alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
Receptors, AMPA
Benzothiadiazines
Kainic Acid
(2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.
Receptors, Glutamate
Cell-surface proteins that bind glutamate and trigger changes which influence the behavior of cells. Glutamate receptors include ionotropic receptors (AMPA, kainate, and N-methyl-D-aspartate receptors), which directly control ion channels, and metabotropic receptors which act through second messenger systems. Glutamate receptors are the most common mediators of fast excitatory synaptic transmission in the central nervous system. They have also been implicated in the mechanisms of memory and of many diseases.
Receptors, Kainic Acid
Excitatory Amino Acid Antagonists
Receptors, N-Methyl-D-Aspartate
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Glutamic Acid
6-Cyano-7-nitroquinoxaline-2,3-dione
N-Methylaspartate
Synaptic Transmission
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
Hippocampus
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
Synapses
Specialized junctions at which a neuron communicates with a target cell. At classical synapses, a neuron's presynaptic terminal releases a chemical transmitter stored in synaptic vesicles which diffuses across a narrow synaptic cleft and activates receptors on the postsynaptic membrane of the target cell. The target may be a dendrite, cell body, or axon of another neuron, or a specialized region of a muscle or secretory cell. Neurons may also communicate via direct electrical coupling with ELECTRICAL SYNAPSES. Several other non-synaptic chemical or electric signal transmitting processes occur via extracellular mediated interactions.
Neurons
Quisqualic Acid
Ibotenic Acid
2-Amino-5-phosphonovalerate
Rats, Sprague-Dawley
Excitatory Postsynaptic Potentials
Carbocysteine
Patch-Clamp Techniques
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Benzodiazepines
Cycloleucine
Excitatory Amino Acid Agents
Electrophysiology
Receptors, Metabotropic Glutamate
Receptors, Neurotransmitter
Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.
Glutamates
Long-Term Potentiation
Cerebellum
The part of brain that lies behind the BRAIN STEM in the posterior base of skull (CRANIAL FOSSA, POSTERIOR). It is also known as the "little brain" with convolutions similar to those of CEREBRAL CORTEX, inner white matter, and deep cerebellar nuclei. Its function is to coordinate voluntary movements, maintain balance, and learn motor skills.
Amino Acids
Cells, Cultured
Glycine
Dizocilpine Maleate
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
Dendrites
Rats, Wistar
Evoked Potentials
Electrical responses recorded from nerve, muscle, SENSORY RECEPTOR, or area of the CENTRAL NERVOUS SYSTEM following stimulation. They range from less than a microvolt to several microvolts. The evoked potential can be auditory (EVOKED POTENTIALS, AUDITORY), somatosensory (EVOKED POTENTIALS, SOMATOSENSORY), visual (EVOKED POTENTIALS, VISUAL), or motor (EVOKED POTENTIALS, MOTOR), or other modalities that have been reported.
Cerebral Cortex
Calcium
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Membrane Potentials
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
Dose-Response Relationship, Drug
Dimethyl Adipimidate
Pyramidal Cells
Projection neurons in the CEREBRAL CORTEX and the HIPPOCAMPUS. Pyramidal cells have a pyramid-shaped soma with the apex and an apical dendrite pointed toward the pial surface and other dendrites and an axon emerging from the base. The axons may have local collaterals but also project outside their cortical region.
Protein Subunits
Neuronal Plasticity
Brain
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
Bicuculline
GABA Antagonists
Sequence Homology, Amino Acid
Organ Culture Techniques
Spinal Cord
Receptors, GABA-A
Protein Binding
Protein Transport
Seizures
Tetrodotoxin
alpha 1-Antitrypsin
Cell Membrane
Signal Transduction
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Phosphorylation
Binding Sites
Mice, Knockout
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
Receptors, Adrenergic, alpha
One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.
Cloning, Molecular
Models, Neurological
Action Potentials
Base Sequence
Hypoxia-Inducible Factor 1, alpha Subunit
Amino Acid Substitution
The naturally occurring or experimentally induced replacement of one or more AMINO ACIDS in a protein with another. If a functionally equivalent amino acid is substituted, the protein may retain wild-type activity. Substitution may also diminish, enhance, or eliminate protein function. Experimentally induced substitution is often used to study enzyme activities and binding site properties.
Molecular Sequence Data
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
NG-Nitroarginine Methyl Ester
Methyl Parathion
Neurotoxins
Mutation
alpha7 Nicotinic Acetylcholine Receptor
Xenopus laevis
Integrin alpha3beta1
Cell surface receptor for LAMININ, epiligrin, FIBRONECTINS, entactin, and COLLAGEN. Integrin alpha3beta1 is the major integrin present in EPITHELIAL CELLS, where it plays a role in the assembly of BASEMENT MEMBRANE as well as in cell migration, and may regulate the functions of other integrins. Two alternatively spliced isoforms of the alpha subunit (INTEGRIN ALPHA3), are differentially expressed in different cell types.
Integrin alpha4
Structure-Activity Relationship
Sequence Alignment
The arrangement of two or more amino acid or base sequences from an organism or organisms in such a way as to align areas of the sequences sharing common properties. The degree of relatedness or homology between the sequences is predicted computationally or statistically based on weights assigned to the elements aligned between the sequences. This in turn can serve as a potential indicator of the genetic relatedness between the organisms.
Integrin alpha6
An integrin alpha subunit that primarily associates with INTEGRIN BETA1 or INTEGRIN BETA4 to form laminin-binding heterodimers. Integrin alpha6 has two alternatively spliced isoforms: integrin alpha6A and integrin alpha6B, which differ in their cytoplasmic domains and are regulated in a tissue-specific and developmental stage-specific manner.
Neuroprotective Agents
Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids.
Amino Acid Sequence
Escherichia coli
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.
Integrin alpha5beta1
Models, Molecular
Protein Conformation
The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).
Methyl Methanesulfonate
Protein Structure, Tertiary
The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.
Amino Acids, Essential
Mutagenesis, Site-Directed
Integrin alpha4beta1
Integrin alpha4beta1 is a FIBRONECTIN and VCAM-1 receptor present on LYMPHOCYTES; MONOCYTES; EOSINOPHILS; NK CELLS and thymocytes. It is involved in both cell-cell and cell- EXTRACELLULAR MATRIX adhesion and plays a role in INFLAMMATION, hematopoietic cell homing and immune function, and has been implicated in skeletal MYOGENESIS; NEURAL CREST migration and proliferation, lymphocyte maturation and morphogenesis of the PLACENTA and HEART.
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
Peptide Fragments
Interleukin-1alpha
DNA, Complementary
Amino Acid Motifs
Receptors, Adrenergic, alpha-1
Substrate Specificity
Amygdala
Integrin alpha2beta1
An integrin found on fibroblasts, platelets, endothelial and epithelial cells, and lymphocytes where it functions as a receptor for COLLAGEN and LAMININ. Although originally referred to as the collagen receptor, it is one of several receptors for collagen. Ligand binding to integrin alpha2beta1 triggers a cascade of intracellular signaling, including activation of p38 MAP kinase.
Immunohistochemistry
Integrin alpha5
Transfection
Calcium Channels
Voltage-dependent cell membrane glycoproteins selectively permeable to calcium ions. They are categorized as L-, T-, N-, P-, Q-, and R-types based on the activation and inactivation kinetics, ion specificity, and sensitivity to drugs and toxins. The L- and T-types are present throughout the cardiovascular and central nervous systems and the N-, P-, Q-, & R-types are located in neuronal tissue.
Integrin alpha1beta1
Integrin alpha1beta1 functions as a receptor for LAMININ and COLLAGEN. It is widely expressed during development, but in the adult is the predominant laminin receptor (RECEPTORS, LAMININ) in mature SMOOTH MUSCLE CELLS, where it is important for maintenance of the differentiated phenotype of these cells. Integrin alpha1beta1 is also found in LYMPHOCYTES and microvascular endothelial cells, and may play a role in angiogenesis. In SCHWANN CELLS and neural crest cells, it is involved in cell migration. Integrin alpha1beta1 is also known as VLA-1 and CD49a-CD29.
Receptors, Adrenergic, alpha-2
A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.
Amino Acid Transport Systems
Integrin alpha6beta1
A cell surface receptor mediating cell adhesion to the EXTRACELLULAR MATRIX and to other cells via binding to LAMININ. It is involved in cell migration, embryonic development, leukocyte activation and tumor cell invasiveness. Integrin alpha6beta1 is the major laminin receptor on PLATELETS; LEUKOCYTES; and many EPITHELIAL CELLS, and ligand binding may activate a number of signal transduction pathways. Alternative splicing of the cytoplasmic domain of the alpha6 subunit (INTEGRIN ALPHA6) results in the formation of A and B isoforms of the heterodimer, which are expressed in a tissue-specific manner.
Macromolecular Substances
Electrophoresis, Polyacrylamide Gel
Recombinant Fusion Proteins
Peptides
Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.
Integrin alpha6beta4
This intrgrin is a key component of HEMIDESMOSOMES and is required for their formation and maintenance in epithelial cells. Integrin alpha6beta4 is also found on thymocytes, fibroblasts, and Schwann cells, where it functions as a laminin receptor (RECEPTORS, LAMININ) and is involved in wound healing, cell migration, and tumor invasiveness.
Methyl Chloride
Sequence Homology, Nucleic Acid
Integrins
A family of transmembrane glycoproteins (MEMBRANE GLYCOPROTEINS) consisting of noncovalent heterodimers. They interact with a wide variety of ligands including EXTRACELLULAR MATRIX PROTEINS; COMPLEMENT, and other cells, while their intracellular domains interact with the CYTOSKELETON. The integrins consist of at least three identified families: the cytoadhesin receptors(RECEPTORS, CYTOADHESIN), the leukocyte adhesion receptors (RECEPTORS, LEUKOCYTE ADHESION), and the VERY LATE ANTIGEN RECEPTORS. Each family contains a common beta-subunit (INTEGRIN BETA CHAINS) combined with one or more distinct alpha-subunits (INTEGRIN ALPHA CHAINS). These receptors participate in cell-matrix and cell-cell adhesion in many physiologically important processes, including embryological development; HEMOSTASIS; THROMBOSIS; WOUND HEALING; immune and nonimmune defense mechanisms; and oncogenic transformation.
Cattle
Integrin alpha Chains
The alpha subunits of integrin heterodimers (INTEGRINS), which mediate ligand specificity. There are approximately 18 different alpha chains, exhibiting great sequence diversity; several chains are also spliced into alternative isoforms. They possess a long extracellular portion (1200 amino acids) containing a MIDAS (metal ion-dependent adhesion site) motif, and seven 60-amino acid tandem repeats, the last 4 of which form EF HAND MOTIFS. The intracellular portion is short with the exception of INTEGRIN ALPHA4.
Transcription Factors
Transcription, Genetic
Integrin alpha1
Gene Expression Regulation
DNA Primers
Chromatography, High Pressure Liquid
Gene Expression
RNA, Messenger
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Receptors, Nicotinic
One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.
Alpha Rhythm
Estradiol increases spine density and NMDA-dependent Ca2+ transients in spines of CA1 pyramidal neurons from hippocampal slices. (1/683)
To investigate the physiological consequences of the increase in spine density induced by estradiol in pyramidal neurons of the hippocampus, we performed simultaneous whole cell recordings and Ca2+ imaging in CA1 neuron spines and dendrites in hippocampal slices. Four- to eight-days in vitro slice cultures were exposed to 17beta-estradiol (EST) for an additional 4- to 8-day period, and spine density was assessed by confocal microscopy of DiI-labeled CA1 pyramidal neurons. Spine density was doubled in both apical and basal dendrites of the CA1 region in EST-treated slices; consistently, a reduction in cell input resistance was observed in EST-treated CA1 neurons. Double immunofluorescence staining of presynaptic (synaptophysin) and postsynaptic (alpha-subunit of CaMKII) proteins showed an increase in synaptic density after EST treatment. The slopes of the input/output curves of both alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and N-methyl-D-aspartate (NMDA) postsynaptic currents were steeper in EST-treated CA1 neurons, consistent with the observed increase in synapse density. To characterize NMDA-dependent synaptic currents and dendritic Ca2+ transients during Schaffer collaterals stimulation, neurons were maintained at +40 mV in the presence of nimodipine, picrotoxin, and 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX). No differences in resting spine or dendritic Ca2+ levels were observed between control and EST-treated CA1 neurons. Intracellular Ca2+ transients during afferent stimulation exhibited a faster slope and reached higher levels in spines than in adjacent dendrites. Peak Ca2+ levels were larger in both spines and dendrites of EST-treated CA1 neurons. Ca2+ gradients between spine heads and dendrites during afferent stimulation were also larger in EST-treated neurons. Both spine and dendritic Ca2+ transients during afferent stimulation were reversibly blocked by D, L-2-amino-5-phosphonovaleric acid (D,L-APV). The increase in spine density and the enhanced NMDA-dependent Ca2+ signals in spines and dendrites induced by EST may underlie a threshold reduction for induction of NMDA-dependent synaptic plasticity in the hippocampus. (+info)Recurrent mossy fiber pathway in rat dentate gyrus: synaptic currents evoked in presence and absence of seizure-induced growth. (2/683)
A common feature of temporal lobe epilepsy and of animal models of epilepsy is the growth of hippocampal mossy fibers into the dentate molecular layer, where at least some of them innervate granule cells. Because the mossy fibers are axons of granule cells, the recurrent mossy fiber pathway provides monosynaptic excitatory feedback to these neurons that could facilitate seizure discharge. We used the pilocarpine model of temporal lobe epilepsy to study the synaptic responses evoked by activating this pathway. Whole cell patch-clamp recording demonstrated that antidromic stimulation of the mossy fibers evoked an excitatory postsynaptic current (EPSC) in approximately 74% of granule cells from rats that had survived >10 wk after pilocarpine-induced status epilepticus. Recurrent mossy fiber growth was demonstrated with the Timm stain in all instances. In contrast, antidromic stimulation of the mossy fibers evoked an EPSC in only 5% of granule cells studied 4-6 days after status epilepticus, before recurrent mossy fiber growth became detectable. Notably, antidromic mossy fiber stimulation also evoked an EPSC in many granule cells from control rats. Clusters of mossy fiber-like Timm staining normally were present in the inner third of the dentate molecular layer at the level of the hippocampal formation from which slices were prepared, and several considerations suggested that the recorded EPSCs depended mainly on activation of recurrent mossy fibers rather than associational fibers. In both status epilepticus and control groups, the antidromically evoked EPSC was glutamatergic and involved the activation of both AMPA/kainate and N-methyl-D-aspartate (NMDA) receptors. EPSCs recorded in granule cells from rats with recurrent mossy fiber growth differed in three respects from those recorded in control granule cells: they were much more frequently evoked, a number of them were unusually large, and the NMDA component of the response was generally much more prominent. In contrast to the antidromically evoked EPSC, the EPSC evoked by stimulation of the perforant path appeared to be unaffected by a prior episode of status epilepticus. These results support the hypothesis that recurrent mossy fiber growth and synapse formation increases the excitatory drive to dentate granule cells and thus facilitates repetitive synchronous discharge. Activation of NMDA receptors in the recurrent pathway may contribute to seizure propagation under depolarizing conditions. Mossy fiber-granule cell synapses also are present in normal rats, where they may contribute to repetitive granule cell discharge in regions of the dentate gyrus where their numbers are significant. (+info)Differences in the properties of ionotropic glutamate synaptic currents in oxytocin and vasopressin neuroendocrine neurons. (3/683)
Oxytocin (OT) and vasopressin (VP) hormone release from neurohypophysial terminals is controlled by the firing pattern of neurosecretory cells located in the hypothalamic supraoptic (SON) and paraventricular nuclei. Although glutamate is a key modulator of the electrical activity of both OT and VP neurons, a differential contribution of AMPA receptors (AMPARs) and NMDA receptors (NMDARs) has been proposed to mediate glutamatergic influences on these neurons. In the present study we examined the distribution and functional properties of synaptic currents mediated by AMPARs and NMDARs in immunoidentified SON neurons. Our results suggest that the properties of AMPA-mediated currents in SON neurons are controlled in a cell type-specific manner. OT neurons displayed AMPA-mediated miniature EPSCs (mEPSCs) with larger amplitude and faster decay kinetics than VP neurons. Furthermore, a peak-scaled nonstationary noise analysis of mEPSCs revealed a larger estimated single-channel conductance of AMPARs expressed in OT neurons. High-frequency summation of AMPA-mediated excitatory postsynaptic potentials was smaller in OT neurons. In both cell types, AMPA-mediated synaptic currents showed inward rectification, which was more pronounced in OT neurons, and displayed Ca2+ permeability. On the other hand, NMDA-mediated mEPSCs of both cell types had similar amplitude and kinetic properties. The cell type-specific expression of functionally different AMPARs can contribute to the adoption of different firing patterns by these neuroendocrine neurons in response to physiological stimuli. (+info)Clozapine, but not haloperidol, prevents the functional hyperactivity of N-methyl-D-aspartate receptors in rat cortical neurons induced by subchronic administration of phencyclidine. (4/683)
Repeated exposure of rats to the psychotomimetic drug phencyclidine (PCP) markedly increased the response of prefrontal cortical neurons to the glutamate agonist N-methyl-D-aspartate (NMDA) relative to agonist alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid. Moreover, acute challenge by PCP produced a significantly reduced block of NMDA-induced current. In addition, the subchronic administration of PCP reduced significantly the paired-pulse facilitation, accompanied by a significant increase of excitatory postsynaptic current variance. These results suggest that repeated exposure to PCP increased evoked release of excitatory amino acids. The enhanced release of excitatory amino acids evoked by NMDA could explain, at least partly, a hypersensitive response to NMDA and a reduced blockade of the NMDA responses by a PCP challenge in rats exposed repeatedly to PCP. Pretreatment with the atypical antipsychotic drug clozapine, but not the typical antipsychotic drug haloperidol, attenuates the repeated PCP-induced effect. Our results support the hypothesis that clozapine may facilitate NMDA receptor-mediated neurotransmission to improve schizophrenic-negative symptoms and cognitive dysfunction. This novel approach is useful for evaluating the cellular mechanisms of action of atypical antipsychotic drugs. (+info)BIIR 561 CL: a novel combined antagonist of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors and voltage-dependent sodium channels with anticonvulsive and neuroprotective properties. (5/683)
Antagonists of glutamate receptors of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) subtype, as well as of voltage-gated sodium channels, exhibit anticonvulsive and neuroprotective properties in vivo. One can postulate that a compound that combines both principles might be useful for the treatment of disorders of the central nervous system, like focal or global ischemia. Here, we present data on the effects of dimethyl-(2-[2-(3-phenyl-[1,2, 4]oxadiazol-5-yl)-phenoxy]ethyl)-amine hydrochloride (BIIR 561 CL) on neuronal AMPA receptors and voltage-dependent sodium channels. BIIR 561 CL inhibited AMPA receptor-mediated membrane currents in cultured cortical neurons with an IC50 value of 8.5 microM. The inhibition was noncompetitive. In a cortical wedge preparation, BIIR 561 CL reduced AMPA-induced depolarizations with an IC50 value of 10.8 microM. In addition to the effects on the glutamatergic system, BIIR 561 CL inhibited binding of radiolabeled batrachotoxin to rat brain synaptosomal membranes with a Ki value of 1.2 microM. The compound reduced sodium currents in voltage-clamped cortical neurons with an IC50 value of 5.2 microM and inhibited the veratridine-induced release of glutamate from rat brain slices with an IC50 value of 2.3 microM. Thus, BIIR 561 CL inhibited AMPA receptors and voltage-gated sodium channels in a variety of preparations. BIIR 561 CL suppressed tonic seizures in a maximum electroshock model in mice with an ED50 value of 2.8 mg/kg after s.c. administration. In a model of focal ischemia in mice, i.p. administration of 6 or 60 mg/kg BIIR 561 CL reduced the area of the infarcted cortical surface. These data show that BIIR 561 CL is a combined antagonist of AMPA receptors and voltage-gated sodium channels with promising anticonvulsive and neuroprotective properties. (+info)SPD 502: a water-soluble and in vivo long-lasting AMPA antagonist with neuroprotective activity. (6/683)
Accumulating preclinical data suggest that compounds that block the excitatory effect of glutamate on excitatory amino acid receptors may have neuroprotective effects and utility for the treatment of neurodegeneration after brain ischemia. In the present study, the in vitro and in vivo pharmacological properties of the novel glutamate antagonist SPD 502 [8-methyl-5(4-(N,N-dimethylsulfamoyl)phenyl)-6,7, 8,9,-tetrahydro-1H-pyrrolo[3,2-h]-isoquinoline-2, 3-dione-3-O-(4-hydroxybutyric acid-2-yl)oxime] are described. In binding studies, SPD 502 was shown to display selectivity for the [3H]alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-binding site (IC50 = 0.043 microM) compared with the [3H]kainate- (IC50 = 81 microM), [3H]cis-4-phosphonomethyl-2-piperidine carboxylic acid-(CGS 19755), and [3H]glycine-binding sites (IC50 > 30 microM) in rat cortical membranes. In an in vitro functional assay, SPD 502 blocked the AMPA-induced release of [3H]gamma-aminobutyric acid from cultured mouse cortical neurons in a competitive manner with an IC50 value of 0.23 microM. Furthermore, SPD 502 potently and selectively inhibited AMPA-induced currents in cortical neurons with an IC50 value of 0.15 microM. In in vivo electrophysiology, SPD 502 blocked AMPA-evoked spike activity in rat hippocampus after i.v. administration with an ED50 value of 6.1 mg/kg and with a duration of action of more than 1 h. Furthermore, SPD 502 increased the seizure threshold for electroshock-induced tonic seizures in mice at i.v doses of 40 mg/kg and higher. In the two-vessel occlusion model of transient forebrain ischemia in gerbils, SPD 502 (10 mg/kg bolus injection followed by a 10 mg/kg/h infusion for 2 h) resulted in a highly significant protection against the ischemia-induced damage in the hippocampal CA1 pyramidal neurons. (+info)Ethanol inhibition of synaptically evoked kainate responses in rat hippocampal CA3 pyramidal neurons. (7/683)
Many studies have demonstrated that intoxicating concentrations of ethanol (10-100 mM) can selectively inhibit the component of glutamatergic synaptic transmission mediated by N-methyl-D-aspartate (NMDA) receptors while having little or no effect on excitatory synaptic transmission mediated by non-NMDA receptors [i.e., alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) and/or kainate (KA) receptors]. However, until the recent development of highly selective AMPA receptor antagonists, it was not possible to assess the relative contribution of AMPA and KA receptors to non-NMDA receptor-mediated synaptic transmission or to determine whether these glutamate receptor subtypes differed in their sensitivity to ethanol. In the present experiments, we used the highly selective AMPA receptor antagonist LY 303070 to pharmacologically isolate KA receptor-mediated excitatory postsynaptic currents (EPSCs) in rat hippocampal CA3 pyramidal neurons and tested their sensitivity to ethanol. Concentrations of ethanol as low as 20 mM significantly and reversibly depressed KA EPSCs. Ethanol also inhibited KA currents evoked by direct pressure application of KA in the presence of LY 303070, suggesting that this inhibition was mediated by a postsynaptic action. In contrast, ethanol had no effect on AMPA EPSCs in these cells, even at the highest concentration tested (80 mM). Ethanol significantly inhibited NMDA EPSCs in these neurons, but these responses were less sensitive to ethanol than KA EPSCs. These results suggest that in addition to its well-described depressant effect on NMDA receptor-mediated synaptic transmission, ethanol has an even greater inhibitory effect on glutamatergic synaptic transmission mediated by KA receptors in rat hippocampal CA3 pyramidal neurons. (+info)Differential roles of ionotropic glutamate receptors in canine medullary inspiratory neurons of the ventral respiratory group. (8/683)
The relative roles of ionotropic N-methyl-D-aspartate (NMDA) and non-NMDA glutamate receptors in supplying excitatory drive to inspiratory (I) augmenting pattern neurons of the ventral respiratory group were studied in anesthetized, ventilated, paralyzed, and vagotomized dogs. Multibarrel micropipettes were used to record simultaneously single-unit neuronal activity and pressure microeject the NMDA antagonist, 2-amino-5-phosphonovalerate (AP5; 2 mM), the non-NMDA antagonist 2, 3-dihydroxy-6-nitro-7-sulfamoyl-benzo(f)quinoxaline (NBQX; 0.25 mM), and an artificial cerebrospinal fluid vehicle. Ejected volume-rates were measured directly via meniscus level changes. The moving time average of phrenic nerve activity was used to determine respiratory phase durations and to synchronize cycle-triggered histograms of the discharge patterns. Both AP5 and NBQX produced dose-dependent reductions in peak spontaneous I neuronal discharge frequency (Fn). The average (+/- SE) maximum reduction in peak Fn produced by AP5 was 69.1 +/- 4.2% and by NBQX was 47.1 +/- 3.3%. Blockade of both glutamate receptor subtypes nearly silenced these neurons, suggesting that their activity is highly dependent on excitatory synaptic drive mediated by ionotropic glutamate receptors. Differential effects were found for the two glutamatergic antagonists. AP5 produced downward, parallel shifts in the augmenting pattern of discharge, whereas NBQX reduced the slope of the augmenting discharge pattern. These results suggest that time-varying excitatory input patterns to the canine I bulbospinal neurons are mediated by non-NMDA glutamate receptors and that constant or tonic input patterns to these neurons are mediated by NMDA receptors. (+info)
Clinical Spectrum of Encephalitis Associated With Antibodies Against the α-Amino-3-Hydroxy-5-Methyl-4-Isoxazolepropionic Acid...
S)-α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid - CAS 83643-88-3 - Calbiochem CAS 83643-88-3 | 155305
Nerve growth factor rapidly suppresses basal, NMDA-evoked, and AMPA-evoked nitric oxide synthase activity in rat hippocampus in...
Inhibition by adenosine A(2A) receptors of NMDA but not AMPA currents in rat neostriatal neurons<...
Functional reconstitution of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) receptors from rat brain. [Muscimol...
GYKI 53655 | AMPA antagonist | LY 300168 | GYKI53655 | LY300168 | CAS [143692-18-6] | Axon 1374 | Axon Ligand™ with |99% purity...
Distribution of neurones expressing inwardly rectifying and Ca(2+)-permeable AMPA receptors in rat hippocampal slices
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GRIA4
2003). "Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor channels lacking the N-terminal domain". J. ... The R/G site is found at amino acid 769 immediately before the 3-amino-acid-long flip and flop modules introduced by ... Ripellino JA, Neve RL, Howe JR (1998). "Expression and heteromeric interactions of non-N-methyl-D-aspartate glutamate receptor ... These channels are also responsive to the glutamate agonist, alpha-amino-3-hydroxy-5-methyl-4-isoxazolpropionate (AMPA). Some ...
Racetam
Ahmed AH, Oswald RE (March 2010). "Piracetam defines a new binding site for allosteric modulators of alpha-amino-3-hydroxy-5- ... methyl-4-isoxazole-propionic acid (AMPA) receptors". Journal of Medicinal Chemistry. 53 (5): 2197-203. doi:10.1021/jm901905j. ... "Nootropic drugs positively modulate alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-sensitive glutamate receptors in ... 58 (4): 1199-204. doi:10.1111/j.1471-4159.1992.tb11329.x. PMID 1372342. Vavers E, Zvejniece L, Veinberg G, Svalbe B, Domracheva ...
Piracetam
Ahmed AH, Oswald RE (March 2010). "Piracetam defines a new binding site for allosteric modulators of alpha-amino-3-hydroxy-5- ... It is a derivative of the neurotransmitter GABA and shares the same 2-oxo-pyrrolidone base structure with pyroglutamic acid. ... methyl-4-isoxazole-propionic acid (AMPA) receptors". Journal of Medicinal Chemistry. 53 (5): 2197-203. doi:10.1021/jm901905j. ... Piracetam is a cyclic derivative of GABA (gamma-Aminobutyric acid). Related drugs include the anticonvulsants levetiracetam and ...
GRIA1
The GRIA1 belongs to a family of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptors. Each of the members ( ... Ripellino JA, Neve RL, Howe JR (1998). "Expression and heteromeric interactions of non-N-methyl-D-aspartate glutamate receptor ... Leonard AS, Davare MA, Horne MC, Garner CC, Hell JW (July 1998). "SAP97 is associated with the alpha-amino-3-hydroxy-5- ... Leonard AS, Davare MA, Horne MC, Garner CC, Hell JW (1998). "SAP97 is associated with the alpha-amino-3-hydroxy-5- ...
GRIK2
"Amino acid substitutions in the pore helix of GluR6 control inhibition by membrane fatty acids". J. Gen. Physiol. 132 (1): 85- ... Leuschner WD, Hoch W (1999). "Subtype-specific assembly of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor ... Ripellino JA, Neve RL, Howe JR (Jan 1998). "Expression and heteromeric interactions of non-N-methyl-D-aspartate glutamate ... The pre-mRNA of GLUR6 is edited at amino acid positions 567, 571, and 621. The Q/R position, which gets its name as editing ...
LY-503430
August 2003). "LY503430, a novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor potentiator with functional ... allosteric modulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors". The Journal of Pharmacology and ... 3 (3): 181-94. doi:10.2174/1568007043337508. PMID 15180479. O'Neill MJ, Witkin JM (May 2007). "AMPA receptor potentiators: ...
Strictly standardized mean difference
"Inhibition of calcineurin-mediated endocytosis and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors ... Nucleic Acids Research. 36 (14): 4667-79. doi:10.1093/nar/gkn435. PMC 2504311. PMID 18628291. Zhang XHD (2009). "A method for ... 4 (9): e6892. doi:10.1371/journal.pone.0006892. PMC 2731218. PMID 19727391. Malo N, Hanley JA, Carlile G, Liu J, Pelletier J, ... 15 (3): 551-8. doi:10.2307/1266860. JSTOR 1266860. Reiser B, Guttman I (1986). "Statistical inference for of Pr(Y-less-thaqn-X ...
Hit selection
"Inhibition of calcineurin-mediated endocytosis and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors ... Nucleic Acids Research. 36 (14): 4667-79. doi:10.1093/nar/gkn435. PMC 2504311. PMID 18628291. Klinghoffer RA, Frazier J, Annis ... 12 (4): 645-55. doi:10.1177/1087057107300646. PMID 17435171. Zhang XH, Yang XC, Chung N, Gates A, Stec E, Kunapuli P, Holder DJ ... 12 (5): 645-55. doi:10.1177/1087057107300645. PMID 17517904. Zhang XH, Ferrer M, Espeseth AS, Marine SD, Stec EM, Crackower MA ...
Brain-derived neurotrophic factor
This point mutation in the coding sequence, a guanine to adenine switch at position 196, results in an amino acid switch: ... "Brain-derived neurotrophic factor regulates the expression and synaptic delivery of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic ... subunit of the N-methyl-D-aspartate receptor". The Journal of Biological Chemistry. 276 (1): 693-99. doi:10.1074/jbc.M008085200 ... The proteins resulting from mRNA that does get translated, are not trafficked and secreted normally, as the amino acid change ...
Brain-derived neurotrophic factor
... results in an amino acid switch: valine to methionine exchange at codon 66, Val66Met, which is in the prodomain of BDNF.[39][38 ... "Brain-derived neurotrophic factor regulates the expression and synaptic delivery of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic ... "PSD-95 promotes Fyn-mediated tyrosine phosphorylation of the N-methyl-D-aspartate receptor subunit NR2A". Proceedings of the ... as the amino acid change occurs on the portion of the prodomain where sortilin binds; and sortilin is essential for normal ...
Brain-derived neurotrophic factor
... results in an amino acid switch: valine to methionine exchange at codon 66, Val66Met, which is in the prodomain of BDNF.[36][35 ... "Brain-derived neurotrophic factor regulates the expression and synaptic delivery of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic ... subunit of the N-methyl-D-aspartate receptor". The Journal of Biological Chemistry. 276 (1): 693-99. doi:10.1074/jbc.M008085200 ... as the amino acid change occurs on the portion of the prodomain where sortilin binds; and sortilin is essential for normal ...
CSPG4
Stegmüller J, Werner H, Nave KA, Trotter J (February 2003). "The proteoglycan NG2 is complexed with alpha-amino-3-hydroxy-5- ... methyl-4-isoxazolepropionic acid (AMPA) receptors by the PDZ glutamate receptor interaction protein (GRIP) in glial progenitor ... "Phosphorylation of NG2 proteoglycan by protein kinase C-alpha regulates polarized membrane distribution and cell motility". The ... 158 (3): 1324-31. PMID 9013976. Iida J, Meijne AM, Oegema TR, Yednock TA, Kovach NL, Furcht LT, McCarthy JB (March 1998). "A ...
GRIP2
Stegmüller J, Werner H, Nave KA, Trotter J (2003). "The proteoglycan NG2 is complexed with alpha-amino-3-hydroxy-5-methyl-4- ... isoxazolepropionic acid (AMPA) receptors by the PDZ glutamate receptor interaction protein (GRIP) in glial progenitor cells. ... "The carboxyl terminus of the prolactin-releasing peptide receptor interacts with PDZ domain proteins involved in alpha-amino-3- ... hydroxy-5-methylisoxazole-4-propionic acid receptor clustering". Mol. Pharmacol. 60 (5): 916-23. doi:10.1124/mol.60.5.916. PMID ...
S-18986
Bourasset F, Bernard K, Muñoz C, Genissel P, Scherrmann JM (August 2005). "Neuropharmacokinetics of a new alpha-amino-3-hydroxy ... 16 (4): 624-37. doi:10.1038/cdd.2008.188. PMID 19136940. Destot-Wong KD, Liang K, Gupta SK, Favrais G, Schwendimann L, Pansiot ... 202 (1-3): 225-35. doi:10.1007/s00213-008-1301-x. PMID 18762915. S2CID 35139538. Gupta SK, Mishra R, Kusum S, Spedding M, Meiri ... 19 (3): 235-44. doi:10.1097/FBP.0b013e3282feb0c1. PMID 18469541. S2CID 20415746. Kelly SJ, Bernard K, Muñoz C, Lawrence RC, ...
NPTX2
It also plays a role in clustering of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptors ... 50 (3): 329-37. doi:10.1016/j.lungcan.2005.06.011. PMID 16115696. Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The Status ... 31 (4): 940-3. doi:10.1016/j.pnpbp.2007.02.016. PMID 17408830. S2CID 23877321. Poulsen TT, Pedersen N, Perin MS, et al. (2006 ... 35 (3): e9-15. doi:10.1097/MPA.0b013e318153fa42. PMID 17895837. S2CID 31006962. Marui T, Koishi S, Funatogawa I, et al. (2007 ...
AGTPBP1 (gene)
Stasi K, Mitsacos A, Triarhou LC, Kouvelas ED (1997). "Cerebellar grafts partially reverse amino acid receptor changes observed ... the decline in binding occurred for the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA receptor) receptor at ... "The Purkinje cell degeneration 5J mutation is a single amino acid insertion that destabilizes Nna1 protein". Mamm Genome. 17 (2 ... Increases per protein weight were also discerned in the granule cell layer and deep nuclei for alpha-1-adrenergic receptor and ...
Metaplasticity
Gliotransmitters include glutamate, ATP, and, more recently, the amino acid D-serine. Once thought to be glycine itself, D- ... alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and N-methyl-D-aspartate (NMDA), respectively, but they both ... A low alpha/beta ratio causes an increased threshold for cellular excitation via calcium influx and thus favors LTP. There are ... Recent research has found that the calcium-dependent enzyme CaMKII, which exists in an alpha and beta isoform, is key in ...
GYKI-52,466
Neuron 10, 51, (1993) Wilding, T.J., Huettner, J.E., Differential antagonism of alpha-amino-3-hydroxy-5-methyl-4- ... isoxazolepropionic acid-preferring and kainate-preferring receptors by 2,3-benzodiazepines. Mol. Pharmacol. 47, 582, (1995) ... Allosteric regulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionate receptors by thiocyanate and cyclothiazide at a ... Unlike conventional 1,4-benzodiazepines, GYKI-52466 and related 2,3-benzodiazepines do not act on GABAA receptors. Like other ...
IDRA-21
... alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor biophysics and synaptic responses". Molecular ... a benzothiadiazine derivative that enhances cognition by attenuating DL-alpha-amino-2,3-dihydro-5-methyl-3-oxo-4- ... isoxazolepropanoic acid (AMPA) receptor desensitization". The Journal of Pharmacology and Experimental Therapeutics. 272 (1): ... 43 (5): 664-9. doi:10.1002/ana.410430517. PMID 9585363. Nagarajan N, Quast C, Boxall AR, Shahid M, Rosenmund C (November 2001 ...
LY-404,187 - Википедија, слободна енциклопедија
... allosteric modulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors". J. Pharmacol. Exp. Ther. 319 (1 ... Antagonisti: Neselektivni: APICA • EGLU • HYDIA • LY-307,452 • LY-341,495 • MCPG • MGS-0039; mGlu2-selektivni: PCCG-4; mGlu3- ... Agonisti: 5-Jodovilardin • ATPA • Domoična kiselina • Kainska kiselina • LY-339,434 • SYM-2081. Antagonisti: CNQX • DNQX • LY- ... Agonisti: 5-Fluoro-vilardin • AMPA • Domoična kiselina • Kuiskualinska kiselina; Pozitivni alosterni modulatori: Aniracetam • ...
List of MeSH codes (D03)
... urocanic acid MeSH D03.383.129.385 - isoxazoles MeSH D03.383.129.385.025 - alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic ... pyridoxic acid MeSH D03.383.725.450 - 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine MeSH D03.383.725.463 - metyrapone MeSH ... niflumic acid MeSH D03.066.515.635 - pipemidic acid MeSH D03.066.515.650 - piromidic acid MeSH D03.066.515.950 - xanthinol ... pipemidic acid MeSH D03.383.725.547.650 - piromidic acid MeSH D03.383.725.547.900 - 3-pyridinecarboxylic acid, 1,4-dihydro-2,6- ...
AMPA
... kainic acid and N-methyl-D-aspartic acid (NMDA) channels. In the synapse, these receptors serve very different purposes. AMPA ... ISBN 978-0-87893-697-7. Dinh, L; Nguyen T; Salgado H; Atzori M (2009). "Norepinephrine homogeneously inhibits alpha-amino-3- ... AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) is a compound that is a specific agonist for the AMPA receptor, ... hydroxyl-5-methyl-4-isoxazole-propionate- (AMPAR-) mediated currents in all layers of the temporal cortex of the rat". ...
Ketamine
Thermal rearrangements of α-amino methyl ketones". Journal of Organic Chemistry. 30 (9): 2967-72. doi:10.1021/jo01020a019. US ... Seeman P, Guan HC, Hirbec H (August 2009). "Dopamine D2High receptors stimulated by phencyclidines, lysergic acid diethylamide ... the metabolite with negligible affinity for the NMDA receptor but a potent alpha-7 nicotinic receptor antagonist may have ... In any case, it has been elucidated that acute blockade of NMDA receptors in the brain results in an activation of α-amino-3- ...
S-18986
Bourasset F, Bernard K, Muñoz C, Genissel P, Scherrmann JM (August 2005). "Neuropharmacokinetics of a new alpha-amino-3-hydroxy ... 4][5][6][7][8][9][10][11][12] Reference[uredi - уреди , uredi izvor]. *↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a ... Agonisti: 5-Jodovilardin • ATPA • Domoična kiselina • Kainska kiselina • LY-339,434 • SYM-2081. Antagonisti: CNQX • DNQX • LY- ... Antagonisti: Neselektivni: APICA • EGLU • HYDIA • LY-307,452 • LY-341,495 • MCPG • MGS-0039; mGlu2-selektivni: PCCG-4; mGlu3- ...
Ligand-gated ion channel
... aminocyclopropanecarboxylic acid; D-cycloserine; L-aspartate; quinolinate, etc. Partial agonists : N-methyl-D-aspartic acid ( ... Excitatory and Inhibitory Amino Acids". In Sydor A, Brown RY (eds.). Molecular Neuropharmacology: A Foundation for Clinical ... harboring an alpha-helix and 10 beta-strands. Following the ECD, four transmembrane segments (TMSs) are connected by ... Domoic acid, Quisqualic acid, etc. Antagonists: CNQX, Kynurenic acid, NBQX, Perampanel, Piracetam, etc. Positive allosteric ...
cAMP-dependent pathway
The Gs alpha subunit of the stimulated G protein complex exchanges GDP for GTP and is released from the complex.[7] ... "Regulation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor trafficking through PKA phosphorylation of the Glu ... The Gs alpha subunit slowly catalyzes the hydrolysis of GTP to GDP, which in turn deactivates the Gs protein, shutting off the ... In a cAMP-dependent pathway, the activated Gs alpha subunit binds to and activates an enzyme called adenylyl cyclase, which, in ...
AMPA receptor
A 38-amino acid sequence found prior to (i.e., before the N-terminus of) the fourth membranous domain in all four AMPAR ... Leonard AS, Davare MA, Horne MC, Garner CC, Hell JW (July 1998). "SAP97 is associated with the alpha-amino-3-hydroxy-5- ... While the amino acid sequence of the subunit indicated that there seemed to be four transmembrane domains (parts of the protein ... The positively charged amino acid at the critical point makes it energetically unfavourable for calcium to enter the cell ...
Astrocyte
In the past, hyperalgesia was thought to be modulated by the release of substance P and excitatory amino acids (EAA), such as ... December 2017). "Human Astrocytes Transfer Aggregated Alpha-Synuclein via Tunneling Nanotubes". The Journal of Neuroscience. 37 ... N-methyl-D-aspartate) and kainate subtypes of ionotropic glutamate receptors follows. It is the activation of these receptors ... Subsequent activation of AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid), NMDA ( ...
AMPA receptor
A 38-amino acid sequence found prior to (i.e., before the N-terminus of) the fourth membranous domain in all four AMPAR ... Mammen AL, Kameyama K, Roche KW, Huganir RL (December 1997). "Phosphorylation of the alpha-amino-3-hydroxy-5-methylisoxazole4- ... While the amino acid sequence of the subunit indicated that there seemed to be four transmembrane domains (parts of the protein ... Here, A→I editing alters the uncharged amino acid glutamine (Q) to the positively charged arginine (R) in the receptor's ion ...
GRIP2 - ويكيبيديا
Stegmüller J, Werner H, Nave KA, Trotter J (2003). "The proteoglycan NG2 is complexed with alpha-amino-3-hydroxy-5-methyl-4- ... isoxazolepropionic acid (AMPA) receptors by the PDZ glutamate receptor interaction protein (GRIP) in glial progenitor cells. ... "The carboxyl terminus of the prolactin-releasing peptide receptor interacts with PDZ domain proteins involved in alpha-amino-3- ... hydroxy-5-methylisoxazole-4-propionic acid receptor clustering". Mol. Pharmacol. 60 (5): 916-23. PMID 11641419.. الوسيط , ...
Nootropic drugs positively modulate alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-sensitive glutamate receptors in...
... and oxiracetam enhanced alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-stimulated 45Ca2+ influx in primary ... Nootropic drugs positively modulate alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-sensitive glutamate receptors in ... Micromolar concentrations of piracetam, aniracetam, and oxiracetam enhanced alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic ... as the drug changed neither the stimulation of 45Ca2+ influx by kainate or N-methyl-D-aspartate nor the activation of inositol ...
Block of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors by polyamines and polyamine toxins. |...
Block of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors by polyamines and polyamine toxins.. M S ... Block of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors by polyamines and polyamine toxins.. M S ... Block of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors by polyamines and polyamine toxins.. M S ... Block of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors by polyamines and polyamine toxins. ...
S)-AMPA [(S)-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid] - Science PRO
S)-AMPA [(S)-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid]. Código:. ALX-550-016 ... S)-AMPA [(S)-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid] ... S)-AMPA [(S)-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid] ... S)-AMPA [(S)-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid] https://www.sciencepro.com.br/produtos/alx-550-016 https ...
Solubilization, characterization, and partial purification of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-,...
... and partial purification of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-, quisqualate-, kainate-sensitive L- ... Substances mentioned in the article: Detergents; Glutamates; Ibotenic Acid; Polyethylene Glycols; Glutamic Acid; alpha-Amino-3- ... Kainic Acid/pharmacology; Polyethylene Glycols; Quisqualic Acid/pharmacology; Solubility; Synapses/metabolism; alpha-Amino-3- ... Quisqualic Acid, Detergents, Glutamates, Nonidet P-40, alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid, Kainic Acid, ...
Virtual Screening of Indonesian Herbal Database as alpha-Amino-3- Hydroxy-5-Methyl-4 Isoxazolepropionic Acid (AMPA) Antagonist ...
Home / Pharmacogn J, Vol 11, Issue 6, Nov-Dec, 2019 / Virtual Screening of Indonesian Herbal Database as alpha-Amino-3- Hydroxy ... Syahdi RR, Martinah CD, Yanuar A. Virtual Screening of Indonesian Herbal Database as alpha-Amino-3- Hydroxy-5-Methyl-4 ... Virtual Screening of Indonesian Herbal Database as alpha-Amino-3- Hydroxy-5-Methyl-4 Isoxazolepropionic Acid (AMPA) Antagonist ... Virtual Screening of Indonesian Herbal Database as alpha-Amino-3- Hydroxy-5-Methyl-4 Isoxazolepropionic Acid (AMPA) Antagonist ...
Inhibition of [3H]alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid binding by the excitotoxin beta-N-oxalyl-L-alpha...
... beta-diaminopropionic acid. Article date: 1988/1/19 PubMed ID: 2895006 Journal name: European journal of pharmacology (ISSN: ... alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid binding by the excitotoxin beta-N-oxalyl-L-alpha, ... N-Methyl-D-Aspartate; Receptors, Neurotransmitter; Toxins, Biological; oxalyldiaminopropionic acid; Ibotenic Acid; alpha-Amino- ... Kainic Acid, oxalyldiaminopropionic acid, Oxadiazoles, Oxazoles, alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid, ...
Role of spinal cord alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors in complete Freund's adjuvant-induced...
Park, JS, Yaster, M, Guan, X, Xu, JT, Shih, MH, Guan, Y, Raja, SN & Tao, YX 2008, Role of spinal cord alpha-amino-3-hydroxy-5- ... Fingerprint Dive into the research topics of Role of spinal cord alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid ... alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Medicine & Life Sciences ... Role of spinal cord alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors in complete Freunds adjuvant-induced ...
RCSB PDB
for 1MY2
Synaptic background activity enhances the responsiveness of neocortical pyramidal neurons
Fish and chips: functional genomics of social plasticity in an African cichlid fish | Journal of Experimental Biology
N-methyl-D-aspartic acid. POA. pre-optic area. POMC. proopiomelanocortin. RI. reproductive index. T. testosterone. TC. ... alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid. AVP. arginine vasopressin. AVT. arginine vasotocin. BPP. Bayesian ... The role of amino acid neurotransmitters in the regulation of pituitary gonadotropin release in fish. Biochem. Cell Biol. 78, ... gamma-aminobutyric acid. GH. growth hormone. GHRH. growth hormone-releasing hormone. GnRH. gonadotrophin-releasing hormone. GO ...
Frontiers | IGFBP-2 Signaling in the Brain: From Brain Development to Higher Order Brain Functions | Endocrinology
... tumor necrosis factor alpha; IFN-g, interferon gamma; AMPAR, α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor; ... GABAR, gamma-aminobutyric acid receptor; NMDAR, N-methyl-D-aspartate receptor; ECS, electroconvulsive seizure therapy; APP, ... On the other hand, in the neural IGF-IR, a polymer of sialic acid is present and is resistant to neuraminidase catalysis (110, ... It has been reported that the accumulation of high levels of Abeta can be toxic, although the alpha-secretase cleaved amyloid ...
Dodging the cognitive hit of early-life seizures - Healthcanal.com : Healthcanal.com
Neurocrine Biosciences, Inc. (NBIX) Company Profile & Facts - Yahoo Finance
... a D-amino acid oxidase inhibitor for the treatment of negative symptoms of schizophrenia; NBI-1065845, an alpha-amino-3-hydroxy ... is 5.. The pillar scores are Audit: 1; Board: 6; Shareholder Rights: 5; Compensation: 5. ... 5-methyl-4-isoxazole propionic acid potentiator for the treatment of resistant depression; and NBI-1065846, a G protein-coupled ...
A Eukaryotic Specific Transmembrane Segment is Required for Tetramerization in AMPA Receptors | Journal of Neuroscience
2002) Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor channels lacking the N-terminal domain. J Biol ... Here, we find that AMPAR subunits lacking M4 or containing single amino acid substitutions in the specific M4 face no longer ... 2007) N-Methyl-D-aspartate (NMDA) receptor subunit NR1 forms the substrate for oligomeric assembly of the NMDA receptor. J Biol ... we find that subunits lacking M4 or containing single amino acid substitutions along an "interacting" face of the M4 helix that ...
Plus it
2002) Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor channels lacking the N-terminal domain. J Biol ... Here, we find that AMPAR subunits lacking M4 or containing single amino acid substitutions in the specific M4 face no longer ... 2007) N-Methyl-D-aspartate (NMDA) receptor subunit NR1 forms the substrate for oligomeric assembly of the NMDA receptor. J Biol ... we find that subunits lacking M4 or containing single amino acid substitutions along an "interacting" face of the M4 helix that ...
Frontiers | Development of inflammation-induced hyperalgesia and allodynia is associated with the upregulation of extrasynaptic...
This upregulation was manifested as a robust increase in the amplitude of AMPAR-mediated currents 2-3 h post-CFA. These changes ... This upregulation was manifested as a robust increase in the amplitude of AMPAR-mediated currents 2-3 h post-CFA. These changes ... we showed that remarkable hyperalgesia and allodynia developes in 1-3 h after intraplantar CFA injection. By utilizing patch- ... we showed that remarkable hyperalgesia and allodynia developes in 1-3 h after intraplantar CFA injection. By utilizing patch- ...
Regulation of endosomal motility and degradation by amyotrophic lateral sclerosis 2/alsin. - White Rose Research Online
... alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; rab5 GTP-Binding Proteins. ... White Rose Research Online is powered by EPrints 3 which is developed by the School of Electronics and Computer Science at the ... 3 more authors) (2009) Regulation of endosomal motility and degradation by amyotrophic lateral sclerosis 2/alsin. Molecular ...
Epilepsy and Seizures Medication: Anticonvulsants, Other, Anticonvulsants, Barbiturates, Anticonvulsants, Benzodiazepine,...
Perampanel is a noncompetitive antagonist of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate ... Ethosuximide, valproic acid, and lamotrigine in childhood absence epilepsy. N Engl J Med. 2010 Mar 4. 362(9):790-9. [Medline]. ... This agent has multiple mechanisms of action, including (1) inhibition of N-methyl-D-aspartate (NMDA)-associated sodium ... Ramon Diaz-Arrastia, MD, PhD is a member of the following medical societies: Alpha Omega Alpha, American Academy of Neurology, ...
Migraine Headache Medication: Serotonin 5-HT1F Agonists (Ditans), Serotonin 5-HT-Receptor Agonists (Triptans), Ergot...
Antagonization of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)/kainate subtype of the glutamate receptor ... Valproic acid reduces the frequency of migraines. This agent is believed to enhance gamma-aminobutyric acid (GABA) ... Dihydroergotamine is an alpha-adrenergic blocking agent with a direct stimulating effect on smooth muscle of peripheral and ... The drug blocks alpha-adrenergic receptors and depresses the release of hypophyseal and hypothalamic hormones. As a rule, ...
AMPA Receptors
- AMPA Receptor
Summary Report | CureHunter
Amino Acids, Peptides, and Proteins*Proteins: 90489*Carrier Proteins: 11456*Membrane Transport Proteins: 165*Ion Channels: 3653 ... A class of ionotropic glutamate receptors characterized by their affinity for the agonist AMPA (alpha-amino-3-hydroxy-5-methyl- ... hydroxy- 5- methyl- 4- isoxazolepropionic Acid (AMPA) 4. Glutamic Acid (Glutamate) ... Amino Acid Receptors: 22*Glutamate Receptors: 2226*Ionotropic Glutamate Receptors: 173*AMPA Receptors: 888*glutamate receptor ...
Glutamate Receptors
- Glutamate Receptor
Summary Report | CureHunter
Glutamate receptors include ionotropic receptors (AMPA, kainate, and N-methyl-D-aspartate receptors), which directly control ... Excitatory Amino Acid Receptor; Receptor, Glutamate; Excitatory Amino Acid Receptors; Receptors, Excitatory Amino Acid ... human alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid subtype glutamate receptor ... Glutamate receptors include ionotropic receptors (AMPA, kainate, and N-methyl-D-aspartate receptors), which directly control ...
Differences and diversity of autoimmune encephalitis in 77 cases from a single tertiary care center | Springer for Research &...
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor. ANNA. anti-neuronal nuclear antibody ... Human N-methyl D-aspartate receptor antibodies alter memory and behaviour in mice. Brain. 2015;138(Pt 1):94-109.PubMedCrossRef ... gamma-aminobutyric acid receptor. GAD. glutamic acid decarboxylase. GFAP. Glial Fibrillary Acidic Protein ... Anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis in children and adolescents. Ann Neurol. 2009;66(1):11-8.PubMed ...
Peripheral neuropathy in limbic encephalitis with anti‐glutamate receptor antibodies: Case report and systematic literature...
... isoxazolepropionic acid (AMPA) receptor and N‐methyl‐d‐aspartate (NMDA) receptor are known to be the causes of autoimmune ... Alpha‐amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid (AMPA) and N‐methyl‐d‐aspartate (NMDA) receptors are two major ... hydroxy‐5‐methyl‐4‐isoxazolepropionic acid receptor: Case series and review of the literature. JAMA Neurology, 72(10), 1163- ... AMPA, alpha‐amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid; NMDA, N‐methyl‐ ... ...
Schoepfer R[au] - PubMed - NCBI
Subunit dependencies of N-methyl-D-aspartate (NMDA) receptor-induced alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid ( ... Identification of amino acid residues of the NR2A subunit that control glutamate potency in recombinant NR1/NR2A NMDA receptors ... Studying block in cloned N-methyl-D-aspartate (NMDA) receptors.. Ruppersberg JP, Mosbacher J, Günther W, Schoepfer R, Fakler B. ... Subcellular localisation of recombinant alpha- and gamma-synuclein.. Specht CG, Tigaret CM, Rast GF, Thalhammer A, Rudhard Y, ...
The Dynamic Effects of Nicotine on the Developing Brain
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid glutamate receptor. G. gestational day. GABA. Gamma-aminobutyric acid ... N- methyl D-aspartate glutamate receptor. P. postnatal day. SIDS. sudden infant death syndrome. SN. substantia nigra. VTA. ... Belhage B, Hansen GH, Elster L, Schousboe A. Effects of gamma-aminobutyric acid (GABA) on synaptogenesis and synaptic function ... Localization of alpha 7 nicotinic receptor subunit mRNA and alpha-bungarotoxin binding sites in developing mouse somatosensory ...
Gene Info
Piracetam and Piracetam-Like Drugs | SpringerLink
Nootropic drugs positively modulate alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-sensitive glutamate receptors in ... Nefiracetam potentiates N-methyl-D-aspartate (NMDA) receptor function via protein kinase C activation and reduces magnesium ... Nebracetam (WEB 1881FU) prevents N-methyl-D-aspartate receptor-mediated neurotoxicity in rat striatal slices. Jpn J Pharmacol ... 5.. Wheble PC, Sena ES, Macleod MR. A systematic review and meta-analysis of the efficacy of piracetam and piracetam-like ...
Gene Info
CC] alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid selective glutamate receptor complex *[CC] endocytic vesicle ... BP] regulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate selective glutamate receptor activity *[BP] synaptic ... calcium channel, voltage-dependent, gamma subunit 4. 3837002. Incomplete. BC004504. calcium channel, voltage-dependent, gamma ...
NMDAReceptorsAMPAGABANeuronsProteinsGlutamate ReceptorReceptor antagonistsExcitatoryAMPARInhibitorSelectiveSubunitKainatePharmacologyDerivativesNMDArBlockadeSingle amino acidNeuronalProteinSeizuresBrain10.1186OxidaseInhibitorsInhibitionMetabotropicCyclic10.1016MembraneVitroNootropicSerotoninMolecular BiologyMechanismsGluR2LigandAnnotationSplice2002RetinalSubstancesContrastSynthesis2016Piracetam
NMDA25
- L-[3H]Glutamate bound to the solubilized preparation could be effectively displaced by agonists of non-N-methyl-D-aspartate (NMDA) L-glutamate receptors but not by NMDA or alpha-amino-4-phosphonobutyrate. (muscimol.xyz)
- This agent has multiple mechanisms of action, including (1) inhibition of N-methyl-D-aspartate (NMDA)-associated sodium channels, (2) potentiation of GABAergic activity, and (3) inhibition of voltage-sensitive sodium channels. (medscape.com)
- Autoantibodies to the alpha‐amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid ( AMPA ) receptor and N ‐methyl‐ d ‐aspartate ( NMDA ) receptor are known to be the causes of autoimmune encephalitis particularly limbic encephalitis. (pubmedcentralcanada.ca)
- Alpha‐amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid (AMPA) and N ‐methyl‐ d ‐aspartate (NMDA) receptors are two major glutamate receptors and are antigens of patients with autoimmune limbic encephalitis (Lai et al. (pubmedcentralcanada.ca)
- Graph theoretical analysis, in silico modeling, prediction of toxicity, metabolism and synthesis of novel 2-(methyl/phenyl)-3-(4-(5-substituted-1,3,4-oxadiazol-2-yl) phenyl) quinazolin-4(3H)-ones as NMDA receptor inhibitor. (bioportfolio.com)
- Adjuvant N-methyl-D-aspartic acid (NMDA)-enhancing agents, such as GlyT-1 inhibitors and NMDA-glycine site agonists have been demonstrated to be beneficial for chronic schizophrenia patien. (bioportfolio.com)
- Zusätzlich kann diese Methodik verwendet werden, um drei Konformationszustände in der Ligandenbindungsdomäne des N-Methyl-D-aspartat (NMDA) -Rezeptors zu identifizieren. (jove.com)
- We evaluated the effects of NMDA-R Ab on the NMDA- and AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid)-mediated regulation of glutamate. (biomedcentral.com)
- N-methyl-D-Aspartate (NMDA)-Type Glutamate Receptor Autoantibody Disorders - Anti-NMDA-Receptor Encephalitis. (arupconsult.com)
- Anti-N-methyl-D-aspartate (NMDA) encephalitis is a treatment-responsive inflammatory encephalopathic autoimmune disease associated with anti-NMDA receptor antibodies. (arupconsult.com)
- Recognition that dissociative anesthetics block the N-methyl-D-aspartate (NMDA) receptor channel has inspired a search for glutamatergic therapeutic mechanisms because ketamine and phencyclidine are known to induce psychotic-like symptoms in healthy volunteers and exacerbate the symptoms of patients with schizophrenia. (genes2cognition.org)
- In addition to discussing the activation of mGlu2 receptors with mGlu2/3 receptor agonists or mGlu2 receptor positive allosteric modulators (PAMs), we discuss other methods that may potentially modulate circuits with hypofunctional NMDA receptors such as glycine transporter inhibitors and mGlu5 receptor PAMs. (genes2cognition.org)
- The three classes of ionotropic glutamate receptors are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), N-methyl-D-aspartate (NMDA), and kainite. (oregonstate.edu)
- Previous studies have reported that information from carotid chemoreceptors activates sympathetic premotor neurons in the rostral ventrolateral medulla (RVLM) exclusively via N-methyl-D-aspartic acid (NMDA) receptors. (unboundmedicine.com)
- In addition, we found that glutamate synapses onto these interneurons can also be N-methyl-d-aspartate (NMDA)-silent, that is, only AMPA-signaling. (gu.se)
- Kainate, a natural product, is an excitotoxic glutamate analogue produced by an algae, while NMDA is N-methyl-d-aspartate. (axonmedchem.com)
- 4] The Role of N-Methyl-D-Aspartate (NMDA) Receptors in Pain: A Review. (axonmedchem.com)
- [3,4] Transient reduction of GABA A receptor-mediated inhibitory postsynaptic currents (IP-SCs) is thought to play a role in regulating N-methyl-D-aspartate (NMDA) receptor-dependent mechanisms of synaptic plasticity. (asahq.org)
- [3,4] The resulting depolarization can recruit previously inactive receptors, for example, by relieving the magnesium-voltage-dependent block of the NMDA receptor-mediated calcium channel. (asahq.org)
- [3,4] Prolongation of the open-time of the GABA A receptor-chloride channel by pentobarbital [2,11] partially depolarizes the postsynaptic membrane, enhancing conductance at the NMDA receptor-mediated calcium channel. (asahq.org)
- In the presence of the GABA A receptor antagonist picrotoxin, the NMDA receptor antagonist AP-5, and the selective AMPA receptor antagonist GYKI 53655, KA receptor-mediated excitatory postsynaptic currents (KA EPSCs) were revealed. (elsevier.com)
- Vulnerability to N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity occurred prior to their localisation in apposition to pre-synaptic terminals, indicating that excitotoxicity can be mediated by extrasynaptic receptor puncta. (edu.au)
- The N-methyl-D-aspartate (NMDA) receptor forms a cation-selective channel with a high calcium permeability and sensitivity to channel block by extracellular magnesium. (sciencemag.org)
- The density of N-methyl-D-aspartate (NMDA) receptors on membranes prepared from cultured cortical neurons was determined using binding assays with [125I]I-MK-801 after exposure of cultures to antagonists of the NMDA receptor complex. (aspetjournals.org)
- The density of NMDA receptors was also increased after exposure of cells to CGS 19755 and MK-801 but not after exposure to the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)/kainate receptor antagonist 6-cyano-7-nitroquinoxaline-2,3-dione. (aspetjournals.org)
Receptors31
- Block of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors by polyamines and polyamine toxins. (aspetjournals.org)
- Spinal cord α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs) mediate acute spinal processing of nociceptive and non-nociceptive information, but whether and how their activation contributes to the central sensitization that underlies persistent inflammatory pain are still unclear. (elsevier.com)
- α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs) expression level at extrasynaptic sites of neuronal plasma membrane is high throughout the central nervous system (CNS). (frontiersin.org)
- Serotonin 5-HT1F receptor agonists (ie, ditans) do not elicit a vasoconstrictive effect, whereas triptans cause vasoconstriction via agonistic action at 5-HT1B/1D receptors. (medscape.com)
- These drugs are selective serotonin agonists, specifically acting at 5-hydroxytryptamine 1B/1D (5-HT 1B/1D ) receptors on intracranial blood vessels and sensory nerve endings. (medscape.com)
- A selective agonist for serotonin 5-HT1B/1D receptors, naratriptan has higher bioavailability and a longer half-life than sumatriptan, which may contribute to a lower rate of headache recurrences. (medscape.com)
- A selective agonist for serotonin 5-HT1B/1D receptors in cranial arteries, zolmitriptan suppresses the inflammation associated with migraine headaches. (medscape.com)
- A selective agonist for serotonin 5-HT1B/1D receptors in cranial arteries, rizatriptan suppresses the inflammation associated with migraine headaches. (medscape.com)
- A class of ionotropic glutamate receptors characterized by their affinity for the agonist AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid). (curehunter.com)
- Glutamate receptors include ionotropic receptors (AMPA, kainate, and N-methyl-D-aspartate receptors), which directly control ion channels, and metabotropic receptors which act through second messenger systems. (curehunter.com)
- [23] It may also modulate the activity of various neurotransmitter receptors, including the Alpha-7 nicotinic receptor . (wikipedia.org)
- Consistent with this insensitivity to PTX, neither adenosine receptors nor GABA(B) (gamma-aminobutyric acid) receptors, which operate via PTX-sensitive G-proteins, mediate the OGD-induced outward current. (uzh.ch)
- When adenosine receptors or GABA(B) receptors were blocked with 1,3-dipropyl-8-psulphophenylxanthine (DPSPX, 5 microM) or CGP 52 432 (10 microM), respectively, the OGD-induced response was not modified. (uzh.ch)
- Alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptors (AMPARs) undergo constitutive cycling between the intracellular compartment and the cell surface in the central nervous system. (sigmaaldrich.com)
- Blockade of 5-hydroxytryptamine(2A) receptors plays a contributory role in the actions of the second generation of antipsychotic drugs, the so-called atypical antipsychotics. (genes2cognition.org)
- Crystal structure of the GluR2 amino-terminal domain provides insights into the architecture and assembly of ionotropic glutamate receptors. (genes2cognition.org)
- Ionotropic glutamate receptors are functionally diverse but have a common architecture, including the 400-residue amino-terminal domain (ATD). (genes2cognition.org)
- In this study, we examined the possible involvement of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)/kainate receptors in the RVLM on sympathetic chemoreceptor reflex in pentobarbitone anaesthetised, vagotomised and artificially ventilated rats. (unboundmedicine.com)
- The proteoglycan NG2 is complexed with alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors by the PDZ glutamate receptor interaction protein (GRIP) in glial progenitor cells. (wikipedia.org)
- Here, we present structural and functional data on two new positive allosteric modulators of AMPA receptors, phenyl-1,4-bis-alkylsulfonamide (CMPDA) and phenyl-1,4-bis-carboxythiophene (CMPDB). (aspetjournals.org)
- α-Amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors mediate the initial peak of excitatory postsynaptic potentials and are critical for the strengthening and weakening of synapses that underlie the cellular basis of learning and memory. (aspetjournals.org)
- 3] Kainate receptors. (axonmedchem.com)
- Photoinactivation of glutamate receptors by genetically encoded unnatural amino acids. (abcam.com)
- On the other hand, cocaine self-administration and withdrawal increases the surface expression of subunit glutamate receptor 1 (GluA1) of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors at the level of the NAc. (dovepress.com)
- 1. The superficial layers II and III of the entorhinal cortex, which form the main cortical input to the hippocampus, receive a large serotonergic projection from the raphe nuclei and express 5-HT receptors at high density. (mdc-berlin.de)
- 6. We conclude that serotonin potently suppresses excitatory synaptic transmission via 5-HT1A receptors in layers II and III of the medial entorhinal cortex by a presynaptic mechanism. (mdc-berlin.de)
- CAMKII regulates numerous physiological functions, including neuronal synaptic plasticity through the phosphorylation of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-type glutamate (AMPA) receptors. (antibodies-online.com)
- In the present paper, we report the lipid kinase phosphatidylinositol 4-kinase II alpha (PI4KIIalpha) is a novel substrate of GSK3 that regulates trafficking and cell-surface expression of neurotransmitter receptors in neurons. (garvan.org.au)
- Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-type glutamate receptors (AMPARs) at excitatory synapse mediate fast neurotransmission. (hku.hk)
- These asparagines are in a position homologous to the site in the TM2 region (Q/R site) of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors that is occupied by either glutamine (Q) or arginine (R) and that controls divalent cation permeability of the AMPA receptor channel. (sciencemag.org)
- Up-regulation of N-methyl-D-aspartate receptors on cultured cortical neurons after exposure to antagonists. (aspetjournals.org)
AMPA21
- Micromolar concentrations of piracetam, aniracetam, and oxiracetam enhanced alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-stimulated 45Ca2+ influx in primary cultures of cerebellar granule cells. (nih.gov)
- Potentiation by oxiracetam was specific for AMPA receptor-mediated signal transduction, as the drug changed neither the stimulation of 45Ca2+ influx by kainate or N-methyl-D-aspartate nor the activation of inositol phospholipid hydrolysis elicited by quisqualate or (+-)-1-aminocyclopentane-trans-1,3-dicarboxylic acid. (nih.gov)
- These channels are also responsive to the glutamate agonist, alpha-amino-3-hydroxy-5-methyl-4-isoxazolpropionate (AMPA). (wikipedia.org)
- This includes 5 subunits of the glutamate receptor ionotropic AMPA glutamate receptor subunits (Glur2, Glur3, Glur4) and Kainate receptor subunits (Glur5, Glur6). (wikipedia.org)
- α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptor antagonists are of potential interest for the treatment of certain acute and chronic neurodegenerative diseases, including amyotrophic lateral sclerosis. (aspetjournals.org)
- The compound displaced [ 3 H]AMPA from rat cortex membranes with a K i of 107 nM. (aspetjournals.org)
- it is a noncompetitive antagonist of the ionotropic alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptor on postsynaptic neurons. (drugs.com)
- TMHS is structurally similar to other ion channel regulatory subunits such as TARPs (transmembrane alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor regulatory proteins). (scoop.it)
- Perampanel is an orally administered, selective non-competitive AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid)-type glutamate receptor antagonist, discovered and being developed by Eisai. (drugs.com)
- In contrast, the ionotropic alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) response was not affected. (uzh.ch)
- TAK-653 is a potential first-in-class Alpha-Amino-3-Hydroxy-5-Methyl-4-Isoxazole Propionic Acid (AMPA) potentiator. (koreanewswire.co.kr)
- However, microinjection of 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX, a selective AMPA/kainate receptor antagonist, 2 mM, 100 nl) into the RVLM after intravenous MK-801 abolished the hypoxia evoked sympathoexcitatory response. (unboundmedicine.com)
- In the hippocampal CA1 area, glutamate transmission to the developing, but not to the adult, principal neurons is characterized by the presence of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) silent synapses and of AMPA silencing induced by test pulse stimulation (0.03-1 Hz). (gu.se)
- RNA encoding the B subunit of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) subtype of ionotropic glutamate receptor (GluR-B) undergoes a posttranscriptional modification in which a genomically encoded adenosine is represented as a guanosine in the GluR-B complementary DNA. (sciencemag.org)
- It is first and only FDA-approved non-competitive AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor antagonist. (guidetopharmacology.org)
- Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid ( AMPA ) is an artificial glutamate analogue. (axonmedchem.com)
- Importantly, a reduction in PI4KIIalpha expression or phosphorylation increases alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor expression at the surface of hippocampal neurons. (garvan.org.au)
- We found that KA EPSCs are 5-10% of AMPA/KA EPSCs in all layers of the adult mouse IC. (elsevier.com)
- alpha-Amino-3-hydroxy-5- methyl-4-isoxazolepropionic acid (AMPA) receptor (AMPAR) trafficking has been implicated in the changes in synaptic strength at central glutamatergic synapses associated with memory formation. (epfl.ch)
- However, vulnerability to alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor-mediated excitotoxicity was related to localisation ofreceptors at synapses and in spines. (edu.au)
- Casals, N., 2015, "Novel Regulation of the Synthesis of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Subunit GluA1 by Carnitine Palmitoyltransferase 1C (CPT1C) in the Hippocampus. (uic.es)
GABA8
- In addition, we studied the effects of infusion of GABA (gamma-amino-butyric acid) after blockade of the alpha2-delta subunit of voltage-gated calcium channels (VGCC) with pregabalin, to assess the responsiveness of the glutamatergic synapses to exogeneous GABA when the presynaptic release of glutamate was blocked. (biomedcentral.com)
- Glutamate transmission to gamma-aminobutyric acid (GABA)ergic interneurons and to principal neurons differs in various important respects. (gu.se)
- Pubmed ID: 11961124 Acid(B) funzionale gamma-amminobutirrico (recettori GABA(B)) montare da due subunità, GABA(B(1)) e GABA(B(2). (jove.com)
- Piracetam (2-oxo-Pyrrolidine Acetamide) - is a derivative of the neurotransmitter GABA (Gamma Amino Butyric Acid). (anabolicminds.com)
- A LARGE body of evidence suggests that the ([Greek small letter gamma]-aminobutyric acid A (GABA A ) receptor complex is an important cellular target for general anesthetics. (asahq.org)
- According to the anion shift model, [3,4] GABA plays a dual role in the inhibition and facilitation of synaptic transmission ( Figure 1 A). High-frequency stimulation, by increasing GABA release, prolongs the open-time of the GABA ( A ) channel. (asahq.org)
- This effect causes the GABA A reversal potential (E GABA ) to shift from E Cl (hyperpolarized) toward E HCO 3 (depolarized). (asahq.org)
- [3,4] (B) The anion gradient shift mechanism for GABA A receptor-mediated depolarization. (asahq.org)
Neurons6
- By utilizing patch-clamp recording combined with Ca 2+ imaging, we found a significant upregulation of extrasynaptic AMPARs in substantia gelatinosa (SG) neurons of the rat spinal cord 2-3 h after CFA injection. (frontiersin.org)
- 2007). Brain-derived neurotrophic factor regulates the expression and synaptic delivery of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor subunits in hippocampal neurons. (springer.com)
- These results indicate that transplantation of X-box-binding protein 1-transfected neural stem cells can promote stem cell survival and differentiation into dopaminergic neurons, increase dopamine and 3,4-dihydroxyphenylacetic acid levels, reduce α-synuclein aggregation in the substantia nigra, and improve the symptoms of Parkinson's disease in rats. (nrronline.org)
- The ECM modifications in the nervous system are likely achieved by the concerted actions of several different proteases that are secreted by neurons and glial cells [ 4 - 6 ]. (hindawi.com)
- Synaptosome preparations subjected to co-immunoprecipitation studies revealed AMPAR subunits (GluA1 and GluA2/3) binding to both syndecan-3 (a transmembrane HS proteoglycan of neurons) and proheparanase, suggesting their clustering in a functional complex. (hku.hk)
- The density of binding sites for [125I]I-MK-801 was increased by 40-80% after exposure to D-2-amino-5-phosphonopentanoic acid (D-AP5), with no change in the number or viability of neurons. (aspetjournals.org)
Proteins5
- The insulin-like growth factor (IGF) system is a mitogenic protein family that includes IGF-I and IGF-II and six binding proteins (IGFBP-I-IGFBP-6) and is involved in functions from embryonic growth to cell differentiation to homeostasis, mostly mediated by IGF-lR ( 1 - 3 ). (frontiersin.org)
- IGF-l signaling yield through the phosphoinositide 3-kinase (PI3K)-AKT and RAS-extracellular signal-related kinase (ERK) cascades via IGF-IR ( 15 ) while the IGF-IIR induces signaling through G proteins that activate protein kinase C (PKC) and phospholipase C (PLC), ultimately regulates Ca 2+ homeostasis ( 16 ). (frontiersin.org)
- Selective Methyl Labeling of Proteins: Enabling Structural and Mechanistic Studies As Well As Drug Discovery Applications by Solution-State NMR. (bioportfolio.com)
- Escherichia coli expression protocols for selective labeling of methyl groups in proteins have been essential in expanding the size range of targets that can be studied by biomolecular NMR. (bioportfolio.com)
- 1-4 KIF proteins act together with motor proteins from the dynein and myosin superfamilies. (bmj.com)
Glutamate Receptor4
- Glutamate receptor 4 is a protein that in humans is encoded by the GRIA4 gene. (wikipedia.org)
- The inward current induced by the metabotropic glutamate receptor agonist 1 S, 3R-1-aminocyclopentane-1,3-dicarboxylate (1S,3R-ACPD) and the outward current elicited by adenosine or baclofen were strongly or completely attenuated. (uzh.ch)
- Ca2+/calmodulin-dependent protein kinase II binds to and phosphorylates a specific SAP97 splice variant to disrupt association with AKAP79/150 and modulate alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-type glutamate receptor (AMPAR) activity. (abcam.com)
- The glutamate receptor α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptor (AMPAR) is important for synaptic transmission, memory, and learning. (biomedcentral.com)
Receptor antagonists1
- 5. The effects of serotonin on intrinsic properties and EPSPs were partially mimicked by 5-HT1A receptor agonists (+/-)-8-hydroxy-2-(di-n-propylamino)tetralin hydrobromide (8-OH-DPAT) and 5-carboxamido-tryptamine maleate (5-CT), and reduced by 5-HT1A receptor antagonists S-(-)-5-fluoro-8-hydroxy-DPAT hydrochloride (S-UH-301), 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine hydrobromide (NAN-190) and spiperone. (mdc-berlin.de)
Excitatory2
- 3. Serotonin depressed mixed as well as isolated {alpha}-amino-3-hydroxy-5-methyl-4-isoxazole- propionic acid receptor (AMPAR)- and N-methyl-D-aspartic acid receptor (NMDAR)-mediated excitatory postsynaptic potentials/currents (EPSPs/EPSCsapproximately 40 % reduction with 1 microM serotonin). (mdc-berlin.de)
- Recently, authors from two laboratories [3,4] proposed that an anion gradient shift contributes to the excitatory postsynaptic effects of high-frequency stimulation of GABAergic interneurons. (asahq.org)
AMPAR2
- Using approaches to assay the native oligomeric state of AMPAR subunits, we find that subunits lacking M4 or containing single amino acid substitutions along an "interacting" face of the M4 helix that block surface expression no longer tetramerize in either homomeric or heteromeric assemblies. (jneurosci.org)
- This upregulation was manifested as a robust increase in the amplitude of AMPAR-mediated currents 2-3 h post-CFA. (frontiersin.org)
Inhibitor3
- Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies. (bioportfolio.com)
- TAK-831 is a potential first-in-class D-Amino Acid Oxidase (DAAO) inhibitor that has completed multiple Phase I studies and is currently in on-going Phase II studies, including the Phase II INTERACT proof-of-concept study in negative symptoms of schizophrenia. (koreanewswire.co.kr)
- This study investigated the effects of daily intraperitoneal injections of N-methyl-D-aspartate receptor antagonist MK-801 and nitric oxide synthase inhibitor nitro-L-arginine (L-NA) on the survival of retinal ganglion cells (RGCs) at 1 and 2 weeks after unilateral optic nerve transection in adult hamsters. (nrronline.org)
Selective2
- A selective 5-HT1B/1D receptor agonist, almotriptan results in cranial vessel constriction, inhibition of neuropeptide release, and reduced pain transmission in trigeminal pathways. (medscape.com)
- Discovery and Development of N-4-(l-Cyclobutylpiperidin-4-yloxy) phenyl-2-(morpholin-4-yl) acetamide dihydrochloride (SUVN-G3031): A Novel, Potent, Selective and Orally Active Histamine H3 Receptor Inverse Agonist with Robust Wake-Promoting Activity. (bioportfolio.com)
Subunit3
- Each subunit is composed of four domains: an amino-terminal domain, a ligand-binding core or domain (LBC or LBD) to which both agonists and allosteric modulators bind, the membrane spanning domains (M1, M3, and M4) and a re-entrant pore loop (M2), and the cytoplasmic domain. (aspetjournals.org)
- After their initial expression, the MAP1A and MAP1B polypeptides are cleaved into light and heavy chains, which are then assembled into mature complexes together with the separately encoded light chain 3 subunit (LC3). (biomedcentral.com)
- Regulation of {alpha}-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor trafficking through PKA phosphorylation of the Glu receptor 1 subunit. (semanticscholar.org)
Kainate2
- Solubilization, characterization, and partial purification of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-, quisqualate-, kainate-sensitive L-glutamate binding sites from porcine brain synaptic junctions. (muscimol.xyz)
- The rank order for the competitive ligands in displacing L-[3H]glutamate was: quisqualate greater than alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid greater than L-glutamate greater than kainate. (muscimol.xyz)
Pharmacology1
- Importanza Del Recettore Gamma-amminobutirrico Acid(B) C-termini Per Accoppiamento G-proteina Molecular Pharmacology. (jove.com)
Derivatives2
- Subgroup 3 includes piracetam derivatives with unknown clinical efficacies, and of these nefiracetam failed to improve cognition in post-stroke patients and rolipram is currently in clinical trials as an antidepressant. (springer.com)
- Then a series of 5-(pyrimidin-2-ylamino)picolinonitrile derivatives as CHK1 inhibitors were discovered by further rational optimization. (bioportfolio.com)
NMDAr2
- Since the discovery of N-methyl-D-aspartate receptor (NMDAr) antibody by Dalmau et al. (springer.com)
- The N-methyl-D-aspartate receptor (NMDAR) is a principal subtype of glutamate-gated ion channel and plays key roles in neuronal plasticity and memory functions. (springer.com)
Blockade1
- The picrotoxin-mediated effect on M1 mACh receptor responsiveness was completely prevented by alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor blockade. (sigmaaldrich.com)
Single amino acid1
- section describes the interaction between a single amino acid and another chemical entity. (uniprot.org)
Neuronal2
- Although subgroup 2 compounds act via binding to another neuronal receptor (synaptic vesicle 2A), some of the subgroup 3 compounds, such as nefiracetam, are similar to those of subgroup 1. (springer.com)
- The encoded protein negatively regulates Ras, Rap and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor trafficking to the postsynaptic membrane to regulate synaptic plasticity and neuronal homeostasis. (genecards.org)
Protein6
- Brain-derived neurotrophic factor , also known as BDNF , is a protein [5] that, in humans, is encoded by the BDNF gene . (wikipedia.org)
- Inhibition of endogenous G protein-coupled receptor kinase 2 by transfection with the non-G(q/11)alpha-binding, catalytically-inactive (D110A,K220R)G protein-coupled receptor kinase 2 mutant, decreased the extent of M1 mACh receptor desensitization under all conditions. (sigmaaldrich.com)
- OGD failed to induce the outward current under conditions where G-protein function was disrupted by loading cells with guanosine 5'-O-(2-thiodiphosphate) [GDPbetaS] or after prolonged injection of guanosine 5'-O(3-thiotdphosphate) [GTPgammaS]. (uzh.ch)
- Moreover, dopamine and 3,4-dihydroxyphenylacetic acid levels in the substantia nigra were significantly increased, α-synuclein expression was decreased, and neurological behaviors were significantly ameliorated in rats following transplantation of X-box-binding protein 1-transfected neural stem cells. (nrronline.org)
- This gene encodes a Ras GTPase activating protein that is a member of the N-methyl-D-aspartate receptor complex. (genecards.org)
- GSK3 phosphorylates two distinct sites in the N-terminus of PI4KIIalpha (Ser5 and Ser47), promoting binding to the adaptor protein 3 (AP-3) complex for trafficking to the lysosome to be degraded. (garvan.org.au)
Seizures5
- Of note, Eisai presented three post-hoc analyses evaluating the potential of FYCOMPA to help patients experience long-term, sustained convulsive seizure freedom, as well as data that supported the recent U.S. Food and Drug Administration (FDA) approval of FYCOMPA for monotherapy and adjunctive use in pediatric patients 4 years and older for the treatment of partial-onset seizures (POS) with or without secondarily generalized seizures. (biospace.com)
- These long-term seizure freedom data showed about 53% of patients with secondarily generalized seizures experienced convulsive seizure freedom at 2 years and close to 35% at 3 years," said Trevor Resnick , MD, Pediatric Neurologist at Nicklaus Children's Hospital. (biospace.com)
- In September 2018 , FYCOMPA was approved for monotherapy and adjunctive use in pediatric patients 4 years and older for the treatment of POS with or without secondarily generalized seizures. (biospace.com)
- 1 ] At randomised doses of 4-12 mg, perampanel conferred significant improvements in reducing seizure frequency and 50% responder rates for all partial seizures and complex partial (CP) seizures with secondary generalisation (SG seizures), compared with placebo. (fiercebiotech.com)
- Methods: Recurrent seizures were induced in the intact hippocampal preparation in vitro by continuous 5-hour exposure to low-Mg2⫹ solution. (docme.ru)
Brain8
- This system is responsible for the regulation of brain mass homeostasis and neural stem cell differentiation and proliferation ( 4 - 9 ). (frontiersin.org)
- There are three members of the ADAR family ADARs 1-3, with ADAR 1 and ADAR 2 being the only enzymatically active members.ADAR3 is thought to have a regulatory role in the brain. (wikipedia.org)
- ADAR1 and ADAR 2 are widely expressed in tissues, while ADAR 3 is restricted to the brain. (wikipedia.org)
- Editing of GluR-3 is regulated in rat brain from low levels in embryonic stage to a large increase in editing levels at birth. (wikipedia.org)
- Identifying major depression using whole-brain functional connectivity: a multivariate pattern analysis," Brain , vol. 135, no. 5, pp. 1498-1507, 2012. (hindawi.com)
- The effect of negative emotional context on neural and behavioural responses to oesophageal stimulation," Brain , vol. 126, Part 3, pp. 669-684, 2003. (hindawi.com)
- Brain indoleamine 2,3-dioxygenase contributes to the comorbidity of pain and depression," The Journal of Clinical Investigation , vol. 122, no. 8, pp. 2940-2954, 2012. (hindawi.com)
- Glutamatergic (N-methyl-D-aspartate receptor) hypofrontality in schizophrenia: too little juice or a miswired brain? (genes2cognition.org)
10.11861
- doi:10.1186/2193-1801-4-S1-P51. (wikipedia.org)
Oxidase1
- Moreover, nNOS carry on transferring electrons to the haem and, hence, oxidase NADPH at a high rate, while in eNOS and iNOS this reaction can happen at a much slower rate [ 5 ]. (intechopen.com)
Inhibitors1
- In this study we aimed to elucidate the mechanisms by which ER stress induction and oxidative stress impair vascular endothelial function.We conducted in vitro studies with primary endothelial cells from coronary arteries stimulated with tunicamycin, 1 μg/mL, in the presence or absence of two ER stress inhibitors: tauroursodeoxycholic acid (Tudca), 500 μg/mL, and 4-phenylbutyric acid (PBA), 5 mM. (chemweb.com)
Inhibition1
- Inhibition of [3H]alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid binding by the excitotoxin beta-N-oxalyl-L-alpha,beta-diaminopropionic acid. (muscimol.xyz)
Metabotropic1
- The demonstration that a metabotropic glutamate 2/3 (mGlu2/3) receptor agonist prodrug decreased both positive and negative symptoms of schizophrenia raised hopes that glutamatergic mechanisms may provide therapeutic advantages. (genes2cognition.org)
Cyclic1
- A series of ferrocenes which contain dinitrogen-fused pyrazolidinone ring were synthesized from acryloylferrocene (4) and N,N'‑cyclic azomethine imines (3). (bioportfolio.com)
10.10161
- doi:10.1016/0197-4580(81)90007-5. (wikipedia.org)
Membrane2
- The amount of GluR2 was markedly increased in the crude cytosolic fraction and decreased in the crude membrane fraction from the ipsilateral L 4-5 dorsal horn at 24 h (but not at 2 h) post-CFA injection. (elsevier.com)
- It has been shown that the quaternary structure of the membrane spanning domain has 4-fold symmetry. (aspetjournals.org)
Vitro2
- A series of chemical optimizations guided by in vitro affinity at histamine H3 receptor (H3R), physico-chemical properties and pharmacokinetics in rats resulted in identification of N-[4-(1-Cyclobutyl. (bioportfolio.com)
- Huperzine A, Vinpocetine, Acetyl-L-carnitine, Rhodiola Rosea and Alpha-lipoic Acid are popular nutritional supplements that have shown promising benefits in improving a range of biological (e.g., blood flow, anti-inflammatory, anti-oxidant, and direct neurotransmitter effects) and cognitive processes from in vitro, animal and human clinical research. (exrx.net)
Nootropic1
- Sixty participants (40 females and 20 males, with a mean age of 45.4 years, SD = 12.6) completed either the odd or even items from the Raven Advanced Progressive Matrices (APM) at baseline and the opposite odd or even items at week 4 after consuming either the combination nootropic or placebo. (exrx.net)
Serotonin1
- Serotonin 5-HT1F receptor agonist indicated to treat acute migraine with or without aura. (medscape.com)
Molecular Biology1
- The role of the CDK Pho85 in cell cycle control", Biochemistry and molecular biology international, 4, 140-149. (uic.es)
Mechanisms1
- Furthermore, the activity of MAP1A and MAP1B is controlled by upstream signaling mechanisms, including the MAP kinase and glycogen synthase kinase-3 β pathways. (biomedcentral.com)
GluR21
- Here we provide insight into the molecular basis of the potency and efficacy elicited by the 5-substituted willardiines on the basis of cocrystal structures with the GluR2 ligand-binding core. (rcsb.org)
Ligand1
- and 3) whether predictions of mechanism of action could be inferred by comparing molecular interactions between the ligand-binding domain and each compound with those of cyclothiazide and CX614. (aspetjournals.org)
Annotation1
- PLOS Biology 11(3): 10.1371/annotation/f32bc670-c9cf-4bb0-9376-cd8cfd1053c1. (plos.org)
Splice2
- The intronic sequence includes a 5' splice site, and the predicted double-stranded region is 30 base pairs in length. (wikipedia.org)
- The intronic sequence involved contains a 5' donor splice site. (wikipedia.org)
20022
- In two- as well as six-transmembrane K + channels, the amino- and carboxy-termini are located intracellularly and are required for tetramerization ( Deutsch, 2002 ). (jneurosci.org)
- 2002 Fall;8(3):255-82. (wikipedia.org)
Retinal2
- A rabbit model of traumatic optic nerve injury, established by occlusion of the optic nerve using a vascular clamp, was used to investigate the effects of alpha-amino-3-hydroxy-5-methyl-4- isoxazolepropionic acid receptor antagonist GYKI 52466 on apoptosis of retinal ganglion cells following nerve injury. (nrronline.org)
- The results demonstrate that following acute optic nerve injury, apoptosis of retinal ganglion cells is a programmed process, which can be inhibited by the alpha-amino-3-hydroxy-5-methyl-4- isoxazolepropionic acid receptor antagonist. (nrronline.org)
Substances2
- All racetams are schedule 4 substances in Australia under the Poisons Standard (February 2020). (wikipedia.org)
- A schedule 4 substance is classified as "Prescription Only Medicine, or Prescription Animal Remedy - Substances, the use or supply of which should be by or on the order of persons permitted by State or Territory legislation to prescribe and should be available from a pharmacist on prescription. (wikipedia.org)
Contrast1
- and (5) to evaluate an equivocal finding on a contrast-enhanced CT or MRI. (medworm.com)
Synthesis1
- Here, we describe the synthesis and pharmacological properties of 9-carboxymethyl-4-oxo-5 H ,10 H -imidazo[1,2- a ]indeno[1,2- e ]pyrazin-2-phosphonic acid (RPR 119990). (aspetjournals.org)
20161
- 2016;126(4):1190-1197. (jci.org)
Piracetam1
- Neurostim +C is a good premade stack, though I like to add piracetam to it when I need to concentrate in order to learn (only 4 more months of grad school at night, yay). (anabolicminds.com)