The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.
An agonist at two subsets of excitatory amino acid receptors, ionotropic receptors that directly control membrane channels and metabotropic receptors that indirectly mediate calcium mobilization from intracellular stores. The compound is obtained from the seeds and fruit of Quisqualis chinensis.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
A broad-spectrum excitatory amino acid antagonist used as a research tool.
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.
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.
Cell surface proteins that bind amino acids and trigger changes which influence the behavior of cells. Glutamate receptors are the most common receptors for fast excitatory synaptic transmission in the vertebrate central nervous system, and GAMMA-AMINOBUTYRIC ACID and glycine receptors are the most common receptors for fast inhibition.
A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.
Organic compounds that generally contain an amino (-NH2) and a carboxyl (-COOH) group. Twenty alpha-amino acids are the subunits which are polymerized to form proteins.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.
One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.
(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.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
Derivatives of GLUTAMIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the 2-aminopentanedioic acid structure.
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.
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.
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.
A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.
Use of electric potential or currents to elicit biological responses.
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.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
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.
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
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.
The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.
Amino acids that are not synthesized by the human body in amounts sufficient to carry out physiological functions. They are obtained from dietary foodstuffs.
Cellular proteins and protein complexes that transport amino acids across biological membranes.
Commonly observed structural components of proteins formed by simple combinations of adjacent secondary structures. A commonly observed structure may be composed of a CONSERVED SEQUENCE which can be represented by a CONSENSUS SEQUENCE.
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.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
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.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
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.
Amino acids containing an aromatic side chain.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
Single-stranded complementary DNA synthesized from an RNA template by the action of RNA-dependent DNA polymerase. cDNA (i.e., complementary DNA, not circular DNA, not C-DNA) is used in a variety of molecular cloning experiments as well as serving as a specific hybridization probe.
The sequential correspondence of nucleotides in one nucleic acid molecule with those of another nucleic acid molecule. Sequence homology is an indication of the genetic relatedness of different organisms and gene function.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
The rate dynamics in chemical or physical systems.
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).
Proteins prepared by recombinant DNA technology.
An essential branched-chain amino acid important for hemoglobin formation.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
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.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
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).
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.
The sum of the weight of all the atoms in a molecule.
Proteins found in any species of bacterium.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.

Plasticity of first-order sensory synapses: interactions between homosynaptic long-term potentiation and heterosynaptically evoked dopaminergic potentiation. (1/986)

Persistent potentiations of the chemical and electrotonic components of the eighth nerve (NVIII) EPSP recorded in vivo in the goldfish reticulospinal neuron, the Mauthner cell, can be evoked by afferent tetanization or local dendritic application of an endogenous transmitter, dopamine (3-hydroxytyramine). These modifications are attributable to the activation of distinct intracellular kinase cascades. Although dopamine-evoked potentiation (DEP) is mediated by the cAMP-dependent protein kinase (PKA), tetanization most likely activates a Ca2+-dependent protein kinase via an increased intracellular Ca2+ concentration. We present evidence that the eighth nerve tetanus that induces LTP does not act by triggering dopamine release, because it is evoked in the presence of a broad spectrum of dopamine antagonists. To test for interactions between these pathways, we applied the potentiating paradigms sequentially. When dopamine was applied first, tetanization produced additional potentiation of the mixed synaptic response, but when the sequence was reversed, DEP was occluded, indicating that the synapses potentiated by the two procedures belong to the same or overlapping populations. Experiments were conducted to determine interactions between the underlying regulatory mechanisms and the level of their convergence. Inhibiting PKA does not impede tetanus-induced LTP, and chelating postsynaptic Ca2+ with BAPTA does not block DEP, indicating that the initial steps of the induction processes are independent. Pharmacological and voltage-clamp analyses indicate that the two pathways converge on functional AMPA/kainate receptors for the chemically mediated EPSP and gap junctions for the electrotonic component or at intermediaries common to both pathways. A cellular model incorporating these interactions is proposed on the basis of differential modulation of synaptic responses via receptor-protein phosphorylation.  (+info)

Low resting potential and postnatal upregulation of NMDA receptors may cause Cajal-Retzius cell death. (2/986)

Using in situ patch-clamp techniques in rat telencephalic slices, we have followed resting potential (RP) properties and the functional expression of NMDA receptors in neocortical Cajal-Retzius (CR) cells from embryonic day 18 to postnatal day 13, the time around which these cells normally disappear. We find that throughout their lives CR cells have a relatively depolarized RP (approximately -50 mV), which can be made more hyperpolarized (approximately -70 mV) by stimulation of the Na/K pump with intracellular ATP. The NMDA receptors of CR cells are subjected to intense postnatal upregulation, but their similar properties (EC50, Hill number, sensitivity to antagonists, conductance, and kinetics) throughout development suggest that their subunit composition remains relatively homogeneous. The low RP of CR cells is within a range that allows for the relief of NMDA channels from Mg2+ blockade. Our findings are consistent with the hypothesis that CR cells may degenerate and die subsequent to uncontrolled overload of intracellular Ca2+ via NMDA receptor activation by ambient glutamate. In support of this hypothesis we have obtained evidence showing the protection of CR cells via in vivo blockade of NMDA receptors with dizocilpine.  (+info)

Activity-dependent metaplasticity of inhibitory and excitatory synaptic transmission in the lamprey spinal cord locomotor network. (3/986)

Paired intracellular recordings have been used to examine the activity-dependent plasticity and neuromodulator-induced metaplasticity of synaptic inputs from identified inhibitory and excitatory interneurons in the lamprey spinal cord. Trains of spikes at 5-20 Hz were used to mimic the frequency of spiking that occurs in network interneurons during NMDA or brainstem-evoked locomotor activity. Inputs from inhibitory and excitatory interneurons exhibited similar activity-dependent changes, with synaptic depression developing during the spike train. The level of depression reached was greater with lower stimulation frequencies. Significant activity-dependent depression of inputs from excitatory interneurons and inhibitory crossed caudal interneurons, which are central elements in the patterning of network activity, usually developed between the fifth and tenth spikes in the train. Because these interneurons typically fire bursts of up to five spikes during locomotor activity, this activity-dependent plasticity will presumably not contribute to the patterning of network activity. However, in the presence of the neuromodulators substance P and 5-HT, significant activity-dependent metaplasticity of these inputs developed over the first five spikes in the train. Substance P induced significant activity-dependent depression of inhibitory but potentiation of excitatory interneuron inputs, whereas 5-HT induced significant activity-dependent potentiation of both inhibitory and excitatory interneuron inputs. Because these metaplastic effects are consistent with the substance P and 5-HT-induced modulation of the network output, activity-dependent metaplasticity could be a potential mechanism underlying the coordination and modulation of rhythmic network activity.  (+info)

Impairment of neocortical long-term potentiation in mice deficient of endothelial nitric oxide synthase. (4/986)

The role of the possible retrograde messenger nitric oxide (NO) in the induction of long-term potentiation (LTP) was studied in supragranular layers of somatosensory cortical slices obtained from adult mice. High-frequency stimulation produced a slowly rising, long-lasting (50 min) and significant (P < 0.001) increase in the extracellular synaptic response by 23%. The induction of LTP was independent from activation of N-methyl-D-aspartate (NMDA) receptors, but prevented by bath application of NG-nitro-L-arginine methyl ester (L-NAME), indicating that one or several of the different NO synthases (NOS) produced NO within the postsynaptic neuron. No LTP could be induced in knockout mice lacking the endothelial NOS (eNOS) isoform. These data suggest that eNOS is involved in an NMDA receptor-independent form of LTP in the rodent cerebral cortex.  (+info)

NMDA-dependent currents in granule cells of the dentate gyrus contribute to induction but not permanence of kindling. (5/986)

Single-electrode voltage-clamp techniques and bath application of the N-methyl-D-aspartate (NMDA) receptor antagonist 2-amino-5-phosphonovaleric acid (APV) were used to study the time course of seizure-induced alterations in NMDA-dependent synaptic currents in granule cells of the dentate gyrus in hippocampal slices from kindled and normal rats. In agreement with previous studies, granule cells from kindled rats examined within 1 wk after the last of 3 or 30-35 generalized tonic-clonic (class V) seizures demonstrated an increase in the NMDA receptor-dependent component of the perforant path-evoked synaptic current. Within 1 wk of the last kindled seizure, NMDA-dependent charge transfer underlying the perforant path-evoked current was increased by 63-111% at a holding potential of -30 mV. In contrast, the NMDA-dependent component of the perforant-evoked current in granule cells examined at 2.5-3 mo after the last of 3 or 90-120 class V seizures did not differ from age-matched controls. Because the seizure-induced increases in NMDA-dependent synaptic currents declined toward control values during a time course of 2.5-3 mo, increases in NMDA-dependent synaptic transmission cannot account for the permanent susceptibility to evoked and spontaneous seizures induced by kindling. The increase in NMDA receptor-dependent transmission was associated with the induction of kindling but was not responsible for the maintenance of the kindled state. The time course of alterations in NMDA-dependent synaptic current and the dependence of the progression of kindling and kindling-induced mossy fiber sprouting on repeated NMDA receptor activation are consistent with the possibility that the NMDA receptor is part of a transmembrane signaling pathway that induces long-term cellular alterations and circuit remodeling in response to repeated seizures, but is not required for permanent seizure susceptibility in circuitry altered by kindling.  (+info)

17beta-estradiol enhances NMDA receptor-mediated EPSPs and long-term potentiation. (6/986)

Gonadal steroid hormones influence CNS functioning through a variety of different mechanisms. To test the hypothesis that estrogen modulates synaptic plasticity in the hippocampus, in vitro hippocampal slices from 2-mo-old Sprague-Dawley male rats were used to determine the effect of 17beta-estradiol on both N-methyl-D-aspartate (NMDA) receptor-mediated excitatory postsynaptic potentials (EPSPs) through intracellular recordings and long-term potentiation (LTP) through extracellular recordings. Intracellular EPSPs and extracellular field EPSPs (fEPSPs) were recorded from CA1 pyramidal cells by stimulating Schaffer collateral fibers. In intracellular experiments, slices were perfused with medium containing bicuculline (5 microM) and low Mg2+ (0.1 mM) to enhance the NMDA receptor-mediated currents and 6, 7-dinitroquinoxaline-2,3-dione (DNQX) (10 microM) to block the alpha-amino-3-hydroxy-5-methyl-4-isoxazoleproprianate (AMPA) receptor-mediated component. The effects of 17beta-estradiol on NMDA receptor-mediated activity were excitatory; concentrations >10 nM induced seizure activity, and lower concentrations (1 nM) markedly increased the amplitude of NMDA-mediated EPSPs (both the first and second responses increased during paired pulse stimulation by 180 and 197%, respectively). In extracellular experiments, slices perfused with 17beta-estradiol (100 pM) exhibited a pronounced, persisting, and significant enhancement of LTP of both the fEPSP slope (192%) and fEPSP amplitude (177%) compared with control slices (fEPSP slope = 155%; fEPSP amplitude = 156%) 30 min after high-frequency stimulation. These data demonstrate that estrogen enhances NMDA receptor-mediated currents and promotes an enhancement of LTP magnitude.  (+info)

Retinal input induces three firing patterns in neurons of the superficial superior colliculus of neonatal rats. (7/986)

By using an in vitro isolated brain stem preparation, we recorded extracellular responses to electrical stimulation of the optic tract (OT) from 71 neurons in the superficial superior colliculus (SC) of neonatal rats (P1-13). At postnatal day 1 (P1), all tested neurons (n = 10) already received excitatory input from the retina. Sixty-nine (97%) superficial SC neurons of neonatal rats showed three response patterns to OT stimulation, which depended on stimulus intensity. A weak stimulus evoked only one spike that was caused by activation of non-N-methyl-D-aspartate (NMDA) glutamate receptors. A moderate stimulus elicited a short train (<250 ms) of spikes, which was induced by activation of both NMDA and non-NMDA receptors. A strong stimulus gave rise to a long train (>300 ms) of spikes, which was associated with additional activation of L-type high-threshold calcium channels. The long train firing pattern could also be induced either by temporal summation of retinal inputs or by blocking gamma-aminobutyric acid-A receptors. Because retinal ganglion cells show synchronous bursting activity before eye opening at P14, the retinotectal inputs appear to be sufficient to activate L-type calcium channels in the absence of pattern vision. Therefore activation of L-type calcium channels is likely to be an important source for calcium influx into SC neurons in neonatal rats.  (+info)

NMDA receptor characterization and subunit expression in rat cultured mesencephalic neurones. (8/986)

1. NMDA-induced changes in free intracellular Ca2+ concentration ([Ca2+]i) were determined in individual cultured rat mesencephalic neurones by the fura-2 method. mRNA expression encoding NMDA receptor subunits (NR1, NR2A-D) was examined by RT-PCR. 2. NMDA (1-100 microM, plus 10 microM glycine) induced a concentration-dependent increase in [Ca2+]i (EC50 = 5.7 microM). The effect of NMDA was virtually insensitive to tetrodotoxin (0.3 microM) and nitrendipine (1 microM), but dependent on extracellular Ca2+. 5,7-Dichlorokynurenic acid (10 microM), a specific antagonist at the glycine binding site on the NMDA receptor, abolished the NMDA response. 3. Memantine, an open-channel blocker, and ifenprodil, a preferential non-competitive NR1/NR2B receptor antagonist diminished the NMDA effect with an IC50 value of 0.17 and 1 microM, respectively. Ethanol at 50 and 100 mM caused about 25 and 45%-inhibition, respectively. 4. Agarose gel analysis of the PCR products followed by ethidium bromide fluorescence or CSPD chemiluminescence detection revealed an almost exclusive expression of the NR1 splice variants lacking exon (E) 5 and E22. The 3' splice form without both E21 and E22 exceeded that containing E21 by approximately 4 fold. The relative amounts of NR2A, NR2B, NR2C corresponded to approximately 1:2:1. NR2D mRNA was also detectable. 5. In conclusion, mesencephalic neurones bear ethanol-sensitive NMDA receptors which might be involved in the development of ethanol dependence and withdrawal. The high affinity of NMDA to this receptor, its sensitivity to ifenprodil and memantine may suggest that the mesencephalic NMDA receptor comprises the NR1 splice variant lacking E5, NR2B, and NR2C, respectively.  (+info)

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1. Non‐competitive antagonists at the glutamatergic N‐methyl D‐ aspartate receptor significantly reduce the volume of ischaemic cerebral infarction in animals and are potential agents for the treatment of acute stroke in humans. 2. CNS 1102, a novel non‐ competitive NMDA antagonist, was administered as a 15 min intravenous infusion to healthy male volunteers in a double‐blind, placebo‐ controlled, dose‐ranging study. This was the first administration to man. 3. Clinically significant sedation, increased mean arterial pressure and pulse rate were seen at doses of 30 micrograms kg‐1 and above. Symptoms of sedation and central nervous excitation became unacceptable for conscious individuals at doses of 45 micrograms kg‐1 and above. 4. Rapid onset of central nervous system effects after administration is in keeping with rapid distribution of CNS 1102 to brain. Steady state volume of distribution was large (444 l) and terminal elimination half‐life from plasma was approximately 4 ...
(2R)-2-Amino-5-phosphonopentanoic acid | C5H12NO5P | CID 135342 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
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Characterization of the cerebroprotective efficacy of the competitive NMDA receptor antagonist CGP40116 in a rat model of focal cerebral ischemia: an in vivo magnetic resonance imaging study. - D Sauer, P R Allegrini, A Cosenti, A Pataki, H Amacker, G E Fagg
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In the 1960s and 70s, biochemical and pharmacological evidence was pointing toward glutamate as a synaptic transmitter at a number of distinct receptor classes, known as NMDA and non-NMDA receptors. The field, however, lacked a potent and highly selective antagonist to block these putative postsynaptic receptors. So, the discoveries in the early 1980s of D-AP5 as a selective NMDA receptor antagonist and of its ability to block synaptic events and plasticity were a major breakthrough leading to an explosion of knowledge about this receptor subtype. During the next 10 years, the role of NMDA receptors was established in synaptic transmission, long-term potentiation, learning and memory, epilepsy, pain, among others. Hints at pharmacological heterogeneity among NMDA receptors were followed by the cloning of separate subunits. The purpose of this review is to recognize the important contributions made in the 1980s by Graham L. Collingridge and other key scientists to the advances in our ...
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These results show that local perfusion with NMDA by retrodialysis produces a sustained increase in dialysate Cho. This effect of NMDA exhibits marked brain regional differences (Fig. 6 B). The NMDA-evoked increase in dialysate Cho precedes delayed excitotoxic cholinergic cell death and is blocked with AP-5, a competitive NMDA receptor antagonist. Interestingly, when NMDA was perfused for a short period of time (30 min), Cho levels remained significantly increased for at least 2 hr after discontinuation of NMDA perfusion (Fig.1 B).. Perfusion with a Ca2+-free medium or with a Ca2+-free medium in the presence of 5 mmEGTA completely blocked the NMDA-evoked increase in dialysate Cho, indicating that this effect is dependent on the extracellular concentration of calcium (Fig. 4). The fact that a strong depolarizing stimulus (i.e., 100 mm KCl), which is able to induce a sixfold increase in extracellular Ach (reflecting activation of voltage-dependent calcium inflow) and does not modify extracellular ...
MW 197.13, Purity | 99%. Competitive NMDA receptor glutamate site antagonist. More active form of DL-AP5.Soluble in 1 ml water to give specified mM/ml concentration. Find out more.
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Im using 10 micromol/l CNQX and 100 micromol/l D-AP5 dissolved in a serum free and protein free medium. I have tried to find information about the stability of these substances in solution, but have failed despite a Medline search. I would like to know if these substances are degraded upon prolonged incubation (i.e. 1-4 days). Jon Henrik Laake, MD --------------------------------------------------------------- Anatomical Institute, University of Oslo, POBox 1105 Blindern, 0317 OSLO, NORWAY Tel +47 22851176/51150, FAX +47 22851278, EMail: jon.laake at basalmed.uio.no ...
Isothiazoles having a 3-amino-2-acycloxy-propoxy or a 3-amino-2-hydroxy-propoxy substituent and 2-(3-amino-2-hydroxypropyl) isothiazole-3-ones are disclosed. These compounds have .beta.-adrenergic blocking activity.
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You are viewing an interactive 3D depiction of the molecule 3-[[(2R,3S,4R,5R)-5-(6-amino-8-bromo-purine-1,3,7-triium-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl]methylcarbamoyl]-3-hydroxy-pentanedioic acid (C16H19BrN6O9) from the PQR.
You are viewing an interactive 3D depiction of the molecule (2S)-5-amino-2-[3-(4-aminobutylamino)propylamino]-5-oxo-pentanoic acid (C12H26N4O3) from the PQR.
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Neuroprotective efficiency of NMDA receptor blockade in the striatum and CA3 hippocampus after various durations of cerebral ischemia in gerbils. - L Radenovic, V Selakovic, B Janac, Pavle R Andjus
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Abundant evidence suggests that NMDA receptors are involved in the nociceptive responses to formalin. Pretreatment with a competitive NMDA receptor antagonist [e.g., APV[3-amino-5-phosphonovaleric acid] or a noncompetitive NMDA receptor antagonist {e.g.,MK-801, [(+)-5 methyl-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten-5,10-imine hydrogen maleate], dextromethorphan or ketamine} reduces nociceptive behavioral and/or electrophysiological responses induced by formalin (Coderre and Melzack, 1992; Haley et al., 1990;Yamamoto and Yaksh, 1992; Vaccarino et al., 1993; Hunter and Singh, 1994; Elliott et al., 1995; Shimoyama et al., 1996). The effects of NMDA receptor antagonists are primarily on phase 2 behaviors of the formalin response (Coderre and Melzack, 1992). Phase 2 of the formalin test appears to reflect central sensitization. The barrage of C-fiber inputs produced by formalin most likely activates spinal cord NMDA receptors, which results in the sensitization of dorsal horn neurons. This results ...
Physiological activation of the N-methyl-D-aspartate (NMDA) subtype of glutamate receptors has been proposed to play a key role in both neuronal cell function and dysfunction. In the present study, we used selective NMDA receptor antagonists to investigate the involvement of NR2A and NR2B subunits in the modulatory effect of basal NMDA receptor activity on the phosphorylation of Tau proteins. We observed, in acute hippocampal slice preparations, that blockade of NR2A-containing NMDA receptors by the NR2A antagonist NVP-AAM077 provoked the hyperphosphorylation of a residue located in the proline-rich domain of Tau (i.e., Ser199). This effect seemed to be Ser199 specific as there was no increase in phosphorylation at Ser262 and Ser409 residues located in the microtubule-binding and C-terminal domains of Tau proteins, respectively. From a mechanistic perspective, our study revealed that blockade of NR2A-containing receptors influences Tau phosphorylation probably by increasing calcium influx into neurons,
TY - ABST. T1 - Differential effects of peripheral NMDA and non-NMDA receptors on response of persistent nociception induced by subcutaneous bee venom injection of the rat. AU - You, Hao-Jun. AU - Chen, J.. AU - Arendt-Nielsen, Lars. PY - 2001. Y1 - 2001. M3 - Conference abstract in proceeding. BT - International Advanced Workshop on Brain/Pain Research : From Molecules to Mind, 30 April-2 May 2001, Xian, China. ER - ...
The present study documents that NMDA channel activity may be upregulated or downregulated by remote NMDA receptors, depending on the amount of Na+ and Ca2+ influx. If Na+ influx is blocked, Ca2+ influx induced by the activation of remote NMDA receptors may inhibit NMDA channel gating. However, this inhibitory effect can be overcome by an increase in [Na+]i of ,5 mm. Thus there may be a functional Na+-Ca2+ interaction in the regulation of NMDA channels.. Further detailed investigations document that the effects of Na+ and Ca2+ influx on NMDA channel gating during the activation of remote NMDA receptors cannot be explained simply by an algebraic sum of two opposite effects growing monotonically, because (1) Ca2+ influx required to downregulate NMDA receptors under the condition of no Na+ influx is found to be much smaller than that during NMDA receptor activation under normal conditions; (2) a modest Na+ influx, which produces a much smaller increase in [Na+]i than that during NMDA receptor ...
Expressions of N-methyl-D-aspartate receptors NR2A and NR2B subunit proteins in normal and sulfite-oxidase deficient rats hippocampus: effect of exogenous sulf
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   Forgive me if some of this is repetitive, much of this has been posted on our Ketamine thread, but I felt like it deserved a thread of its own. Ever since I ended up in the ER with a cluster and they gave me I.V. magnesium I have been interested in glutamate toxicity in the brain. I could...
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TY - JOUR. T1 - Age dependence of homosynaptic non-NMDA mediated long-term depression in field CA1 of rat hippocampal slices. AU - Velíšek, Libor. AU - Moshé, Solomon L.. AU - Stanton, Patric K.. PY - 1993/10/15. Y1 - 1993/10/15. N2 - It has been hypothesized that high levels of presynaptic activity that fail to activate postsynaptic N-methyl-d-aspartate (NMDA) receptors may lead to long-term depression (LTD). Therefore, we tested the ability of high-frequency (50 Hz) synaptic stimulation in the presence of a blocker of NMDA receptors to elicit homosynaptic LTD at Schaffer collateral-CA1 synapses in hippocampal slices from 15-, 30- and 60-day-old rats. In control slices, there were no developmental differences in the incidence of long-term potentiation (LTP) of either EPSP slope or population spike amplitude. However, while NMDA receptor blockade with the specific antagonist d-2-amino-5-phosphonopentanoic acid (AP5; 25 μM) completely eliminated LTP in 30 and 60-day-olds, a significant number ...
TY - JOUR. T1 - NMDA receptor blockade prevents the increase in protein kinase C substrate (protein F1) phosphorylation produced by long-term potentiation. AU - Linden, David J.. AU - Wong, Ka L.. AU - Sheu, Fwu Shan. AU - Routtenberg, Aryeh. PY - 1988/8/16. Y1 - 1988/8/16. N2 - Recent evidence has implicated activation of the N-methyl-d-aspartate (NMDA) class of glutamate receptor in the initiation of hippocampal long-term potentiation (LTP), an electrophysiological model of information storage in the brain. A separate line of evidence has suggested that activation of protein kinase C (PKC) and the consequent phosphorylation of it substrates is necessary for the maintenance of the LTP response. To determine if PKC activation is a consequence of NMDA receptor activation during LTP, we applied the NMDA receptor antagonist drug, dl-aminophosphonovalerate (APV) both immediately prior to and following high frequency stimulation, resulting in successful and unsuccessful blockade of LTP initiation, ...
Ananth, C., Dheen, S.T., Gopalakrishnakone, P., Kaur, C. (2003). Distribution of NADPH-diaphorase and expression of nNOS, N-Methyl-D-Aspartate receptor (NMDAR1) and Non-NMDA glutamate receptor (GlutR2) genes in the neurons of the hippocampus after domoic acid-induced lesions in adult rats. Hippocampus 13 (2) : 260-272. [email protected] Repository. https://doi.org/10.1002/hipo. ...
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. 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. The effect of D-AP5 was concentration dependent, with an EC50 of 10 microM. Up-regulation of NMDA receptors was observed after 2-7 days but not after 1 day of exposure to 100 microM D-AP5. 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. The binding of [3H]AMPA was unaltered after exposure to D-AP5. These results demonstrate that the density of NMDA receptors on cultured ...
Selfotel (CGS-19755) is a drug which acts as a competitive NMDA antagonist, directly competing with glutamate for binding to the receptor. Initial studies showed it to have anticonvulsant, anxiolytic, analgesic and neuroprotective effects, and it was originally researched for the treatment of stroke, but subsequent animal and human studies showed phencyclidine-like effects, as well as limited efficacy and evidence for possible neurotoxicity under some conditions, and so clinical development was ultimately discontinued. Lehmann J, Hutchison AJ, McPherson SE, Mondadori C, Schmutz M, Sinton CM, Tsai C, Murphy DE, Steel DJ, Williams M, et al. CGS 19755, a selective and competitive N-methyl-D-aspartate-type excitatory amino acid receptor antagonist. Journal of Pharmacology and Experimental Therapeutics. 1988 Jul;246(1):65-75. PMID 2899170 Bennett DA, Lehmann J, Bernard PS, Liebman JM, Williams M, Wood PL, Boast CA, Hutchison AJ. CGS 19755: a novel competitive N-methyl-D-aspartate (NMDA) receptor ...
Olneys lesions Olneys lesions, also known as NMDA receptor antagonist neurotoxicity (NAN), are a form of brain damage caused by high doses of dissociative
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... amino - amino acid - amino acid receptor - amino acid sequence - amino acid sequence homology - aminobutyric acid - ammonia - ... Essential amino acid - Ester - estradiol receptor - estrogen receptor - Ethanol - Ether - eukaryote - evolution - evolutionary ... Articles related to biochemistry include: Contents: Top 0-9 A B C D E F G H I J K L M N O P Q R S T U V W X Y Z 2-amino-5- ... phosphonovalerate - 3' end - 5' end ABC-Transporter Genes - abl gene - acetic acid - acetyl CoA - acetylcholine - ...
... amino acids, aromatic MeSH D12.125.072.050.342 - dextrothyroxine MeSH D12.125.072.050.685 - phenylalanine MeSH D12.125.072.050. ... 2-aminoadipic acid MeSH D12.125.119.170 - aspartic acid MeSH D12.125.119.170.150 - d-aspartic acid MeSH D12.125.119.170.275 - ... 5-hydroxytryptophan MeSH D12.125.072.050.875 - tyrosine MeSH D12.125.072.050.875.064 - betalains MeSH D12.125.072.050.875.064. ... 2-amino-5-phosphonovalerate MeSH D12.125.740.675 - phosphocreatine MeSH D12.125.740.700 - phosphoserine MeSH D12.125.740.725 - ...
... (also known as APV, (2R)-amino-5-phosphonovaleric acid, or (2R)-amino-5-phosphonopentanoate) is a chemical compound used as ... Disruption by the NMDA Receptor Antagonist DL-2-Amino-5-Phosphonovalerate Gustafsson B., Wigström H., Abraham W.C., and Huang Y ...
Fourth, D-AβP(1-40), AβP(1-40) composed of all D-amino acid residues, also caused the elevation of [Ca2+]i in a manner similar ... AβPs were reported to bind to NMDA (N-methyl D-aspartate-)type or AMPA (α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid)- ... This different C-terminal cleavage of APP causes various truncated AβPs, such as AβP(1-40), the first 40 amino acid residues, ... AβP is a small peptide with 39-43 amino acid residues. It is secreted by the cleavage of the N-terminal of a large precursor ...
Excitatory Amino Acid Antagonists / pharmacology * Exocytosis * GTP-Binding Proteins / physiology* * In Vitro Techniques ...
Amino Acids / pharmacology * Animals * Animals, Newborn / physiology* * Bicuculline / pharmacology * Evoked Potentials / drug ... 2. The GDPs were synchronously generated by a population of neurones; they reversed polarity at -27 mV when recorded with KCl- ... 4. The GDPs were reduced in frequency or blocked by the N-methyl-D-aspartate (NMDA) receptor antagonists DL-2-amino-7- ... The NMDA receptor antagonists AP-5 (50 microM), AP-7 (50 microM) and CPP (30 microM) usually reduced the amplitude and the ...
Epub 2016 Jan 5. Research Support, Non-U.S. Govt ... De Rossi P1,2,3, Harde E4,5,6, Dupuis JP7,8, Martin L1,2,3, ... 2,3, Watrin C1,2,3, Benetollo C1,2,9, Pernet-Gallay K10,11, Luhmann HJ12, Honnorat J1,2,13, Malleret G1,2,14, Groc L7,8, Acker- ... n=10 independent experiments for PSD95, n=5 for GluN2B and n=12 for GluN2A. Data were analyzed using a Kruskal-Wallis and when ... Figure 5. Hippocampal LTP as well as contextual and cued fear memory are impaired in VEGFR2 conditional knockout mice and upon ...
... excitatory amino acid receptors. Categories:. * Info Excitatory Amino Acid Agents ... 2-Amino-5-phosphonovalerate View Synonyms. View Structure. Description:. The D-enantiomer is a potent and specific antagonist ...
3-((4-Amino-2-methyl-5-pyrimidinyl)methyl)-4-methyl-5-(4,6,8,8-tetrahydroxy-3,5,7-trioxa-4,6,8-triphosphaoct-1-yl)thiazolium ... Alpha-Amino-3-Hydroxy-5-Methyl-4- Isoxazole Propionic Acid Receptor Components of the Anti-Depressant Ketamine Response ... Toluenes in which one hydrogen of the methyl group is substituted by an amino group. Permitted are any substituents on the ... D-amino Acid Oxidase Inhibition (DAAOI-1) add-on Treatment for Chronic Schizophrenia ...
... scanning photostimulation revealed that NCAM deletion increased the strength of close-in inhibitory connections to layer 2/3 ... scanning photostimulation revealed that NCAM deletion increased the strength of close-in inhibitory connections to layer 2/3 ... In vesicular gamma-amino butyric acid (GABA) transporter (VGAT)-channelrhodopsin2 (ChR2)-enhanced yellow fluorescent protein ( ... 2. *. (. 1. −. exp. (. −. (. I. −. I. break. ). /. I. rate. ). ). +. (. F. 0. +. F. 1. ). (. 1. ). ...
... amino]methylene]-3-methyl-5-isoxazoleacet-amide; 5-HI, 5-hydroxyindole; A-867744, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H ... At lower concentrations, no evidence of a distinct secondary component was evident in contrast to 4-naphthalen-1-yl-3a,4,5,9b- ... However, unlike these PAMs, A-867744 displaced the binding of the agonist [3H](1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5 ... In this study, we describe a novel type II α7 PAM, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide ...
Gabapentin, an amino acid designed as a structural analog of GABA (Sills, 2006), is a novel anticonvulsant drug that came into ... amino-2-hydroxypropyl](phenylmethyl)phosphinic acid hydrochloride [CGP 55845A (CGP); a GABAB receptor antagonist] to further ... 5A), nor did any dose of gabapentin alter water responding by any group of rats (Fig. 5B) (p , 0.05 in all cases). Data for two ... 2A). In the presence of 50 μm gabapentin, 44 mm ethanol, a maximally effective concentration (Roberto et al., 2003, 2004a) ...
2C,D,F,G), with relatively small measurement errors (Fig. 2I,J). More important, we now observed a strong correlation between ... H, Average optic trace of a 200 Hz 5-AP train recorded from the cell in A. I, Quantification of the fifth to first AP width ... 2E,H). Together, our data provides strong evidence that Ace-mNeon and Archon2 can be used to measure AP kinetics reliably both ... 5A-C). The speed of orthodromic axonal AP propagation was calculated from a linear fit to the latency of the distal axonal AP ...
CGP 40116 (5-40 mg/kg i.v.) was injected immediately following permanent occlusion of the left middle cerebral artery (MCA). MK ... The cerebroprotective properties of the competitive NMDA antagonist D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid (CGP ...
Effect of theanine on brain amino acids and monoamines, and the striatal release of dopamine (DA)... ... is one of the major components of amino acids in Japanese green tea. ... Amino acid assignment to one of three blood-brain barrier amino acid carriers. Am. J. Physiol. 230:94-98.Google Scholar ... Developments in amino acid transport, illustrated for the blood-brain barrier. Biochem. Pharmacol. 28:1989-1992.Google Scholar ...
... amino-2-(S)-hydroxypropyl-p-benzyl-phosphinic acid; TTX, tetrodotoxin; sIPSC, spontaneous IPSC; sEPSC, spontaneous EPSC; mIPSC ... 5). Ethanol (40 mM) increased the mean frequency of mIPSCs from 0.7 ± 0.1 to 0.9 ± 0.1 Hz in WT mice (n = 9, p , 0.01), with ... 5. Ethanol effects on mIPSCs in CeA neurons from MOR KO and WT mice. A and B, representative mIPSCs before and during ethanol ... 2. Baseline activities of evoked GABAergic synaptic responses in CeA from MOR KO and WT mice. Inhibitory synaptic responses ...
Reviewer #2:. The authors have satisfactorily addressed many of my criticisms, although I would like to place on record that ... 2) Missing information about cell types: The paper is about "pyramidal cells" in the PCx but many of the figures do not show ... Reviewer #2:. I suggested that the authors state that they studied principal cells located in layer 2, mainly focusing on ... 2) Missing information about cell types: The paper is about "pyramidal cells" in the PCx but many of the figures do not show ...
1983) Excitatory amino acids in synaptic transmission in the Schaffer collateral-commissural pathway of the rat hippocampus. J ... a potent and selective antagonist of amino acid-induced and synaptic excitation. Neurosci Lett 21(1):77-81. ... 2 A and B, 5B, and 6D and Fig. S1, K-Gluconate was substituted with equimolar Cs-methanesulfonate. Synaptic responses were ... 2B). In the presence of 7CK LTD was still observed (Fig. 1D), supporting the view that ion flux through the NMDAR channel is ...
Its chemical name is 2-amino-5-phosphonovalerate.. Riluzole: is a drug used to treat amyotrophic lateral sclerosis. Riluzole ... Chemical name: (+)-5-methyl-10,11-dihydroxy-5h-dibenzo (a,d)cyclohepten-5, 10-imine,/span,. DEA Schedule: Not Controlled, ... CAS #: 10024-97-2. DEA Schedule: Un-Scheduled, OTC. Classification: Dissociative Anesthetic Gas. Other names: Nitrous, Hippy ... LD50: 229±5 mg/kg (rats). Classification: Dissociative; Psychedelic Common rote of administration: Snorted, IM. Injection. ...
Phencyclidine-like behavioral effects in pigeons induced by systemic administration of the excitatory amino acid antagonist, 2- ... The effects of intrathecal administration of several inhibitory amino acids and an excitatory amino acid antagonist in the ... The excitatory amino acid antagonist amino-phosphono-valeric acid (APV) provides protection against penicillin-induced ... Retardation of amygdaloid kindling by and the behavioral effects of kynurenic acid an antagonist of excitatory amino acids a ...
5. The NMDA component of the EPSC could be switched off with a hyperpolarizing voltage step at the soma. The kinetics of this ... 2. Excitatory postsynaptic currents (EPSCs) had a fast component whose amplitude was voltage insensitive and a slow component ... 3. The voltage-dependent component was abolished by the N-methyl-D-aspartate (NMDA) receptor antagonist DL-2-amino-5- ... phosphonovalerate (APV; 50 microM), which had no effect on the fast component. Conversely, the fast voltage-insensitive ...
... were higher than those of the transported amino acids, D- and L-aspartate (EC50 = 250 μM and 300 μM) and D- and L-glutamate (EC ... potencies of these amino acids; (ii) the potency of APV towards the actions of transported agonists acting at NMDA receptors ... Diffusion of transported amino acids into brain slices. Authors. *. J. Garthwaite. * Dept Veterinary Physiology & Pharmacology ... responses to excitatory amino acids and their analogues were compared in slices and dissociated cells from the developing rat ...
2, B and C). When added in the presence of NBQX and d-APV, suramin (10 μM) also reduced the amplitude (by 55 ± 8%, n = 7) and ... 5 A, top). The amplitude distribution of the evoked EPSC had a single peak located at ∼4-12 pA (Fig. 5 B, top); it was better ... 2 A) and suramin (10 μM, Fig. 2 B), which both block most of P2X receptor subtypes (North and Surprenant, 2000). PPADS (3 μM) ... Cloning of P2X5 and P2X6 receptors and the distribution and properties of an extended family of ATP-gated ion channels. J. ...
Correlation between kinetics and RNA splicing of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptors in ... Controlling brain states. Neuron Bennett, C., Arroyo, S., Hestrin, S. 2014; 83 (2): 260-261 Abstract. Neurons in mouse V1 ... In layer 5/6 (L5/6), we recorded from two or three FS and/or pyramidal (PYR) neurons to study the development of electrical and ... 5. The NMDA component of the EPSC could be switched off with a hyperpolarizing voltage step at the soma. The kinetics of this ...
Alternative splicing of APP yields eight isoforms with lengths of 677-770 amino acid residues, of which APP695 is the primary ... Intraneuronal accumulation of Aβ peptides occurs already at 2 months of age in the CA1 region of the hippocampus (E) and ... It has been shown that γ-secretase consists of a complex of different proteins including presenilin-1 (PS1) or presenilin-2 ( ... These cases represent only a minor portion (∼5%), whereas the vast majority of AD cases develop sporadically. Most of the ...
Metabolism and Signaling Functions of Amino Acids in the Regulation of Cell/Tissue Function in Health and Disease. Deadline for ... 2C. Measurements of serum hormone levels confirmed the cycle stage on the basis of a vaginal cytology pattern. TS on the pelvic ... Measurements were made ∼5-8 h after the lights were turned on and when the rats were in either the proestrus (high estradiol ... 2. Western blot assay of NMDA NR2A and NR2B subunits. A: representative Western blot showing the basal and phosphorylated NMDA ...
The effects of excitatory amino acids on the membrane current of isolated retinal glial cells (Müller cells) were investigated ... phosphonovalerate (APV; 100 microMs), 6‐cyano‐7‐nitroquinoxaline‐2,3‐dione (CNQX; 20 microMs), and kynurenate (1mM) had no ... 8. The voltage dependence, cation dependence and pharmacological profile of the current evoked by excitatory amino acids ... 8. The voltage dependence, cation dependence and pharmacological profile of the current evoked by excitatory amino acids ...
Martin, D; Swartzwelder, HS (1992). Ethanol inhibits release of excitatory amino acids from slices of hippocampal area CA1.. ... ALTERATIONS IN ALCOHOL INTAKE IN THE RAT BY INHIBITION OF AMINE-ALDEHYDE CONDENSATION OR AMINO-ACID TREATMENT. Alcoholism: ... Alterations in alcohol intake in the rat by inhibition of amine-aldehyde condensation or amino acid treatment. Alcoholism: ... The Journal of neuroscience : the official journal of the Society for Neuroscience, 13(5), 2264-2272. [8478698] [abs] ...
Excitatory amino acid receptors in the vertebrate central nervous system. Pharmacol. Rev. 40:143-210.Google Scholar ... Displacement of excitatory amino acid receptor ligands by acidic oligopeptides. Neurochem. Res. 14:1223-1227.Google Scholar ... Excitatory amino acid neurotoxicity and neurodegenerative disease. Trends Pharmacol. Sci. 11:379-387.Google Scholar ... 3H-Labeled MK-801 binding to the excitatory amino acid receptor complex from rat brain is enhanced by glycine. Proc. Natl. Acad ...
... gamma-amino butyric acid (GABA), glutamate, nitric oxide, carbon monoxide and the like. Agents which act as agonists for the ... 2[0130] a and 2 b. Autonomic blockade resulted in a slightly larger decrease in HR in mdx than C57 mice such that there was no ... 2. Bia B L, Cassidy P J, Young M E, Rafael J A, Leighton B, Davies K E, Radda G K, Clarke K. Decreased myocardial nNOS, ... 2[0037] a illustrates in vivo response of HR to atropine, propranolol, and the combination of both drugs. Agents were ...
The effects of a series of omega-phosphonic alpha-carboxylic amino acids on electrically evoked and excitant amino acid-induced ... Actions of D and L forms of 2-amino-5-phosphonovalerate and 2-amino-4-phosphonobutyrate in the cat spinal cord.. Brain Res 235: ... and in 5 µM NMDA (blue). Mibefradil (20 µM), nimodipine (20 µM) and TTX (0.5 µM) were present throughout. ...
The NMDA receptor-antagonist dl-2-amino-5-phosphonovalerate significantly disrupted synaptic enhancement after associative ...
... amino-3-hydroxyl-5-methyl-4-isoxazole-propionate (AMPA)/kainate receptor antagonist; D-2-amino-phosphonovalerate (AP-5), an N- ... Officials in Ballwin, Mo., have voted 6-2 not to accept a donation to display the motto "In God We Trust" in its board room.. ... E8875), [P.sub.4] + [E.sub.2] + ICI182,780 (ICI; an estrogen receptor antagonist; 100 ng/ml; Tocris, Ballwin, MO, USA), or [E. ... We used the following receptor/channel antagonists during whole-cell recordings: 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), ...
  • APB) excitatory amino acid receptors. (nih.gov)
  • Glutamate, the major excitatory transmitter in the brain, acts on several receptors that have been divided into ionotropic [(AMPA, NMDA, kainate) those whose primary function is to allow entry of ions into neurons] and metabotropic [(mGluR1-8) those that through conformational changes drive intracellular signaling pathways independent of ion-channel flow] classes ( 1 , 2 ). (pnas.org)
  • These results support the hypothesis that the behavioral effects of PCP-like drugs result at least in part from reduced neurotransmission at excitatory amino acid synapses utilizing N-methyl-D-aspartate preferring receptors. (eurekamag.com)
  • Excitatory amino acid receptors in the vertebrate central nervous system. (springer.com)
  • The rapid, desensitizing glutamate current exhibited a linear current-voltage relation and it was not blocked by 2-amino-5-phosphonovalerate, suggesting that it was mediated by N-methyl-D-aspartate-insensitive (G2) receptors. (pnas.org)
  • Desensitization of G 2 receptors may be agonist-dependent: currents evoked by kainate, a selective G 2 agonist, did not decay, whereas prior application of glutamate did reduce the size of kainate responses. (elsevier.com)
  • 7. The results indicate that the PSP evoked by focal stimulation within the nucleus locus coeruleus results from an excitatory amino acid acting predominantly at non-NMDA receptors, and from GABA acting at GABA(A) receptors. (elsevier.com)
  • This released glutamate activates ionotropic glutamate receptors such as α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid and N -methyl-d-aspartate (NMDA) receptors in the postsynaptic membrane of the DH neurons, causing membrane depolarization and the firing of action potentials. (asahq.org)
  • 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)
  • 1. The effects of the K + channel blocker 9-amino-1,2,3,4- tetrahydroacridine (THA) on the actions of baclofen and γ-aminobutyric acid (GABA) at post- and presynaptic GABA(B) receptors were studied with whole- cell voltage-clamp recording in area CA3 of rat hippocampal slices. (elsevier.com)
  • 5. These results indicate that THA blocks the actions of baclofen and GABA at post- but not presynaptic GABA(B) receptors. (elsevier.com)
  • Robustness of the results was achieved instrumentally and pharmacologically, by means of nitric oxide synthase (NOS) inhibitors and antagonists of NMDA (D-(-)-2-amino-5-phosphonopentanoic acid, AP5) and AMPA (2,3-dioxo-6-nitro-1,2,3,4-tetrahydrobenzo[f]quinoxaline-7-sulfonamide, NBQX) receptors. (unboundmedicine.com)
  • This observation is consistent with an action of N-methyl-D-aspartate and 2-amino-5-phosphonovalerate at receptors located on the auditory nerve dendrites contacting the inner hair cells. (neuroreille.com)
  • Open up in another home window Fig. 2 Glutamate causes a reduced amount of Kv4.2 clusters in the soma and dendrites of cultured hippocampal neurons through NR2B-containing NMDA receptors. (paccon2016.com)
  • All tumors but one were investigated immunohistochemically to detect the somatostatin receptors and expressed at least 3 of 5 subtypes of somatostatin receptors. (nel.edu)
  • 50 microM), D(-)2-amino-5-phosphonovalerate (AP-5, 10-50 microM) and (+-)3-(2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid (CPP, 10-50 microM) or NMDA channel blockers phencyclidine (2 microM) and ketamine (20 microM). (nih.gov)
  • The NMDA receptor antagonists AP-5 (50 microM), AP-7 (50 microM) and CPP (30 microM) usually reduced the amplitude and the duration of the evoked GDPs. (nih.gov)
  • 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)
  • The cerebroprotective properties of the competitive NMDA antagonist D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid ( CGP 40116 ) were evaluated in a rat model of focal cerebral ischemia . (curehunter.com)
  • Identification of selective NMDA receptor (NMDAR) antagonists ( 3 ) permitted ascribing its requirement ( 4 ) for the long-term potentiation (LTP) of synaptic transmission triggered by a high-frequency stimulus ( 5 ). (pnas.org)
  • 5. The NMDA component of the EPSC could be switched off with a hyperpolarizing voltage step at the soma. (nih.gov)
  • 2 In slices, the potencies of the weakly (or non-) transported analogues, N-methyl-D-aspartate (NMDA) and kainate (KA) (EC 50 = 40 μM each) were higher than those of the transported amino acids, D- and L-aspartate (EC 50 = 250 μM and 300 μM) and D- and L-glutamate (EC 50 = 540 μM and 480 μM). (wiley.com)
  • A study was made of the effects of reduced (GSH) and oxidized (GSSG) glutathione on the Na + -independent and N-methyl-D-aspartate (NMDA) displaceable bindings of glutamate, on the binding of kainate, 2-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA), and ligands of the brain NMDA receptor-ionophore complex: glycine, dizocilpine (MK-801) and (±)-3-(2-car-boxypiperazin-4-yl)propyl-1-phosphonate (CPP). (springer.com)
  • The activation of dizocilpine binding by GSH and GSSG was prevented by the competitive NMDA and glycine antagonists DL-2-amino-5-phosphonovalerate and 7-chlorokynurenate. (springer.com)
  • Averaged Ca2+ transients (500 Hz line scans) evoked by 40 ms voltage step in a dendrite (left) and spine (right) in control (black), D-AP5 (red, 10 µM), after a 10 min washout of D-AP5 (green), and in 5 µM NMDA (blue). (abcam.com)
  • The NMDA receptor-antagonist dl -2-amino-5-phosphonovalerate significantly disrupted synaptic enhancement after associative training but did not disrupt synaptic enhancement after nonassociative training. (sciencemag.org)
  • 2-amino-5-phosphonovalerate (APV), a specific NMDA antagonist, abolished the sEPSP, while it did not affect fEPSP. (nii.ac.jp)
  • 2-APV (50 μM) selectively blocked the effect of NMDA. (elsevier.com)
  • 10,11 ] Similarly, glutamate-like immunoreactivity [ 12 ] and NMDA, kainate, and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid binding sites [ 13 ] are present in the dorsal and ventral horn of the spinal cord. (asahq.org)
  • LTP induction was dependent on NMDA receptor activation, being blocked by perfusing the preparation with 2-amino-5-phosphonovalerate (AP-5). (mblwhoilibrary.org)
  • This LTP also was NMDA-dependent and was more sensitive to blockade by the NMDA antagonists 2-amino-5-phosphonovalerate (APV) and N-acetyl-aspartyl-glutamate, than the excitatory LTP produced by Schaffer collateral stimulation. (elsevier.com)
  • The prototypic NMDA receptor agonist NMDA, or the selective NMDA receptor antagonist D(-)-2-amino-5-phosphonopentanoic acid (D-AP-5) was microinjected into the CeA of satiated and euhydrated rats. (bvsalud.org)
  • Quantitative autoradiographic techniques were used to obtain a preliminary description of the pharmacological characteristics and anatomical distribution of the selective N-methyl-d-aspartate (NMDA) receptor antagonist d-2-[ 3 H]amino-5-phosphonopentanoate (d-[ 3 H]AP5). (nebraska.edu)
  • Me-B 12 induced enhhncement of FP was strongly blocked by an N-methyl-D-aspartate (NMDA) receptor antagonist, DL-2-amino-5-phosphonovaleric acid (APV). (elsevier.com)
  • Application of the non-NMDA receptor antagonist, 6,7-dinitroquinoxaline-2,3-dione (DNQX), inhibited the ATP-evoked responses in both groups. (umn.edu)
  • These results suggest that NMDA-dependent mechanisms contribute to the enhanced ATP-evoked responses of TMJ units in superficial laminae at the Vc/C 1-2 region under high E2 conditions, while non-NMDA-dependent mechanisms modify the encoding properties of TMJ units independent of E2 status. (umn.edu)
  • The responses for maximally effective concentrations of QA with either ibotenate or kainate were not additive, which suggested that all the excitatory amino acid agonists which stimulate InsPs accumulation (quisqualate, kainate, NMDA, glutamate, ibotenate, aspartate) have a common site of action. (muscimol.xyz)
  • CGP 40116 is the active (R)-enantiomer of the most potent N-methyl-d-aspartic acid (NMDA) receptor antagonist presently available: 2-amino-4-methyl-5-phosphono-3-pentenoic acid (CGP 37849). (openaire.eu)
  • Competitive NMDA receptor antagonist AP-5 and noncompetitive NMDA receptor blocker MK-801 was injected via brain cannula or vein cannula and was restrained for 3 hours. (nel.edu)
  • Theanine, r-glutamylethylamide, is one of the major components of amino acids in Japanese green tea. (springer.com)
  • Effect of theanine on brain amino acids and monoamines, and the striatal release of dopamine (DA) was investigated. (springer.com)
  • Determination of amino acids in the brain after the intragastric administration of theanine showed that theanine was incorporated into brain through blood-brain barrier via leucine-preferring transport system. (springer.com)
  • Inhibition pattern by analogs indicates the presence of ten or more transport systems for amino acids in brain cells. (springer.com)
  • Effect of dietary level of protein or methionine and threonine on the amino acids and catecholamines in brain of rats fed a high tyrosine diet. (springer.com)
  • 1 Pharmacological properties of the guanosine 3′5′-cyclic monophosphate (cyclic GMP) responses to excitatory amino acids and their analogues were compared in slices and dissociated cells from the developing rat cerebellum maintained in vitro . (wiley.com)
  • 5 These conclusions are supported by theoretical considerations relating to the diffusion of transported amino acids into brain slices, as elaborated in the Appendix. (wiley.com)
  • Attwell, D 1991-05-01 00:00:00 The effects of excitatory amino acids on the membrane current of isolated retinal glial cells (Müller cells) were investigated using whole‐cell patch clamping. (deepdyve.com)
  • 8. The voltage dependence, cation dependence and pharmacological profile of the current evoked by excitatory amino acids indicate that it is caused by activation of the high‐affinity glutamate uptake carrier. (deepdyve.com)
  • The effects of a series of omega-phosphonic alpha-carboxylic amino acids on electrically evoked and excitant amino acid-induced responses in isolated spinal cord preparations. (abcam.com)
  • Quisqualate-sensitive sites accounted for 80% of the total binding sites already at postnatal day 15, while displacement by alpha-amino-3-hydroxy-methyl-4-isoxazolepropionic and ibotenic acids attained the maximum (68%) at postnatal day 60. (muscimol.xyz)
  • Effects of bath-applied excitatory amino acids and their analogs on spinal interneurons of the lamprey. (children-of-the-amphioxus.com)
  • Quisqualate was strongest among these amino acids in producing depolarizations and conductance increases. (children-of-the-amphioxus.com)
  • The glymphatic system, analogous to the lymphatic system of the rest of the body, consists of perivascular tunnels, formed by astroglial cells, to promote efficient elimination of waste products of cerebral metabolism from the CNS as well as to facilitates brain-wide distribution of several compounds, including glucose, lipids, amino acids, growth factors, and neuromodulators. (medlink.com)
  • Stimulatory and inhibitory actions of excitatory amino acids on inositol phospholipid metabolism in rabbit retina. (muscimol.xyz)
  • In this study, we describe the effect of CGP 40116 on whole-cell currents induced by excitatory amino acids in cultured mouse spinal cord cells by use of the whole-cell patch-clamp technique. (openaire.eu)
  • EPSCs are illustrated in baseline condition in presence of gammaaminobutyric acid type A and AMPA receptor antagonists (1), after VEGF application (2) and APV (50 μ M ) (3) treatment. (nih.gov)
  • Isomers of 2-amino-7-phosphonoheptanoic acid as antagonists of neuronal excitants. (semanticscholar.org)
  • In the presence of the excitatory amino acid receptor antagonists 6,7-dinitroquinoxaline-2,3-dione (DNQX) and (±)-2-amino-5- phosphonovalerate (APV), stimulation in stratum pyramidale or proximal stratum radiatum evoked GABA(A) receptor-mediated, fast monosynaptic inhibitory postsynaptic currents (IPSCs) and GABA(B) receptor-mediated, late monosynaptic IPSCs. (elsevier.com)
  • The μ-selective opioid peptide [d-Ala 2 ,N-Me-Phe 4 ,Gly-ol 5 ]-enkephalin (DAGO) reversibly depressed directly-activated, monosynaptic inhibitory postsynaptic potentials (IPSPs) evoked in the presence of the excitatory amino acid receptor antagonists 6,7-dinitroquinoxaline-2,3-dione (DNQX) and d,l-2-amino-5-phosphonovalerate (APV) in a naloxone-sensitive manner. (elsevier.com)
  • The PAF effect was blocked by the PAF receptor antagonists BN 52021 and WEB 2086 and the N-methyl-D-aspartate receptor antagonists MK 801 and 2-amino-5-phosphonovalerate. (semanticscholar.org)
  • None of the following antagonists: DL-2-amino-5-phosphonovalerate (APV), DL-2-amino-4-phosphonobutyrate (APB) and glutamate dimethyl ester (GDEE), prazosin, ketanserin or atropine influenced the excitatory amino agonist stimulation of InsPs. (muscimol.xyz)
  • In vesicular gamma-amino butyric acid (GABA) transporter (VGAT)-channelrhodopsin2 (ChR2)-enhanced yellow fluorescent protein (EYFP) transgenic mice, NCAM is expressed postnatally at perisomatic synaptic puncta of EYFP-labeled parvalbumin, somatostatin and calretinin-positive interneurons, and in the neuropil in the anterior cingulate cortex (ACC). (frontiersin.org)
  • Gamma-amino butyric acid (GABA) GABAergic interneurons are critical determinants of cortical network function. (frontiersin.org)
  • At lower concentrations, no evidence of a distinct secondary component was evident in contrast to 4-naphthalen-1-yl-3 a ,4,5,9 b -tetrahydro-3 H -cyclopenta[ c ]quinoline-8-sulfonic acid amide (TQS), another type II α7 PAM. (aspetjournals.org)
  • Gabapentin, an amino acid designed as a structural analog of GABA ( Sills, 2006 ), is a novel anticonvulsant drug that came into clinical use as adjunctive therapy in the treatment of human seizures. (jneurosci.org)
  • The concentrations of norepinephrine, 3,4-dihydroxyphenylacetic acid (DOPAC) and 5-hydroxyindole acetic acid (5HIAA) in the brain regions were unaffected by the theanine administration except in striatum. (springer.com)
  • Amino acid assignment to one of three blood-brain barrier amino acid carriers. (springer.com)
  • Developments in amino acid transport, illustrated for the blood-brain barrier. (springer.com)
  • Effects of thiol-reagents on [ 3 H]α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid binding to rat telencephalic membranes. (springer.com)
  • Displacement of excitatory amino acid receptor ligands by acidic oligopeptides. (springer.com)
  • Single amino acid deletion in transmembrane segment D4S6 of sodium channel Scn8a (Nav1.6) in a mouse mutant with a chronic movement disorder. (neurotree.org)
  • The causative toxin (the excitatory amino acid domoic acid or DA) was produced by the diatom species Pseudo-nitzschia pungens f. multiseries (= Nitzschia pungens f. multiseries ) (Hallegraeff, 1995). (fao.org)
  • DA is a crystalline water-soluble acidic amino acid. (fao.org)
  • Pharmacological studies indicate that these photoisomers bind less strongly to the kainate receptor proteins than DA itself suggesting that they are not as toxic as the parent amino acid. (fao.org)
  • 2-Amino-7-phosphonoheptanoic acid inhibits insulin-induced convulsions and striatal aspartate accumulation in rats with frontal cortical ablation. (semanticscholar.org)
  • Focal injection of 2-amino-7-phosphonoheptanoic acid into prepiriform cortex protects against pilocarpine-induced limbic seizures in rats. (semanticscholar.org)
  • Anticonvulsant action of 2-amino-7-phosphonoheptanoic acid and muscimol in the deep prepiriform cortex. (semanticscholar.org)
  • Effect of 2-amino-7-phosphonoheptanoic acid on regional brain amino acid levels in fed and fasted rodents. (semanticscholar.org)
  • Protection against chemically induced seizures by 2-amino-7-phosphonoheptanoic acid. (semanticscholar.org)
  • MK-801 and d-2-amino-5-phosphonovaleric acid (d-(-)-AP5) selectively inhibited the labeling of M r 68,000 and 90,000 polypeptides. (elsevier.com)
  • 4. Exogenously applied γ-aminobutyric acid (GABA) depolarized cells when the recording electrode contained potassium chloride (reversal potential was -45 mV) and hyperpolarized cells when the recording electrode contained potassium methylsulphate (reversal potential was -70 mV). 5. (elsevier.com)
  • In the presence of bicuculline, the residual PSP was blocked by kynurenic acid, whereas DL-2-amino-5-phosphonovaleric acid (2-APV) reduced its amplitude to 80% of control. (elsevier.com)
  • In adults, the majority of glutamate binding sites were ion-independent and mainly sensitive to D,L-amino-5-phospho-valeric acid and N-methyl-D-aspartate. (muscimol.xyz)
  • Throughout development and in both layers, sites displaced by kainate were present at low density and sites displaced by D,L-2-amino-4-phosphonobutyric acid were not detected. (muscimol.xyz)
  • The rats receiving microinjections of naloxone (NTX, a nonselective opioid antagonist) or D-AP-5 (a selective N-methyl-D-aspartic acid-type glutamate receptor antagonist) prior to DAMGO microinjection were tested for food intake at 60, 120, and 240 min after the injections. (bvsalud.org)
  • ATP-evoked unit responses in HE2 rats were reduced significantly by topical application of the N-methyl-d-aspartate receptor antagonist, d(-)-2-amino-5-phosphonopentanoic acid (AP5) in a dose-related manner, while units from LE2 were not affected. (umn.edu)
  • An excitatory amino acid, possibly L-glutamate, which probably acts as a neurotransmitter at the inner hair cell-afferent fiber synapses in the cochlea. (neuroreille.com)
  • In the present study, we have used an electrophysiological approach to investigate at this level the presence of a major type of excitatory amino acid receptor, namely the glutamatergic receptor for which N-methyl-D-aspartate is a selective agonist. (neuroreille.com)
  • 2. Iontophoretic ejection of gamma-aminobutyric acid (GABA) from a micropipette placed near the surface of a cell resulted in a slight hyperpolarization, accompanied by a marked reduction in input resistance. (children-of-the-amphioxus.com)
  • N-methylaspartate, quinolinic acid and quisqualic acid depressed the responses, but only the former two compounds appeared to be antagonized by 2-amino-5-phosphonovalerate. (zoneroot.icu)
  • We isolated four mycophenolic acid (MA) -resistant clones (MA0.4, MA2, MA5, MA20) of murine leukemia (L1210) cells which were 2- to 125-fold more resistant than the parent cells to MA and had a 4- to 50-fold increase in the activity of the enzyme inosine monophosphate dehydrogenase (IMPDase). (statescale.tk)
  • The effects of excitatory amino acid agonists on [3H]inositol phosphates (InsPs) levels have been examined in rabbit retinal tissues under basal conditions and after agonist stimulation. (muscimol.xyz)
  • Quisqualate (QA) is the most effective excitatory amino acid agonist at stimulating InsPs accumulation with an EC50 value of 0.1 microM. (muscimol.xyz)
  • QA, and to a lesser extent other excitatory amino acid agonists, were also effective in stimulating InsPs accumulation and the mobilization of internal calcium levels in 3-5-day-old retinal cultures but not in the older cultures (25-30 days old), which lack neurones but contain Müller cells. (muscimol.xyz)
  • We tested whether GABA release to identified hippocampal neurons is influenced by group III mGluR activation using the agonist L-(+)-2-amino-4-phosphonobutyric acid (L-AP4) on inhibitory postsynaptic currents (IPSCs) evoked in CA1 interneurons and pyramidal cells. (ox.ac.uk)
  • An amino acid that occurs in endogenous proteins. (uchicago.edu)
  • In keeping with the notion of random convergence and divergence of OB axons in PCx, electrophysiological studies show that each odorant activates an apparently random population of from 3% to 15% of the neurons in layer 2 of the PCx at low concentration ( Stettler and Axel, 2009 ). (elifesciences.org)
  • However, anatomical reconstructions of individual layer 6 corticothalamic (L6 CT) neurons include examples with axonal processes ramifying within layer 5, and the relative input of the overall population of L6 CT neurons to layers 4 and 5 is not well understood. (stanford.edu)
  • We compared the synaptic impact of L6 CT cells on neurons in layers 4 and 5. (stanford.edu)
  • 2. The effect of THA on postsynaptic GABA(B) receptor-mediated responses was studied in neurons perfused internally with potassium gluconate and guanosine triphosphate (GTP). (elsevier.com)
  • Neurons had CCG-1423 been treated with Ro 25C6981 (0.5 M, 15 min) or Co 101244 (5 M, 15 min) before and during glutamate exposure. (paccon2016.com)
  • 3) growth factors such as ciliary neuronotrophic factor or basic fibroblast growth factor but not nerve growth factor repress 5-hydroxytryptamine and calcitonin gene-related peptide immunoreactivity in cultured sensory neurons. (ac.be)
  • A selective N-methyl-D-aspartate antagonist, DL-2-amino-5-phosphonovalerate, was found to produce PCP-like catalepsy, discriminative stimulus effects, and stereotyped operant responding in pigeons when administered intramuscularly. (eurekamag.com)
  • GC migration toward VEGF in vitro was blocked by the NMDAR antagonist D -APV ( D -2-amino-5-phosphono-valerate), and analyses of the effects of D -APV and αFlk1 on GC migration in cerebellar slices were consistent with Flk1 and NMDAR mediating GC migration through a common pathway. (sciencemag.org)
  • Yamada, N & Bilkey, DK 1993, ' Induction of trypsin-induced hyperexcitability in the rat hippocampal slice is blocked by the N-methyl-d-aspartate receptor antagonist, MK-801 ', Brain Research , vol. 624, no. 1-2, pp. 336-338. (elsevier.com)
  • Our results show that, when N-methyl-D-aspartate and the antagonist 2-amino-5-phosphonovalerate are perfused through the perilymphatic scalae, they induced, by different mechanisms, a significant reduction of the amplitude of the compound action potential and an increase of the N1 latency, both predominant at high intensity tone burst stimulations. (neuroreille.com)
  • DL- 2-Amino-5-phosphonovalerate (AP5) is a potent and highly selective NMA antagonist 8. (awaremed.com)
  • Lambert, NA & Wilson, WA 1993, ' Discrimination of post- and presynaptic GABA(B) receptor-mediated responses by tetrahydroaminoacridine in area CA3 of the rat hippocampus ', Journal of Neurophysiology , vol. 69, no. 2, pp. 630-635. (elsevier.com)
  • Previous reports suggested that a novel stimulus pattern of multi-train stimulus at low-frequency (2-Hz or 5-Hz) could induce stable long-term depression (LTD) in the CA1 area of adult rat hippocampus . (bvsalud.org)
  • 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)
  • It is used as an adjunct to inhaled beta -2 selective agonists and systemically administered corticosteroids. (lookformedical.com)
  • Consistently, silencing the expression of the VEGF receptor 2 (VEGFR2) in neural cells impairs hippocampal-dependent synaptic plasticity and consolidation of emotional memory. (nih.gov)
  • Laser scanning photostimulation revealed that NCAM deletion increased the strength of close-in inhibitory connections to layer 2/3 pyramidal cells of the ACC. (frontiersin.org)
  • Conditioning stumulation of white matter (2 Hz, 15 minutes) produced LTPs of f- (8 cells out of 13 tested cells) and sEPSP (10/13). (nii.ac.jp)
  • The level of the labeled cytoplasmic TfR mRNA exhibited about 2-3-fold increase and the level of the labeled GSHPx mRNA about 2-fold increase in induced Friend 707 cells in comparison with uninduced cells. (faintpower.tk)
  • 2) The agreement, hailed as a 'landmark' deal and a breakthrough by politicians and the green lobby alike, came before a crucial EU summit opening in Brussels tomorrow at which 27 prime ministers and presidents are supposed to finalise an ambitious package to cut greenhouse gas emissions by 20% by 2020. (comparewords.com)
  • Transverse slices (∼300 μm) were kept for 1-4 h before recording at 22-24°C, in the above solution but with (in mM) CaCl 2 2.5, MgCl 2 1. (rupress.org)
  • 2 The activation of MORs result in reduction of 3′-5′-cyclic adenosine monophosphate, membrane hyperpolarization, and subsequent neuronal depression. (asahq.org)
  • However, unlike these PAMs, A-867744 displaced the binding of the agonist [ 3 H](1 S ,4 S )-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane (A-585539) in rat cortex, with a K i value of 23 nM. (aspetjournals.org)
  • A-867744 neither increased agonist-evoked responses nor displaced the binding of [ 3 H]A-585539 in an α7/5-hydroxytryptamine 3 (α7/5-HT 3 ) chimera, suggesting an interaction distinct from the α7 N terminus or M2-3 loop. (aspetjournals.org)
  • 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)
  • Although the precise cause of AD remains elusive, it is widely accepted that oligomerization of A β P and the consequent neurodegeneration might be the cause of neuronal death in AD patients [ 2 , 3 ]. (hindawi.com)
  • 5. Stimulation of the hilus during the first week of life evoked a GDP followed by a hyperpolarization. (nih.gov)
  • Here, we utilized the serendipitous placement of subthalamic deep brain stimulation leads in 6 + 5 Parkinsonian patients to directly investigate the effects of zona incerta stimulation on human pain perception. (bvsalud.org)
  • Depression of monosynaptic inhibitory postsynaptic potentials (IPSPs) by DAGO was not prevented by 1-2 mM Ba 2+ . (elsevier.com)
  • Reduction effect of theanine on blood pressure and brain 5-hydroxyindoles in spontaneously hypertensive rats. (springer.com)
  • Ovariectomized (OvX) female rats were treated with high E2 (HE2) or low dose E2 (LE2) for 2 days and neural activity was recorded in laminae I-II at the Vc/C 1-2 region. (umn.edu)
  • or 5 mg/kg, iv) and was partially inhibited by pretreatment of AP-5 (50, 100 microg/rat, icv), but was not changed by systemic administration of AP-5 (10 mg/kg, iv). (nel.edu)
  • In vitro measurements with Elvax containing 3H-MK801 revealed that the amount of drug released declined sharply over the first 10 d and then stabilized at a fairly constant rate for the following 5 weeks. (ox.ac.uk)
  • Actions of D and L forms of 2-amino-5-phosphonovalerate and 2-amino-4-phosphonobutyrate in the cat spinal cord. (abcam.com)
  • Biochemistry laboratory training is an essential component of careers in biochemistry, molecular biology, chemistry, and related molecular life sciences such â ¦ 2-amino-5-phosphonovalerate - 3' end - 5' end. (consolehealthcare.com)
  • So it is suggested that LTD induced by 2-Hz multi-train tetanus involves co-activation of NMDARs and mGluRs, while LTD induced by 5-Hz multi-train tetanus is only related to activation of mGluRs. (bvsalud.org)
  • Somatosensory cortex layer 2/3 neurones with pyramidal shaped somata were selected using an infrared differential interference contrast optics, and recordings were made with patch pipettes (4 MΩ) filled with (in mM) 50 KCl, 55 K-gluconate, 10 NaCl, 10 HEPES, 2 MgATP, 0.1 EGTA, pH 7.35. (rupress.org)
  • To cast light on this issue in the CA1 region of the hippocampal slice, we used a train of stimuli, to the pyramidal layer, comprising 1 s at 40 Hz followed by 2--3 s at 10 Hz, to mimic the frequency pattern observed during fast oscillations. (ox.ac.uk)
  • The results showed that both AP5 and MCPG inhibited the LTD induced by 2-Hz multi-train stimulus. (bvsalud.org)
  • In the present study, sustained application (5 min) of nicotine significantly lowered the threshold for synaptic plasticity, and thus a long-lasting potentiation was induced by a stimulus that would normally evoke only a short-term potentiation. (ox.ac.uk)
  • 2. L‐Glutamate evoked an inward current at membrane potentials between ‐140 and +50 mV. (deepdyve.com)
  • The reversal point for the potential change was about 5 mV greater than the resting membrane potential. (children-of-the-amphioxus.com)
  • Submitted for publication February 2, 1996. (asahq.org)
  • There are several mechanisms that account for A β P-induced calcium dyshomeostasis [ 5 - 7 ]. (hindawi.com)
  • Adenosine did not change fast inhibitory synaptic potentials (IPSPs) but depressed late IPSPs evoked by direct activation of interneurons in the presence of 6,7-dinitroquinoxaline-2,3-dione (DNQX) and D,L-2-amino-5-phosphonovalerate (APV). (omeka.net)
  • NTX (26.5 nmol in 0.5 µl) injected into the CeA antagonized DAMGO-induced feeding but D-AP-5 (6.3-25.4 nmol in 0.5 µl) injections did not produce such an effect. (bvsalud.org)
  • Without affecting the food intake, injection of 6.34, 12.70, or 25.40 nmol D-AP-5 into the CeA significantly decreased water intake 0-1 h after the injection (F(3,28)=3.118, P=0.042) independent of food intake. (bvsalud.org)
  • CGP 40116 (5-40 mg/kg i.v.) was injected immediately following permanent occlusion of the left middle cerebral artery (MCA). (curehunter.com)
  • Brains were removed rapidly and placed into ice-cold saline (in mM) NaCl 138, KCl 3, CaCl 2 0.5, MgCl 2 2.5, NaH 2 PO 4 1, NaHCO 3 25, glucose 15, pH 7.4 gassed with 95% O 2 -5% CO 2 . (rupress.org)
  • Our cross sectional study was conducted on 150 Egyptian pregnant females with gestational diabetes aged 19-39 years diagnosed by 75-g 2-hour oral glucose tolerance test. (statescale.tk)
  • glu·co·sa·mine/ ( gloo-ko´sah-mēn ) an amino derivative of glucose, occurring in glycosaminoglycans and a variety of complex polysaccharides such as blood group substances. (thefreedictionary.com)
  • An amino derivative of glucose, C 6 H 13 NO 5 , in which an amino group replaces a hydroxyl group. (thefreedictionary.com)