for the kainate receptor. This potent agonist has nearly 3,000 fold- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors, respectively
SYM-2081
Short-acting barbiturate
barbiturates, pentobarbital binds to the barbiturate-binding site on the GABAA receptor. This action increases the duration of ion-channel opening. At high doses
Pentobarbital
Spice made from crocus flowers
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
Saffron
Chemical compound
glutamate receptor antagonist, which is a non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA-, kainate- and NMDA-induced
GYKI_52466
Chemical compound
3-dione) is a competitive antagonist at AMPA and kainate receptors, two ionotropic glutamate receptor (iGluR) subfamilies. It is used in a variety of molecular
DNQX
Medication used to treat epilepsy and migraine
channels, high-voltage-activated calcium channels, GABAA receptors, AMPA/kainate receptors, and carbonic anhydrase isoenzymes. There is evidence that
Topiramate
Chemical compound
addition to its actions at the NMDA receptor, licostinel also acts as an antagonist of the AMPA and kainate receptors at high concentrations (Kb = 0.9 μM
Licostinel
Naturally occurring glutamate receptor agonist neurotoxin
glutamate receptors, strongly activating NMDA, group I and II metabotropic glutamate receptors, and weakly activating AMPA and kainate receptors. Taken systemically
Ibotenic_acid
Chemical compound
selective agonist for some kainate receptor subunits with only limited effects at AMPA receptors. It activates kainate receptors containing GluK1 (GluR5)
5-Iodowillardiine
Chemical compound
is an agonist of the AMPA, kainate, and group I metabotropic glutamate receptors. It is one of the most potent AMPA receptor agonists known. It causes
Quisqualic_acid
Chemical compound
better known as AMPA, is a compound that is a specific agonist for the AMPA receptor, where it mimics the effects of the neurotransmitter glutamate. There are
AMPA
Chemical compound
antagonist of the AMPA receptor. NBQX blocks AMPA receptors in micromolar concentrations (~10–20 μM) and also blocks kainate receptors. In experiments, it
NBQX
Blue dye also used as a medication
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
Methylene_blue
Pharmacodynamics and pharmacokinetics of ethanol
allosteric modulator Kainate receptor: negative allosteric modulator Glycine receptor: positive allosteric modulator Serotonin 5-HT3 receptor: positive allosteric
Pharmacology_of_ethanol
Amino acid derivative
and regulates the NMDA receptor and has no effect on other glutamate receptors (such as those for AMPA and kainate). NMDA receptors are particularly important
N-Methyl-D-aspartic_acid
Dissociative hallucinogenic drug, mostly used recreationally
member of the arylcyclohexylamine class. PCP works primarily as an NMDA receptor antagonist. PCP is most commonly used in the US. While usage peaked in
Phencyclidine
Investigational antimigraine drugs
ionotropic glutamate AMPA and kainate receptor antagonist – migraine [109] Sergolexole (LY-281067) – serotonin 5-HT2 receptor antagonist and ergoline – migraine
List of investigational headache and migraine drugs
List_of_investigational_headache_and_migraine_drugs
Chemical compound
modulator of the AMPA and kainate receptors and as an inhibitor of vesicular glutamate transporters. It also acts on P2 receptors. It was named after Herbert
Evans_blue_(dye)
Chemical compound
cyanquixaline (6-cyano-7-nitroquinoxaline-2,3-dione) is a competitive AMPA/kainate receptor antagonist. Its chemical formula is C9H4N4O4. CNQX is often used in
CNQX
Experimental antidepressant
(PAM) of the AMPA receptor. Osavampator and other AMPA PAMs potentiate the effects of agonists at the main site of the AMPA receptor by slowing the rate
Osavampator
Chemical compound
reversibly inhibit AMPA (also called the "quisqualate receptor"), kainate, and NMDA ionotropic glutamate receptors (iGluRs). Philanthotoxins have a hydrophobic
Philanthotoxin
Chemical compound
on glutamate receptors, such as NMDA, calcium-dependent AMPA, and kainate receptors. The activation of the metabotropic glutamate receptor 5 is believed
Β-Methylamino-L-alanine
Chemical compound
UBP-302 is a highly selective kainate receptor antagonist used in the study of many neurological processes. It is active at micromolar concentration within
UBP-302
Chemical compound
and Kainate glutamate receptors in the concentration range of 0.1-2.5 mM. As a noncompetitive antagonist at the glycine site of the NMDA receptor. As
Kynurenic_acid
Chemical compound
of tezampanel and thereby competitive antagonist of the AMPA and kainate receptors which was under development by Raptor Pharmaceuticals/Torrey Pines
Dasolampanel
Australian-born vision scientist
Venkataramani, S., Gayet-Primo, J., Grünert, U., & Taylor, W. R. (2014). Kainate Receptors Mediate Synaptic Input to Transient and Sustained OFF Visual Pathways
Teresa_Puthussery
Combination medication
metoprolol, and tamoxifen. Dextromethorphan acts as an NMDA receptor antagonist, σ1 receptor agonist, and serotonin–norepinephrine reuptake inhibitor, among
Dextromethorphan/bupropion
Medication used to treat ADHD
affinity for opioid receptors, acting as an antagonist at the μ-opioid receptor (MOR) and as a partial agonist at the κ-opioid receptor (KOR). The affinities
Atomoxetine
Medication of the barbiturate type
neuron will be increased. Direct blockade of glutamatergic AMPA and kainate receptors are also believed to contribute to the hypnotic/anticonvulsant effect
Phenobarbital
Dissociative anesthetic and anti-depressant
Ketamine is a cyclohexanone-derived general anesthetic and NMDA receptor antagonist with analgesic and hallucinogenic properties, used medically for anesthesia
Ketamine
Class of intracellular transport proteins
Ryanodine receptors (RyR) are classified as high-conductance, intracellular calcium release channels, typically present in the membrane of the sarcoplasmic
Ryanodine_receptor
Chemical compound
useful to isolate the action of other glutamate receptors in the brain, i.e., AMPA and kainate receptors. AP5 can block the conversion of a silent synapse
AP5
Persistent and intrusive thoughts about food
effects of glucagon-like peptide-1 receptor signaling in the ventral tegmental area are mediated by AMPA/kainate receptors". American Journal of Physiology
Food_noise
Investigational cognition and memory disorder drugs
ionotropic glutamate AMPA receptor agonists, ionotropic glutamate kainate receptor antagonists, and metabotropic glutamate mGlu2 receptor modulators [45] Research
List of investigational cognition and memory disorder drugs
List_of_investigational_cognition_and_memory_disorder_drugs
Obsolete anaesthetic
5-HT3 receptors, and as a negative allosteric modulator of the AMPA, kainate, and NMDA receptors, as well as of nicotinic acetylcholine receptors. Clinically
Enflurane
Chemical compound
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
3-Methyl-PCP
Spider toxin
especially potent at kainate receptors and AMPA receptors, with inhibitory potencies summarised in the table: The inhibition of kainate receptors by NPTX-8 is
Nephila_polyamine_toxin_8
Molecule used to overcome antibiotic resistance in bacteria
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
Clavulanic_acid
Investigational substance-related disorder drugs
Tezampanel (LY-293558; NGX-424; PRN-001-01) – ionotropic glutamate AMPA and kainate receptor antagonist – opioid-related disorders Zabaglurant (Heptares 25; HTL-0014242;
List of investigational substance-related disorder drugs
List_of_investigational_substance-related_disorder_drugs
Diuretic medication
HCT (with fosinopril), Lotensin HCT (with benazepril), etc. Angiotensin receptor blockers – e.g. Hyzaar (with losartan), Co-Diovan or Diovan HCT (with valsartan)
Hydrochlorothiazide
Medication used to treat overdose of paracetamol
redox state of the NMDA receptor complex. In addition, glutathione has been found to bind to and activate ionotropic receptors that are different from
Acetylcysteine
Affecting glutamate systems in the brain
or brain. Examples include: Excitatory amino acid receptor agonists Excitatory amino acid receptor antagonists Excitatory amino acid reuptake inhibitors
Glutamatergic
Medication
anxiolytic. Aniracetam has been shown to positively modulate the AMPA receptor. When ingested orally aniracetam is quickly broken down via first pass
Aniracetam
Chemical compound
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
2F-NENDCK
Drug that induces convulsions
and an agonist for kainate receptors in the brain which makes it a potent neurotoxin and excitant.[citation needed] GABAA receptor antagonists are drugs
Convulsant
Dissociative anesthetic designer drug
the highest affinity for the NMDA receptor, it also binds with submicromolar affinity to the σ1 receptor, σ2 receptor, and dopamine transporter. Diphenidine
Diphenidine
Amino acid
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
Glutamine
Ubiquitous antioxidant compound in living organisms
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
Glutathione
Chemical compound
where it binds to its receptor, which is a calcium channel located in the endoplasmic reticulum. When IP3 binds its receptor, calcium is released into
Inositol_trisphosphate
Chemical element with atomic number 12 (Mg)
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
Magnesium
Investigational tinnitus drugs
[13] Selurampanel (BGG-492; BGG-492A) – ionotropic glutamate AMPA and kainate receptor antagonist [14] Sodium phenylbutyrate slow-release (4-PB-D-alanin;
List of investigational tinnitus drugs
List_of_investigational_tinnitus_drugs
Branch of neuroscience
receptors can include NMDA, AMPA, and kainate receptors. These receptors are named after agonists that facilitate glutamate activity. NMDA receptors are
Molecular_neuroscience
Medication used to treat dyskinesia
as a sigma σ1 receptor agonist, nicotinic acetylcholine receptor negative allosteric modulator, dopaminergic agent, and weak NMDA receptor antagonist, among
Amantadine
Chemical compound
array of nuclear and cell surface receptors, and acting as a neurosteroid and modulator of neurotrophic factor receptors. In the United States, DHEA is sold
Dehydroepiandrosterone
Neuroscientist and award-winning author
Swanson G (2015). "Identification of critical functional determinants of kainate receptor modulation by auxiliary protein Neto2". Journal of Physiology. 593
Theanne_Griffith
General anaesthetic
activates 5-HT3 and twin-pore K+ channels. It does not affect the AMPA or kainate receptors. Halothane (2-bromo-2-chloro-1,1,1-trifluoroethane) is a very dense
Halothane
Synthetic opioid pain medication
O-desmethyltramadol (desmetramadol), an opioid with a stronger affinity for the μ-opioid receptor. Tramadol was patented in 1972 and launched under the brand name Tramal
Tramadol
Chemical compound
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
Fluorexetamine
Pharmaceutical compound
central sleep apnea. It is a positive allosteric modulator of the AMPA receptor (ampakine). CX1739 has similar pharmacological effects and favorable safety
CX1739
Chemical compound
and was reasonably selective over other receptors tested including monoamine transporters and opioid receptors. Given its status as a novel psychoactive
MDPCP
Cough suppressant and dissociative drug
"The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan"
Dextromethorphan
Professor of neuroscience
glutamate receptors. There are 3 ionotropic glutamate receptors that Heinemann contributed to differentiating: AMPA receptors, NMDA receptors, and kainate receptors
Stephen_Heinemann
Pharmaceutical drug
Memantine Dextromethorphan acts as a σ1 receptor agonist, serotonin–norepinephrine reuptake inhibitor, and NMDA receptor antagonist, while quinidine is an antiarrhythmic
Dextromethorphan/quinidine
Colourless non-flammable greenhouse gas
channels, weakly inhibits AMPA, kainate, GABAA-ρ and 5-HT3 receptors, and slightly potentiates GABAA and glycine receptors. It also has been shown to activate
Nitrous_oxide
Chemical substance that enables neurotransmission
Voltage- gated Ca++ channel Synaptic vesicle Neurotransmitter transporter Receptor Neurotransmitter Axon terminal Synaptic cleft Dendrite A neurotransmitter
Neurotransmitter
Chemical compound
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
2-Bromodeschloroketamine
Antibiotic medication
(IL-12), which at high levels might antagonize the proinflammatory IL-12 receptor, were elevated over 18 months of treatment, as were levels of soluble vascular
Minocycline
Active ingredient in fermented drinks
neurotransmitter in the brain; by facilitating GABA's actions in the GABAA receptor, alcohol suppresses the activity of the central nervous system. Alcohol
Alcohol_(drug)
Opioid analgesic
higher doses. Methadone is made by chemical synthesis and acts on opioid receptors. Methadone was developed in Germany in the late 1930s by Gustav Ehrhart
Methadone
Pharmaceutical compound
by the glycine receptor antagonist strychnine in vitro. The NMDA receptor antagonists magnesium and DL-AP5, the AMPA and kainate receptor antagonist CNQX
Quisqualamine
Organic chemical compound
Sevoflurane Talampanel; Unknown/unsorted antagonists: Minocycline KARTooltip Kainate receptor Agonists: Main site agonists: 5-Bromowillardiine 5-Iodowillardiine
Diethyl_ether
Chemical compound
receptor. Binding to the target receptor leads to depolarization of the postsynaptic cell. This depolarization subsequently activates NMDA receptors,
Acromelic_acid_A
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