Endogenous amino acids released by neurons as excitatory neurotransmitters. Glutamic acid is the most common excitatory neurotransmitter in the brain. Aspartic acid has been regarded as an excitatory transmitter for many years, but the extent of its role as a transmitter is unclear.
Drugs that bind to and activate excitatory amino acid receptors.
A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.
A neuronal and epithelial type glutamate plasma membrane transporter protein.
A glial type glutamate plasma membrane transporter protein found predominately in ASTROCYTES. It is also expressed in HEART and SKELETAL MUSCLE and in the PLACENTA.
A glutamate plasma membrane transporter protein found in ASTROCYTES and in the LIVER.
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 glutamate plasma membrane transporter protein that is primarily expressed in cerebellar PURKINJE CELLS on postsynaptic DENDRITIC SPINES.
A family of plasma membrane neurotransmitter transporter proteins that couple the uptake of GLUTAMATE with the import of SODIUM ions and PROTONS and the export of POTASSIUM ions. In the CENTRAL NERVOUS SYSTEM they regulate neurotransmission through synaptic reuptake of the excitatory neurotransmitter glutamate. Outside the central nervous system they function as signal mediators and regulators of glutamate metabolism.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
A family of POTASSIUM and SODIUM-dependent acidic amino acid transporters that demonstrate a high affinity for GLUTAMIC ACID and ASPARTIC ACID. Several variants of this system are found in neuronal tissue.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
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.
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.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
A glutamate plasma membrane transporter protein that is primarily expressed in the RETINA.
(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 broad-spectrum excitatory amino acid antagonist used as a research tool.
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.
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.
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.
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.
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 neurotoxic isoxazole (similar to KAINIC ACID and MUSCIMOL) found in AMANITA mushrooms. It causes motor depression, ataxia, and changes in mood, perceptions and feelings, and is a potent excitatory amino acid agonist.
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.
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.
An IBOTENIC ACID homolog and glutamate agonist. The compound is the defining agonist for the AMPA subtype of glutamate receptors (RECEPTORS, AMPA). It has been used as a radionuclide imaging agent but is more commonly used as an experimental tool in cell biological studies.
A family of tricyclic hydrocarbons whose members include many of the commonly used tricyclic antidepressants (ANTIDEPRESSIVE AGENTS, TRICYCLIC).
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.
Depolarization of membrane potentials at the SYNAPTIC MEMBRANES of target neurons during neurotransmission. Excitatory postsynaptic potentials can singly or in summation reach the trigger threshold for ACTION POTENTIALS.
A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.
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.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
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.
The most common inhibitory neurotransmitter in the central nervous system.
Derivatives of BUTYRIC ACID that contain one or more amino groups attached to the aliphatic structure. Included under this heading are a broad variety of acid forms, salts, esters, and amides that include the aminobutryrate structure.
Drugs used for their actions on any aspect of excitatory amino acid neurotransmitter systems. Included are drugs that act on excitatory amino acid receptors, affect the life cycle of excitatory amino acid transmitters, or affect the survival of neurons using excitatory amino acids.
A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.
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.
Substances used for their pharmacological actions on any aspect of neurotransmitter systems. Neurotransmitter agents include agonists, antagonists, degradation inhibitors, uptake inhibitors, depleters, precursors, and modulators of receptor function.
A class of ionotropic glutamate receptors characterized by their affinity for the agonist AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid).
A non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.
Toxic substances from microorganisms, plants or animals that interfere with the functions of the nervous system. Most venoms contain neurotoxic substances. Myotoxins are included in this concept.
A metabolite in the principal biochemical pathway of lysine. It antagonizes neuroexcitatory activity modulated by the glutamate receptor, N-METHYL-D-ASPARTATE; (NMDA).
An amino acid formed by cyclization of leucine. It has cytostatic, immunosuppressive and antineoplastic activities.
The lower portion of the BRAIN STEM. It is inferior to the PONS and anterior to the CEREBELLUM. Medulla oblongata serves as a relay station between the brain and the spinal cord, and contains centers for regulating respiratory, vasomotor, cardiac, and reflex activities.
The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
Membrane transporters that co-transport two or more dissimilar molecules in the same direction across a membrane. Usually the transport of one ion or molecule is against its electrochemical gradient and is "powered" by the movement of another ion or molecule with its electrochemical gradient.
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.
A class of ionotropic glutamate receptors characterized by their affinity for KAINIC ACID.
The D-isomer of ASPARTIC ACID.
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.
Use of electric potential or currents to elicit biological responses.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
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.
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
The relationship between the dose of an administered drug and the response of the organism to the drug.
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).
Cellular proteins and protein complexes that transport amino acids across biological membranes.
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.
Therapeutic introduction of ions of soluble salts into tissues by means of electric current. In medical literature it is commonly used to indicate the process of increasing the penetration of drugs into surface tissues by the application of electric current. It has nothing to do with ION EXCHANGE; AIR IONIZATION nor PHONOPHORESIS, none of which requires current.
The thin layer of GRAY MATTER on the surface of the CEREBRAL HEMISPHERES that develops from the TELENCEPHALON and folds into gyri and sulchi. It reaches its highest development in humans and is responsible for intellectual faculties and higher mental functions.
An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
A technique for measuring extracellular concentrations of substances in tissues, usually in vivo, by means of a small probe equipped with a semipermeable membrane. Substances may also be introduced into the extracellular space through the membrane.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
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.
The function of opposing or restraining the excitation of neurons or their target excitable cells.
A class of large neuroglial (macroglial) cells in the central nervous system - the largest and most numerous neuroglial cells in the brain and spinal cord. Astrocytes (from "star" cells) are irregularly shaped with many long processes, including those with "end feet" which form the glial (limiting) membrane and directly and indirectly contribute to the BLOOD-BRAIN BARRIER. They regulate the extracellular ionic and chemical environment, and "reactive astrocytes" (along with MICROGLIA) respond to injury.
The rate dynamics in chemical or physical systems.
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.
A conditionally essential nutrient, important during mammalian development. It is present in milk but is isolated mostly from ox bile and strongly conjugates bile acids.
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.
The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments.
A metabolite of tryptophan with a possible role in neurodegenerative disorders. Elevated CSF levels of quinolinic acid are correlated with the severity of neuropsychological deficits in patients who have AIDS.
Bluish-colored region in the superior angle of the FOURTH VENTRICLE floor, corresponding to melanin-like pigmented nerve cells which lie lateral to the PERIAQUEDUCTAL GRAY.
An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.
The domestic cat, Felis catus, of the carnivore family FELIDAE, comprising over 30 different breeds. The domestic cat is descended primarily from the wild cat of Africa and extreme southwestern Asia. Though probably present in towns in Palestine as long ago as 7000 years, actual domestication occurred in Egypt about 4000 years ago. (From Walker's Mammals of the World, 6th ed, p801)
Neurons which activate MUSCLE CELLS.
Refers to animals in the period of time just after birth.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
Drugs that interrupt transmission at the skeletal neuromuscular junction by causing sustained depolarization of the motor end plate. These agents are primarily used as adjuvants in surgical anesthesia to cause skeletal muscle relaxation.
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.
The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.
A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.
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.
Cell surface proteins that bind signalling molecules external to the cell with high affinity and convert this extracellular event into one or more intracellular signals that alter the behavior of the target cell (From Alberts, Molecular Biology of the Cell, 2nd ed, pp693-5). Cell surface receptors, unlike enzymes, do not chemically alter their ligands.
Substances that act in the brain stem or spinal cord to produce tonic or clonic convulsions, often by removing normal inhibitory tone. They were formerly used to stimulate respiration or as antidotes to barbiturate overdose. They are now most commonly used as experimental tools.
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 that are not synthesized by the human body in amounts sufficient to carry out physiological functions. They are obtained from dietary foodstuffs.
Drugs used to prevent SEIZURES or reduce their severity.
Drugs that bind to and activate dopamine receptors.
Extensions of the nerve cell body. They are short and branched and receive stimuli from other NEURONS.
An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison.
Elements of limited time intervals, contributing to particular results or situations.
The part of the brain that connects the CEREBRAL HEMISPHERES with the SPINAL CORD. It consists of the MESENCEPHALON; PONS; and MEDULLA OBLONGATA.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust.
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.
Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.
Common name for the only family (Petromyzontidae) of eellike fish in the order Petromyzontiformes. They are jawless but have a sucking mouth with horny teeth.
Most generally any NEURONS which are not motor or sensory. Interneurons may also refer to neurons whose AXONS remain within a particular brain region in contrast to projection neurons, which have axons projecting to other brain regions.
Transport proteins that carry specific substances in the blood or across cell membranes.
Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.
A plant genus of the family GERANIACEAE. Geranium is also used as a common name for PELARGONIUM.
Paired bundles of NERVE FIBERS entering and leaving the SPINAL CORD at each segment. The dorsal and ventral nerve roots join to form the mixed segmental spinal nerves. The dorsal roots are generally afferent, formed by the central projections of the spinal (dorsal root) ganglia sensory cells, and the ventral roots are efferent, comprising the axons of spinal motor and PREGANGLIONIC AUTONOMIC FIBERS.
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.
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.
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.
A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.
The ten-layered nervous tissue membrane of the eye. It is continuous with the OPTIC NERVE and receives images of external objects and transmits visual impulses to the brain. Its outer surface is in contact with the CHOROID and the inner surface with the VITREOUS BODY. The outer-most layer is pigmented, whereas the inner nine layers are transparent.
The commonest and widest ranging species of the clawed "frog" (Xenopus) in Africa. This species is used extensively in research. There is now a significant population in California derived from escaped laboratory animals.
Established cell cultures that have the potential to propagate indefinitely.
A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.
A metallic element that has the atomic symbol Mg, atomic number 12, and atomic weight 24.31. It is important for the activity of many enzymes, especially those involved in OXIDATIVE PHOSPHORYLATION.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
An opioid analgesic with actions and uses similar to MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1095)
The output neurons of the cerebellar cortex.
Interstitial space between cells, occupied by INTERSTITIAL FLUID as well as amorphous and fibrous substances. For organisms with a CELL WALL, the extracellular space includes everything outside of the CELL MEMBRANE including the PERIPLASM and the cell wall.
Introduction of therapeutic agents into the spinal region using a needle and syringe.
Pinched-off nerve endings and their contents of vesicles and cytoplasm together with the attached subsynaptic area of the membrane of the post-synaptic cell. They are largely artificial structures produced by fractionation after selective centrifugation of nervous tissue homogenates.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
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.
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.
A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.
Peptides composed of two amino acid units.
Cell membranes associated with synapses. Both presynaptic and postsynaptic membranes are included along with their integral or tightly associated specializations for the release or reception of transmitters.
The non-neuronal cells of the nervous system. They not only provide physical support, but also respond to injury, regulate the ionic and chemical composition of the extracellular milieu, participate in the BLOOD-BRAIN BARRIER and BLOOD-RETINAL BARRIER, form the myelin insulation of nervous pathways, guide neuronal migration during development, and exchange metabolites with neurons. Neuroglia have high-affinity transmitter uptake systems, voltage-dependent and transmitter-gated ion channels, and can release transmitters, but their role in signaling (as in many other functions) is unclear.
A class of opioid peptides including dynorphin A, dynorphin B, and smaller fragments of these peptides. Dynorphins prefer kappa-opioid receptors (RECEPTORS, OPIOID, KAPPA) and have been shown to play a role as central nervous system transmitters.
Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.
The distal terminations of axons which are specialized for the release of neurotransmitters. Also included are varicosities along the course of axons which have similar specializations and also release transmitters. Presynaptic terminals in both the central and peripheral nervous systems are included.
A reduction in brain oxygen supply due to ANOXEMIA (a reduced amount of oxygen being carried in the blood by HEMOGLOBIN), or to a restriction of the blood supply to the brain, or both. Severe hypoxia is referred to as anoxia, and is a relatively common cause of injury to the central nervous system. Prolonged brain anoxia may lead to BRAIN DEATH or a PERSISTENT VEGETATIVE STATE. Histologically, this condition is characterized by neuronal loss which is most prominent in the HIPPOCAMPUS; GLOBUS PALLIDUS; CEREBELLUM; and inferior olives.
Changes in the amounts of various chemicals (neurotransmitters, receptors, enzymes, and other metabolites) specific to the area of the central nervous system contained within the head. These are monitored over time, during sensory stimulation, or under different disease states.
A bundle of NERVE FIBERS connecting each posterior horn of the spinal cord to the opposite side of the THALAMUS, carrying information about pain, temperature, and touch. It is one of two major routes by which afferent spinal NERVE FIBERS carrying sensations of somaesthesis are transmitted to the THALAMUS.
Neural tracts connecting one part of the nervous system with another.
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.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.
A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Picrotoxin blocks the GAMMA-AMINOBUTYRIC ACID-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
Specific sites or molecular structures on cell membranes or in cells with which phencyclidine reacts or to which it binds to elicit the specific response of the cell to phencyclidine. Studies have demonstrated the presence of multiple receptor sites for PCP. These are the PCP/sigma site, which binds both PCP and psychotomimetic opiates but not certain antipsychotics, and the PCP site, which selectively binds PCP analogs.
Proteins prepared by recombinant DNA technology.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
A family of vesicular neurotransmitter transporter proteins that were originally characterized as sodium dependent inorganic phosphate cotransporters. Vesicular glutamate transport proteins sequester the excitatory neurotransmitter GLUTAMATE from the CYTOPLASM into SECRETORY VESICLES in exchange for lumenal PROTONS.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
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 interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
Gated, ion-selective glycoproteins that traverse membranes. The stimulus for ION CHANNEL GATING can be due to a variety of stimuli such as LIGANDS, a TRANSMEMBRANE POTENTIAL DIFFERENCE, mechanical deformation or through INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
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).
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
Elongated gray mass of the neostriatum located adjacent to the lateral ventricle of the brain.
Amino acids containing an aromatic side chain.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
An involuntary movement or exercise of function in a part, excited in response to a stimulus applied to the periphery and transmitted to the brain or spinal cord.
A family of voltage-gated eukaryotic porins that form aqueous channels. They play an essential role in mitochondrial CELL MEMBRANE PERMEABILITY, are often regulated by BCL-2 PROTO-ONCOGENE PROTEINS, and have been implicated in APOPTOSIS.
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.
The ability of a substrate to allow the passage of ELECTRONS.
GRAY MATTER located in the dorsomedial part of the MEDULLA OBLONGATA associated with the solitary tract. The solitary nucleus receives inputs from most organ systems including the terminations of the facial, glossopharyngeal, and vagus nerves. It is a major coordinator of AUTONOMIC NERVOUS SYSTEM regulation of cardiovascular, respiratory, gustatory, gastrointestinal, and chemoreceptive aspects of HOMEOSTASIS. The solitary nucleus is also notable for the large number of NEUROTRANSMITTERS which are found therein.
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.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
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.
Nerve structures through which impulses are conducted from a peripheral part toward a nerve center.
A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.
A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.
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 thiol-containing non-essential amino acid that is oxidized to form CYSTINE.
Negatively charged atoms, radicals or groups of atoms which travel to the anode or positive pole during electrolysis.
The observable response an animal makes to any situation.
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or "seizure disorder."
Amino acids which have a branched carbon chain.
Central gray matter surrounding the CEREBRAL AQUEDUCT in the MESENCEPHALON. Physiologically it is probably involved in RAGE reactions, the LORDOSIS REFLEX; FEEDING responses, bladder tonus, and pain.
The phylogenetically newer part of the CORPUS STRIATUM consisting of the CAUDATE NUCLEUS and PUTAMEN. It is often called simply the striatum.
An essential branched-chain amino acid important for hemoglobin formation.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
Used as a solvent, in the manufacture of insecticides, and for treating sweet potatoes before planting. May cause nausea, vomiting, pains in head and chest, stupefaction. Irritates mucous membranes and causes kidney and liver degeneration.
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
The front part of the hindbrain (RHOMBENCEPHALON) that lies between the MEDULLA and the midbrain (MESENCEPHALON) ventral to the cerebellum. It is composed of two parts, the dorsal and the ventral. The pons serves as a relay station for neural pathways between the CEREBELLUM to the CEREBRUM.
A process of selective diffusion through a membrane. It is usually used to separate low-molecular-weight solutes which diffuse through the membrane from the colloidal and high-molecular-weight solutes which do not. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
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.
Microscopy in which the samples are first stained immunocytochemically and then examined using an electron microscope. Immunoelectron microscopy is used extensively in diagnostic virology as part of very sensitive immunoassays.
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
The physical activity of a human or an animal as a behavioral phenomenon.
The motor nerve of the diaphragm. The phrenic nerve fibers originate in the cervical spinal column (mostly C4) and travel through the cervical plexus to the diaphragm.
Slender processes of NEURONS, including the AXONS and their glial envelopes (MYELIN SHEATH). Nerve fibers conduct nerve impulses to and from the CENTRAL NERVOUS SYSTEM.

Activity-dependent metaplasticity of inhibitory and excitatory synaptic transmission in the lamprey spinal cord locomotor network. (1/1909)

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)

Ischemic tolerance in murine cortical cell culture: critical role for NMDA receptors. (2/1909)

Murine cortical cultures containing both neurons and glia (days in vitro 13-15) were exposed to periods of oxygen-glucose deprivation (5-30 min) too brief to induce neuronal death. Cultures "preconditioned" by sublethal oxygen-glucose deprivation exhibited 30-50% less neuronal death than controls when exposed to a 45-55 min period of oxygen-glucose deprivation 24 hr later. This preconditioning-induced neuroprotection was specific in that neuronal death induced by exposure to excitotoxins or to staurosporine was not attenuated. Neuroprotection was lost if the time between the preconditioning and severe insult were decreased to 7 hr or increased to 72 hr and was blocked if the NMDA antagonist 100 microM 3-((D)-2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid was applied during the preconditioning insult. This was true even if the duration of preconditioning was increased as far as possible (while still remaining sublethal). A similar preconditioning effect was also produced by sublethal exposure to high K+, glutamate, or NMDA but not to kainate or trans-1-aminocyclopentane-1, 3-dicarboxylic acid.  (+info)

Ergoline derivative LEK-8829-induced turning behavior in rats with unilateral striatal ibotenic acid lesions: interaction with bromocriptine. (3/1909)

LEK-8829 [9,10-didehydro-N-methyl-(2-propynyl)-6-methyl-8- aminomethylergoline bimaleinate] is an antagonist of dopamine D2 receptors and serotonin (5-HT)2 and 5-HT1A receptors in intact animals and a D1 receptor agonist in dopamine-depleted animals. In the present study, we used rats with unilateral striatal lesions with ibotenic acid (IA) to investigate the dopamine receptor activities of LEK-8829 in a model with innervated dopamine receptors. The IA-lesioned rats circled ipsilaterally when challenged with apomorphine, the mixed agonist on D1/D2 receptors. LEK-8829 induced a dose-dependent contralateral turning that was blocked by D1 receptor antagonist SCH-23390. The treatment with D1 receptor agonist SKF-82958 induced ipsilateral turning, whereas the treatment with D2 receptor antagonist haloperidol induced contralateral posture. The combined treatment with SKF-82958 and haloperidol resulted in a weak contralateral turning, indicating the possible receptor mechanism of contralateral turning induced by LEK-8829. Bromocriptine induced a weak ipsilateral turning that was blocked by haloperidol. The ipsilateral turning induced by bromocriptine was significantly potentiated by the coadministration of a low dose but not by a high dose of LEK-8829. The potentiation of turning was blocked either by SCH-23390 or by haloperidol. The potentiation of ipsilateral turning suggests the costimulation of D2 and D1 receptors by bromocriptine and LEK-8829, respectively, whereas the lack of potentiation by the highest dose of LEK-8829 may be explained by the opposing activity of LEK-8829 and bromocriptine at D2 receptors. We propose that the D2 and 5HT2 receptor-blocking and D1 receptor-stimulating profile of LEK-8829 is promising for the treatment of negative symptoms of schizophrenia.  (+info)

Neuroprotection of the developing brain by systemic administration of vasoactive intestinal peptide derivatives. (4/1909)

Periventricular leukomalacia (PVL), a necrotic and often cystic lesion of the cerebral white matter occurring in very premature babies, is the leading cause of cerebral palsy in this population. Increased glutamate release and the excitotoxic cascade thus triggered may be critical factors in the development of PVL. The glutamatergic analog ibotenate injected intracerebrally into newborn mice produces white matter cysts that mimic human PVL. Concomitant injection of vasoactive intestinal peptide (VIP), a trophic factor, protects the white matter against excitotoxic lesions. The goal of the present study was to assess the protective properties of systemically injected VIP analogs against ibotenate-induced excitotoxic white matter lesions in newborn mice. VIP analogs were selected on the basis of their low susceptibility to endopeptidases and their potential ability to cross biological membranes. RO-25-1553, a long-lasting cyclic VIP analog, and stearyl-norleucine-VIP, a fatty derivative of VIP, reduced ibotenate-induced white matter cysts by up to 87% and 84%, respectively, when injected i.p. immediately after ibotenate. By comparison, i.p. coadministration of VIP and ibotenate was not protective against the excitotoxic insult. Furthermore, RO-25-1553 and stearyl-norleucine-VIP still induced significant neuroprotection of the developing white matter when injected systemically 8 and 12 h, respectively, after ibotenate, establishing these peptides as therapeutic agents in this murine model. VIP analogs may have therapeutic potential in human premature babies at high risk for PVL.  (+info)

Activation of metabotropic glutamate receptors modulates the voltage-gated sustained calcium current in a teleost horizontal cell. (5/1909)

In the teleost retina, cone horizontal cells contain a voltage-activated sustained calcium current, which has been proposed to be involved in visual processing. Recently, several studies have demonstrated that modulation of voltage-gated channels can occur through activation of metabotropic glutamate receptors (mGluRs). Because glutamate is the excitatory neurotransmitter in the vertebrate retina, we have used whole cell electrophysiological techniques to examine the effect of mGluR activation on the sustained voltage-gated calcium current found in isolated cone horizontal cells in the catfish retina. In pharmacological conditions that blocked voltage-gated sodium and potassium channels, as well as N-methyl-D-aspartate (NMDA) and non-NMDA channels, application of L-glutamate or 1-aminocyclopentane-1,3-dicarboxylic acid (1S,3R-ACPD) to voltage-clamped cone horizontal cells acted to increase the amplitude of the calcium current, expand the activation range of the calcium current by 10 mV into the cell's physiological operating range, and shift the peak calcium current by -5 mV. To identify and characterize the mGluR subtypes found on catfish cone horizontal cells, agonists of group I, group II, or group III mGluRs were applied via perfusion. Group I and group III mGluR agonists mimicked the effect of L-glutamate or 1S,3R-ACPD, whereas group II mGluR agonists had no effect on L-type calcium current activity. Inhibition studies demonstrated that group I mGluR antagonists significantly blocked the modulatory effect of the group I mGluR agonist, (S)-3,5-dihydroxyphenylglycine. Similar results were obtained when the group III mGluR agonist, L-2-amino-4-phosphonobutyric acid, was applied in the presence of a group III mGluR antagonist. These results provide evidence for two groups of mGluR subtypes on catfish cone horizontal cells. Activation of these mGluRs is linked to modulation of the voltage-gated sustained calcium current.  (+info)

Eye movement deficits following ibotenic acid lesions of the nucleus prepositus hypoglossi in monkeys II. Pursuit, vestibular, and optokinetic responses. (6/1909)

The eyes are moved by a combination of neural commands that code eye velocity and eye position. The eye position signal is supposed to be derived from velocity-coded command signals by mathematical integration via a single oculomotor neural integrator. For horizontal eye movements, the neural integrator is thought to reside in the rostral nucleus prepositus hypoglossi (nph) and project directly to the abducens nuclei. In a previous study, permanent, serial ibotenic acid lesions of the nph in three rhesus macaques compromised the neural integrator for fixation but saccades were not affected. In the present study, to determine further whether the nph is the neural substrate for a single oculomotor neural integrator, the effects of those lesions on smooth pursuit, the vestibulo-ocular reflex (VOR), vestibular nystagmus (VN), and optokinetic nystagmus (OKN) are documented. The lesions were correlated with long-lasting deficits in eye movements, indicated most clearly by the animals' inability to maintain steady gaze in the dark. However, smooth pursuit and sinusoidal VOR in the dark, like the saccades in the previous study, were affected minimally. The gain of horizontal smooth pursuit (eye movement/target movement) decreased slightly (<25%) and phase lead increased slightly for all frequencies (0.3-1.0 Hz, +/-10 degrees target tracking), most noticeably for higher frequencies (0.8-0.7 and approximately 20 degrees for 1.0-Hz tracking). Vertical smooth pursuit was not affected significantly. Surprisingly, horizontal sinusoidal VOR gain and phase also were not affected significantly. Lesions had complex effects on both VN and OKN. The plateau of per- and postrotatory VN was shortened substantially ( approximately 50%), whereas the initial response and the time constant of decay decreased slightly. The initial OKN response also decreased slightly, and the charging phase was prolonged transiently then recovered to below normal levels like the VN time constant. Maximum steady-state, slow eye velocity of OKN decreased progressively by approximately 30% over the course of the lesions. These results support the previous conclusion that the oculomotor neural integrator is not a single neural entity and that the mathematical integrative function for different oculomotor subsystems is most likely distributed among a number of nuclei. They also show that the nph apparently is not involved in integrating smooth pursuit signals and that lesions of the nph can fractionate the VOR and nystagmic responses to adequate stimuli.  (+info)

Distinct populations of NMDA receptors at subcortical and cortical inputs to principal cells of the lateral amygdala. (7/1909)

Fear conditioning involves the transmission of sensory stimuli to the amygdala from the thalamus and cortex. These input synapses are prime candidates for sites of plasticity critical to the learning in fear conditioning. Because N-methyl-D-aspartate (NMDA)-dependent mechanisms have been implicated in fear learning, we investigated the contribution of NMDA receptors to synaptic transmission at putative cortical and thalamic inputs using visualized whole cell recording in amygdala brain slices. Whereas NMDA receptors are present at both of these pathways, differences were observed. First, the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-receptor-mediated component of the synaptic response, relative to the NMDA component, is smaller at thalamic than cortical input synapses. Second, thalamic NMDA responses are more sensitive to Mg2+. These findings suggest that there are distinct populations of NMDA receptors at cortical and thalamic inputs to the lateral amygdala. Differences such as these might underlie unique contributions of the two pathways to fear conditioning.  (+info)

NMDA receptor characterization and subunit expression in rat cultured mesencephalic neurones. (8/1909)

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)

TY - JOUR. T1 - Bidirectional shift of group III metabotropic glutamate receptor-mediated synaptic depression in the epileptic hippocampus. AU - Dammann, Fabian. AU - Kirschstein, Timo. AU - Guli, Xiati. AU - Müller, Steffen. AU - Porath, Katrin. AU - Rohde, Marco. AU - Tokay, Tursonjan. AU - Köhling, Rüdiger. PY - 2018/1/1. Y1 - 2018/1/1. N2 - A common function of group III metabotropic glutamate receptors (mGluRs) located at the presynaptic site of a glutamatergic synapse is synaptic depression. Here, we studied synaptic depression mediated by group III mGluR activation at Schaffer collateral-CA1 (SC-CA1) synapses and associational-commissural-CA3 (AC-CA3) synapses by recording field excitatory postsynaptic potentials in the in vitro brain slice preparation. In order to gauge the impact of synaptic depression in chronically epileptic tissue, we compared rats after pilocarpine-induced status epilepticus (post-SE) with control animals. We observed that synaptic transmission at control AC-CA3 ...
Current therapies for Parkinsons disease are able to ameliorate the symptoms in the early stages, however as the disease progresses, they become less effective and patients often develop debilitating side effects. There is currently a significant unmet need for disease modifying or neuroprotective drugs to slow the rate of disease progression and provide long-term symptomatic relief. Novel therapeutics that can provide symptomatic relief whilst attenuating the ongoing neurodegeneration are therefore sought. The targeting of metabotropic glutamate (mGlu) receptors has become a therapeutic focus in recent years. The group III mGlu receptors are the focus of this thesis as they currently hold the most therapeutic promise, with evidence suggesting activation of these receptors not only modulates aberrant neurotransmission in the basal ganglia to provide symptom relief, but also provides neuroprotective effects in the nigrostriatal system through a variety of mechanisms. Recent advances in the ...
Acosta-Cabronero J, Betts MJ, Cardenas-Blanco A, Yang S, Nestor PJ (2015). In vivo MRI mapping of brain iron deposition across the adult lifespan. J.Neurosci. (in press). Betts MJ, ONeill M, Duty S (2012). Allosteric modulation of the group III mGlu receptor 4 provides functional neuroprotection in the rodent 6-OHDA model of Parkinsons disease. Br J Pharmacol. Aug;166(8):2317-30. Broadstock M, Austin P, Betts MJ, Duty S (2012). Antiparkinsonian potential of targeting group III metabotropic glutamate receptor subtypes in the rodent substantia nigra pars reticulata. Br J Pharmacol. Feb;165(4b):1034-45. Austin P, *Betts MJ, Broadstock M, ONeill M, Mitchell S, Duty S (2010). Symptomatic and neuroprotective effects following activation of nigral group III metabotropic glutamate receptors in rodent models of Parkinsons disease. Br J Pharmacol. Aug;160(7):1741-5. * Denotes co-first author. Book chapters. Düzel E, Guitart-Masip M, Maaß A, Haemmerer D, Betts M, Speck O, Weiskopf N, Kanowski M ...
The role of phospholipase C-coupled (group I) metabotropic glutamate receptors (mGluR1 and mGluR5) in post-traumatic neuronal injury was examined using rat in vivo and in vitro models. Traumatic injury to mixed neuronal/glial cultures induced phosphoinositide hydrolysis and caused neuronal death. Pharmacological blockade of group I receptors significantly reduced these effects in vitro and decreased neurological deficits as well as neuronal loss produced by traumatic brain injury in vivo. In contrast, activation of group I receptors by a specific agonist in vitro exacerbated post-traumatic neuronal death in a dose-dependent manner. Antisense oligodeoxynucleotide directed to mGluR1, but not to mGluR5, was neuroprotective in vitro, although each oligodeoxynucleotide reduced the respective receptor-stimulated accumulation of inositol phosphates to a similar degree. Together, these findings suggest that activation of mGluR1 contributes to post-traumatic neuronal injury and that mGluR1 antagonists may have
TY - JOUR. T1 - Synthesis of N1-substituted analogues of (2R,4R)-4-amino-pyrrolidine-2,4-dicarboxylic acid as agonists, partial agonists, and antagonists of group II metabotropic glutamate receptors. AU - Mukhopadhyaya, Jayanta Kumar. AU - Kozikowski, Alan P.. AU - Grajkowska, Ewa. AU - Pshenichkin, Sergey. AU - Wroblewski, Jarda T.. PY - 2001/7/23. Y1 - 2001/7/23. N2 - The chemical synthesis of a series of N1-substituted derivatives of (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylic acid [(2R,4R)-APDC] as constrained analogues of γ-substituted glutamic acids is described. Appropriate substitution of the N1-position results in agonist, partial agonist, or antagonist activity at mGluR2, mGluR3, and/or mGluR6.. AB - The chemical synthesis of a series of N1-substituted derivatives of (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylic acid [(2R,4R)-APDC] as constrained analogues of γ-substituted glutamic acids is described. Appropriate substitution of the N1-position results in agonist, partial agonist, or ...
Buy LY 379268 (CAS 191471-52-0), a water soluble systemically active group II mGluR agonist. Join researchers using high quality LY 379268 from Abcam and…
1S50: Crystal structures of the GluR5 and GluR6 ligand binding cores: Molecular mechanisms underlying kainate receptor selectivity
Research proven bioactive human Gas-1 Recombinant Protein mediates the antiapoptotic effect of VEGF. In contrast, Gas1 is induced in hippocampal neurons after NMDA exposure but functions as a proapoptotic effector of NMDA mediated excitotoxicity. Gas1 exhibits a range of developmental actions including either promoting or inhibiting growth and differentiation of somite, limb, cerebellar, and eye tissues
Սինապասային հաղորդման ժամանակ նախասինապսային թաղանթը էկզոցիտոզի միջոցով արտազատում է էնդոկաննաբինոիդներին սինապսային ճեղքի մեջ, որոնք այնուհետև ազդում են հետսինապսային թաղանթի վրա գտնվող ընկալիչների վրա։ Կախված ընկալիչների տեսակից, էնդոկաննաբինոիդների ազդեցությունից կարող է առաջանալ ինչպես դրդում, այնպես էլ արգելակում, կամ էլ երկրորդային միջնորդների ակտիվացում։[9] Օրինակ, պարզվել է, որ պոտենցիալակախյալ L-տիպի կալցիումական անցուղիների ակտիվացումը խթանում է 2-AG-ի արտադրությունը, մինչ mGluR1/5 գլյուտամատային ընկալիչների ակտիվացումը նպաստում է ...
Montville - You wouldnt ordinarily expect Craig Parker to be so effusive with his praise on such an occasion.Parker, the New London High School
L-serine-O-phosphate (L-SOP) is the immediate precursor to L-serine in the serine synthesis pathway and is also an agonist at the Group III metabotropic glutamate receptors (mGluRs). L-SOP is produced by the enzyme phosphoserine aminotransferase (PSAT) and metabolized to L-serine by phosphoserine ph …
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 ...
The metabotropic glutamate receptors (mGluRs) are key receptors in the modulation of excitatory synaptic transmission in the central nervous system. Here we have determined three different crystal structures of the extracellular ligand-binding region of mGluR1--in a complex with glutamate and in two …
TY - JOUR. T1 - Functional partnership between mGlu3 and mGlu5 metabotropic glutamate receptors in the central nervous system. AU - Di Menna, Luisa. AU - Joffe, Max E.. AU - Iacovelli, Luisa. AU - Orlando, Rosamaria. AU - Lindsley, Craig W.. AU - Mairesse, Jèrome. AU - Gressèns, Pierre. AU - Cannella, Milena. AU - Caraci, Filippo. AU - Copani, Agata. AU - Bruno, Valeria. AU - Battaglia, Giuseppe. AU - Conn, P. Jeffrey. AU - Nicoletti, Ferdinando. PY - 2017/10/25. Y1 - 2017/10/25. N2 - mGlu5 receptors are involved in mechanisms of activity-dependent synaptic plasticity, and are targeted by drugs developed for the treatment of CNS disorders. We report that mGlu3 receptors, which are traditionally linked to the control of neurotransmitter release, support mGlu5 receptor signaling in neurons and largely contribute to the robust mGlu5 receptor-mediated polyphosphoinositide hydrolysis in the early postnatal life. In cortical pyramidal neurons, mGlu3 receptor activation potentiated mGlu5 ...
Thank you for your interest in spreading the word about Biochemical Society Transactions.. NOTE: We only request your email address so that the person you are recommending the page to knows that you wanted them to see it, and that it is not junk mail. We do not capture any email address.. ...
TY - JOUR. T1 - Dexamethasone attenuates kainate-induced AP-1 activation in rat brain. AU - Unlap, Tino. AU - Jope, Richard S.. PY - 1994/7. Y1 - 1994/7. N2 - The goal of this investigation was to determine if administration of the synthetic glucocorticoid dexamethasone modulates rat brain AP-1 DNA binding activity. Treatment with the selective excitatory amino acid agonist kainate was used to activate AP-1 formation. Kainate (12 mg/kg) administration induced a biphasic activation of AP-1 in rat cerebral cortex and hippocampus with maximal levels observed at 1.5 h and 4.5 h and lower levels at 3 h and 6 h. Kainate also induced biphasic increases in the concentrations of some of the AP-1 constituent proteins (immediate early gene protein products), with initial increases of c-Jun, Fos, and Jun B occurring at 1.5 h and secondary larger increases at 4.5 h, but the level of Jun D was not altered by kainate treatment. Pretreatment with dexamethasone (1 mg/kg) reduced AP-1 activity at both 1.5 h and ...
Attwell PJ, Singh Kent N, Jane DE, Croucher MJ, Bradford HF (1998). „Anticonvulsant and glutamate release-inhibiting properties of the highly potent metabotropic glutamate receptor agonist (2S,2R, 3R)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV). Brain Research. 805 (1-2): 138-43. PMID 9733953. doi:10.1016/S0006-8993(98)00698-2 ...
1ISS: Structural views of the ligand-binding cores of a metabotropic glutamate receptor complexed with an antagonist and both glutamate and Gd3+.
Buy (S)-3,5-DHPG (CAS 162870-29-3), a water soluble selective group I mGluR agonist cited in 20 publications. Join researchers using high quality (S)-3,5-DHPG…
Several genes encoding proapoptotic proteins also elevated expression right after NMDA injection: Amounts of Stat1 mRNA were significantly improved at 24 h, and caspase one mRNA was threefold and fourfold elevated in contrast to controls at 24 h and 48 h, respectively. In contrast, monocyte chemotactic protein 1 , a cytokine involved with recruiting white blood cells to websites of infection or inflammation , was similarly expressed from the NMDA and PBS handled retinas, despite the fact that a tendency for greater expression was detected in NMDA retinas at 24 h right after injection. Activation of a number of these molecules immediately after NMDA injection was also detecinhibitors on the protein level with western blotting . At 24 h soon after injection, we found strongly elevated levels of phospho STAT3, STAT3, phospho STAT1, and STAT1 from the NMDA taken care of retinas compared on the PBS injected controls. On top of that, expression of glial fibrillary acidic protein along with the proform ...
TY - JOUR. T1 - Homer 1b regulates the trafficking of group I metabotropic glutamate receptors. AU - Roche, Katherine W.. AU - Tu, Jian Cheng. AU - Petralia, Ronald S.. AU - Xiao, Bo. AU - Wenthold, Robert J.. AU - Worley, Paul F. PY - 1999/9/3. Y1 - 1999/9/3. N2 - The molecular basis for glutamate receptor trafficking to the plasma membrane is not understood. In the present study, we demonstrate that Homer 1b (H1b), a constitutively expressed splice form of the immediate early gene product Homer (now termed Homer 1a) regulates the trafficking and surface expression of group I metabotropic glutamate receptors. H1b inhibits surface expression of the metabotropic glutamate receptor mGluR5 in heterologous cells, causing mGluR5 to be retained in the endoplasmic reticulum (ER). In contrast, mGluR5 alone or mGluR5 coexpressed with Homer 1a successfully travels through the secretory pathway to the plasma membrane. In addition, point mutations that disrupt mGluR5 binding to H1b eliminate ER retention of ...
Group II metabotropic glutamate receptors (mGluR2 and mGluR3, encoded by GRM2 and GRM3) are implicated in hippocampal function and cognition, and in the pathophysiology and treatment of schizophrenia and other psychiatric disorders. However, pharmacological and behavioral studies with group II mGluR agonists and antagonists have produced complex results. Here, we studied hippocampus-dependent memory in GRM2/3 double knockout (GRM2/3-/-) mice in an iterative sequence of experiments. We found that they were impaired on appetitively motivated spatial reference and working memory tasks, and on a spatial novelty preference task that relies on animals exploratory drive, but were unimpaired on aversively motivated spatial memory paradigms. GRM2/3-/-mice also performed normally on an appetitively motivated, non-spatial, visual discrimination task. These results likely reflect an interaction between GRM2/3 genotype and the arousal-inducing properties of the experimental paradigm. The deficit seen on appetitive
Materials. All tissue culture reagents were obtained from Invitrogen (Carlsbad, CA). G418 sulfate was obtained from Mediatech, Inc., (Herndon, VA). [3H]LY341495 (28.28 Ci/mmol) was obtained from American Radiolabeled Chemicals, Inc. (St Louis, MO). l-Glutamate, DCG-IV, l-AP4 [l-(+)-2-amino-4-phosphonobutyric acid], and LY341495 were obtained from Tocris (Ellisville, MO). Methotrexate was purchased from Calbiochem (La Jolla, CA). BINA was synthesized as described previously (Galici et al., 2006). The Calcium 3 Assay Kit was obtained from Molecular Devices (Sunnyvale, CA). The indicator dye fluo-4 was obtained from Invitrogen. Probenecid, dimethyl sulfoxide (DMSO), puromycin dihydrochloride, GDP, and guanosine 5′-3-O-(thio)triphosphate were purchased from Sigma-Aldrich, Inc., (St. Louis, MO). Unifilter-96 GF/B plates and MicroScint-20 were obtained from PerkinElmer Life and Analytical Sciences (Boston, MA). BioCoat poly-d-lysine 96-well culture plates were obtained from BD Biosciences Discovery ...
We use cookies to ensure that we give you the best experience on our website. If you click Continue well assume that you are happy to receive all cookies and you wont see this message again. Click Find out more for information on how to change your cookie settings ...
A family of metabotropic glutamate receptors (mGluRs) has been elucidated by molecular cloning. To study the possible modulatory role of mGluRs in synaptic transmission, we tested the effect of a mGluR agonist, (±)-l-aminocyclopentane-trans-l,3-dicarboxylic acid (trans-ACPD), on the excitatory post-synaptic currents (EPSCS) recorded from neurons in thin slices of rat visual cortex, by using the whole-cell patch-clamp method. We found that trans-ACPD) markedly suppressed the evoked EPSCS without affecting the mean amplitude of spontaneous miniature EPSCS. This effect on the evoked EPSCS was blocked by a potassium channel blocker, 4-aminopyridine (4-AP) in a dose-dependent manner We suggest that trans-ACPD presynaptically inhibits EPSCS by a mechanism involving the 4-AP-sensitive channels. ...
Title: Targeting the Metabotropic Glutamate Receptor mGluR4 for the Treatment of Diseases of the Central Nervous System. VOLUME: 5 ISSUE: 9. Author(s):Michael J. Marino, J. F. Hess and Nigel Liverton. Affiliation:Neuroscience Drug Discovery - Movement Disorders Research, Merck Research Laboratories, Merck&Co., PO Box 4, West Point, PA 19486, USA.. Keywords:mglur, glutamate, parkinsons disease. Abstract: Over the last several years a great deal of interest has been focused on the metabotropic glutamate receptors as potential targets for the treatment of a variety of disorders of the central nervous system. Recently, selective agonist or allosteric potentiators of mGluR4, one of the group III mGluRs, have been proposed as potential novel therapeutics for the palliative treatment of Parkinsons disease and some forms of epilepsy. mGluR4 stands out amongst the group III mGluRs due to its relatively restricted localization and apparent role in several key neuronal circuits. Work from a number of ...
Metabotropic glutamate receptors (mGluRs) are G protein-coupled receptors (GPCRs) that contribute to the regulation of integrative brain functions such as cognition, motor control, and neural development. Metabotropic glutamate receptors are members of a unique class of GPCRs (class III) that include the calcium sensing and γ-aminobutyric acid type B receptors. Although mGluRs bear little sequence homology to well-characterized members of the GPCR superfamily, both second messenger-dependent protein kinases and G protein-coupled receptor kinases (GRKs) contribute to mGluR desensitization. Therefore, in the present study, we examined whether β-arrestins, regulators of GPCR desensitization and endocytosis, are required for mGluR1a desensitization and internalization in human embryonic kidney (HEK) 293 cells. Unlike what has been reported for other GPCRs, we find that in response to agonist stimulation, mGluR1a internalization is selectively mediated by β-arrestin1 in HEK 293 cells. However, ...
Metabotropic glutamate receptors (mGluRs) are coupled to effector systems through GTP-binding proteins (G-proteins) and appear to mediate slow synaptic responses in the CNS. Although mGluR-mediated increases in phosphoinositide hydrolysis have been well characterized, other mechanisms for signal transduction employed by mGluRs are poorly understood. We recently reported that the selective mGluR agonist 1- aminocyclopentane-1 S,3R-dicarboxylic acid (1S,3R-ACPD) increases cAMP accumulation in rat hippocampal slices. We have now investigated the mechanisms involved in this response. A number of G-protein-linked receptors that are not directly coupled to adenylate cyclase increase cAMP accumulation by potentiating cAMP responses to other agonists. Furthermore, previous studies suggest that glutamate increases cAMP accumulation by a mechanism that is dependent upon the presence of endogenous adenosine. Therefore, we tested the hypothesis that 1S,3R- ACPD-stimulated increases in cAMP accumulation in ...
Immunoreactivity for the group I mGluRs was observed in neuropil of the dendritic fields of the hippocampal principal cells as described previously (Luján et al., 1996), whereas immunoreactivity for the group II and group III mGluRs was observed more or less in a laminated fashion corresponding to the terminal zones of the major hippocampal pathways (Fig. 2). All hippocampal fields were immunopositive for mGluR5 and mGluR7a, whereas immunoreactivity for the other mGluRs was restricted to some areas or layers in the hippocampus. Immunoreactivity for mGluR6 was hardly detected in the hippocampus (Fig.2 G).. For the group I mGluRs, we used the antibodies reactive to all splice variants of mGluR1 (pan mGluR1) and mGluR5, as well as the mGluR1α-specific antibody. In CA1 dendritic fields, only the mGluR5 antibody showed intense immunolabeling of neuropil, whereas the pan mGluR1 and mGluR5 antibodies revealed similar patterns of immunolabeling in CA3 dendritic fields and dentate molecular layer ...
Close The Infona portal uses cookies, i.e. strings of text saved by a browser on the users device. The portal can access those files and use them to remember the users data, such as their chosen settings (screen view, interface language, etc.), or their login data. By using the Infona portal the user accepts automatic saving and using this information for portal operation purposes. More information on the subject can be found in the Privacy Policy and Terms of Service. By closing this window the user confirms that they have read the information on cookie usage, and they accept the privacy policy and the way cookies are used by the portal. You can change the cookie settings in your browser. ...
Metabotropic glutamate receptors (mGluRs) play key roles in the modulation of many synapses. Chloride (Cl(-)) is known to directly bind and regulate the function of different actors of neuronal activity, and several studies have pointed to the possible modulation of mGluRs by Cl(-). Herein, we demonstrate that Cl(-) behaves as a positive allosteric modulator of mGluRs. For example, whereas glutamate potency was 3.08 ± 0.33 μM on metabotropic glutamate (mGlu) 4 receptors in high-Cl(-) buffer, signaling activity was almost abolished in low Cl(-) in cell-based assays. Cl(-) potency was 78.6 ± 3.5 mM. Cl(-) possesses a high positive cooperativity with glutamate (Hill slope ≈6 on mGlu4), meaning that small variations in [Cl(-)] lead to large variations in glutamate action. Using molecular modeling and mutagenesis, we have identified 2 well-conserved Cl(-) binding pockets in the extracellular domain of mGluRs. Moreover, modeling of activity-dependent Cl(-) variations at GABAergic synapses ...
Anti Metabotropic Glutamate Receptor 2/3 (mGluR2/3) Antibody , Rabbit Anti-Rat Polyclonal Antibody validated in WB, IHC-P, IHC-F (ABD13051), Abgent
BioAssay record AID 252326 submitted by ChEMBL: Percentage of maximal glutamate (1 mM) response of human metabotropic glutamate receptor 2 done at 30 degree C for 1 hr.
Transgenic Huntingtons disease (HD) mice, expressing exon 1 of the human HD gene (lines R6/1 and R6/2), are totally resistant to striatal lesions caused by the NMDA receptor agonist quinolinic acid (QA). Here we show that this resistance develops gradually over time in both R6/1 and R6/2 mice, and that it occurred earlier in R6/2 (CAG-155) than in R6/1 (CAG-115) mice. The development of the resistance coincided with the appearance of nuclear inclusions and with the onset of motor deficits. In the HD mice, hippocampal neurons were also resistant to QA, especially in the CA1 region. Importantly, there was no change in susceptibility to QA in transgenic mice with a normal CAG repeat (CAG-18). R6/1 mice were also resistant to NMDA-, but not to AMPA-induced striatal damage. Interestingly, QA-induced current and calcium influx in striatal R6/2 neurons were not decreased. However, R6/2 neurons had a better capacity to handle cytoplasmic calcium ([Ca2+](c)) overload following OA and could avoid ...
The IUPHAR/BPS Guide to Pharmacology. mGlu5 receptor - Metabotropic glutamate receptors. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
The IUPHAR/BPS Guide to Pharmacology. mGlu4 receptor - Metabotropic glutamate receptors. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
The Report Metabotropic Glutamate Receptor 5 (GPRC1E or MGLUR5 or GRM5) - Pipeline Review, H2 2017 provides information on pricing, market analysis,...
BioAssay record AID 107086 submitted by ChEMBL: Compound was tested for its antagonist activity against Ser152 and Thr175 (Metabotropic glutamate receptor 5).
Gentaur molecular products has all kinds of products like :search , Allele \ Metabotropic Glutamate Receptor 2_3 Polyclonal Antibody \ ABP-PAB-22025 for more molecular products just contact us
Lately there has been alot of hype around ketamine for the treatement of depression. There has also been some talks regarding NMDA receptor agonists...
Buy (S)-ATPA - an affordable, high quality AMPA receptor Agonist from Hello Bio, a trusted supplier for life science researchers worldwide
N-Metil-D-aspartinska kiselina (N-metil-D-aspartat, NMDA) je aminokiselinski derivat koji deluje kao specifični agonist NMDA receptora. NMDA oponaša dejstvo glutamata, neurotransmitera koji je endogeni ligand tog receptora. Za razliju od glutamata, NMDA se jedino vezuje za i reguliše NMDA receptore, i nema efekta na druge tipove glutamatnih receptora (kao što su AMPA i kainatni). NMDA receptori su posebno važni kad postanu prekomerno aktivni tokom povlačenja alkohola, a to uzrokuje simptome poput agitacije, i u nekim slučajevima epileptičke napade. ...
Fan, Wei. Conditions for activation of group I metabotropic glutamate receptors in rat hippocampus. 2010, University of Zurich, Faculty of Science. ...
PubMed Central Canada (PMC Canada) provides free access to a stable and permanent online digital archive of full-text, peer-reviewed health and life sciences research publications. It builds on PubMed Central (PMC), the U.S. National Institutes of Health (NIH) free digital archive of biomedical and life sciences journal literature and is a member of the broader PMC International (PMCI) network of e-repositories.
TY - JOUR. T1 - Nerve Growth Factor Content of Rat Brain Increases Following Basal-Forebrain Lesions Induced by Ibotenic Acid but Not by Electrolysis. AU - Furukawa, Yoshiko. AU - Hayashi, Kyozo. AU - Nabeshima, Toshitaka. PY - 1994. Y1 - 1994. N2 - We attempted to measure the change in the nerve growth factor (NGF) content in the hippocampus and parietal cortex following basal-forebrain lesions induced by ibotenic acid and electrolysis. The NGF content of the parietal cortex and hippocampus increased transiently on days 3 to 7, and then returned to the control level on day 14 after the lesion of the basal forebrain induced by ibotenic acid. Ibotenic acid decreased both the choline acetyltransferase (ChAT) activity in the parietal cortex and the dopamine content in the striatum. Electrolytic lesions of the basal forebrain decreased the dopamine content in the striatum, but did not affect the NGF content and ChAT activity in any of the brain regions examined. These results suggest that the ...
Krystal JH, Abi-Saab W, Perry E, DSouza DC, Liu N, Gueorguieva R et al. (2005). Preliminary evidence of attenuation of the disruptive effects of the NMDA glutamate receptor antagonist, ketamine, on working memory by pretreatment with the group II metabotropic glutamate receptor agonist, LY354740, in healthy human subjects. Psychopharmacology (Berl) 179: 303-309 ...
Carroll, F. (2008). Antagonists at Metabotropic Glutamate Receptor Subtype 5 Structure Activity Relationships and Therapeutic Potential for Addiction: Addiction Reviews 2008. Annals of the New York Academy of Sciences, 1141, 221-232 ...
Microglia are the immune cell of the central nervous system and become reactive in response to infection or trauma. In Multiple Sclerosis (MS) microglia show early reactivity which may contribute to subsequent neurotoxicity. Glutamate has been implicated in the neurodegeneration in MS. Microglia express subtypes of metabotropic glutamate receptors (mGluRs), the activation of which can lead to microglial evoked neurotoxicity (group II) or neuroprotection (group III). This suggests that release of glutamate from neurones or glial cells may activate microglia via these receptors. Increased microglial reactivity during disease is possibly due to an imbalance of mGluR expression with neurotoxic group II increased above neuroprotective group III mGluRs. Microglial expression of mGluR subtypes was therefore investigated on activated compared with untreated cells. It was found that microglia exposed to myelin expressed increased levels of group II and mGluRl and 8 subtypes compared with control cells. ...
The design, synthesis and evaluation of eight contrast agents for metabotropic glutamate receptors is reported. Each of the contrast agents contains a selective mGluR5 binding moiety linked to a DOTA-derived gadolinium complex. The potential of these systems was evaluated in vitro for application as respon
Glutamate ((S)-Glu) is the major excitatory amino acid in the central nervous system. It acts by stimulating ionotropic and metabotropic glutamate receptors (iGluR and mGluR respectively). Glutamate has been shown to be involved not only in many neuropathologies such as anxiety, pain, ischemia, Parkinsons disease, epilepsy and schizophrenia. More recently, mGlu receptors have also been detected in non-neuronal cells suggesting that they could be implicated in carcinogenesis.. mGlu receptors are G-protein-coupled receptors and eight subtypes (mGluR1 to mGluR8) have been identified and classified into three groups (I-III) based upon sequence homology, transduction mechanism and pharmacological profile.. Because of their modulating properties, mGlu receptors are recognized as promising therapeutic targets and many ligands (agonists and antagonists) have been prepared to better understand the pharmacology of mGlu receptors in order to selectively activate the different groups and subtypes of ...
Metabotropic glutamate receptors are G-protein coupled receptors that respond to glutamate by activating proteins inside nerve cells that affect cell metabolism, thereby fine-tuning the signals sent between cells to maintain balance in neuronal activity. Metabotropic Glutamate receptors (mGluR5) are Group I receptors localized post-synaptically and found in several regions of the brain including the striatum, hippocampus, amygdala, and cortex. Activation of mGluR5 stimulates phospholipase C, resulting in phosphoinositide hydrolysis and increase of intracellular Ca2+ levels. Several potent antagonists for mGluR5 have been developed, including 6 methyl-2-(phenylethynyl)pyridine (MPEP) and 3-[(2-methyl-1,3-thiazol-4yl)ethynyl] pyridine (MTEP) however, no simple derivatives of MPEP or MTEP had proven to be useful for in vivo imaging.. In the present protocol, we will use a new PET ligand [(18)F]SP203 for two reasons: Part 1.) we will perform kinetic brain imaging to quantify mGluR5 binding ...
Matosin N and Newell KA. Metabotropic Glutamate Receptor 5 in the Pathology and Treatment of Schizophrenia.Neuroscience & Biobehavioural Reviews. 2013. 37 (3): 256-268. Abstract Metabotropic glutamate receptor 5 (mGluR5) potentiates the NMDA receptor (NMDAR) in brain regions implicated in schizophrenia, making it a viable therapeutic target for the treatment of this disorder. mGluR5 positive allosteric modulators may…
NMDA receptors are glutamate- and glycine-gated channels that mediate fast excitatory transmission in the central nervous system and are critical to synaptic development, plasticity and integration. They have a rich complement of modulatory sites, which represent important pharmacologic targets. Ifenprodil is a well-tolerated NMDA receptor inhibitor; it is selective for GluN2B-containing receptors; and has neuroprotective effects. The mechanism by which ifenprodil inhibits NMDA receptor responses is not fully understood. The inhibition is incomplete and non-competitive with other known NMDA receptor agonists or modulators, although reciprocal effects have been reported between ifenprodil potency and that of extracellular ligands including glutamate, glycine, zinc, protons and polyamines. Recently, structural studies revealed that ifenprodil binds to a unique site at the interface between the extracellular N-termini of GluN1 and GluN2B subunits supporting the view that interactions with other ...
ウサギ・ポリクローナル抗体 ab53090 交差種: Ms,Rat,Chk,Hu 適用: WB,ELISA,IHC-P,IHC-Fr,ICC/IF…Metabotropic Glutamate Receptor…
Metabotropic Glutamate Receptor 3兔多克隆抗体(ab10309)可与大鼠样本反应并经WB实验严格验证,被1篇文献引用。所有产品均提供质保服务,中国75%以上现货。
Metabotropic Glutamate Receptor 6兔多克隆抗体(ab83576)可与人样本反应并经WB, ELISA实验严格验证。所有产品均提供质保服务,中国75%以上现货。
Excitotoxicity is one of the most extensively studied processes of neuronal death and plays an important role in Alzheimers disease. In the present study, the protective effects of Gossypium herbaceam extracts (GHE) on learning and memory impairment
In multiple sclerosis, blocking the source - rather than the target - of excitotoxic glutamate is a more feasible therapeutic strategy for CNS protection. Neuroscientist Tara DeSilva, PhD, explains why, along with the research implications.
(RS)-3,5-DHPG | mGluR1 agonist | CAS [146255-66-5] | Axon 1739 | Axon Ligand™ with >99% purity available from supplier Axon Medchem, prime source of life science reagents for your research
Examples include excitatory amino acid receptor agonists, excitatory amino acid receptor antagonists, and excitatory amino acid ... is a chemical that directly modulates the excitatory amino acid (glutamate/aspartate) system in the body or brain. ...
Malenka RC, Nestler EJ, Hyman SE (2009). "Chapter 5: Excitatory and Inhibitory Amino Acids". In Sydor A, Brown RY (eds.). ... lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor ... phenethylamine is produced directly from L-phenylalanine by the aromatic amino acid decarboxylase (AADC) enzyme, which converts ... benzoic acid, hippuric acid, norephedrine, and phenylacetone. Among these metabolites, the active sympathomimetics are 4- ...
SLC1A1 is excitatory amino acid transporter 3 (EAAT3), a glutamate transporter located in neurons, SLC22A3 is an extraneuronal ... Amphetamine has been identified as a potent full agonist of trace amine-associated receptor 1 (TAAR1), a Gs-coupled and Gq- ... Malenka RC, Nestler EJ, Hyman SE (2009). "Chapter 5: Excitatory and Inhibitory Amino Acids". In Sydor A, Brown RY (eds.). ... and the biosynthetic enzyme aromatic amino acid decarboxylase (AADC). ... AMPH release of DA from synapses requires both an ...
Malenka RC, Nestler EJ, Hyman SE (2009). "Chapter 5: Excitatory and Inhibitory Amino Acids". In Sydor A, Brown RY (eds.). ... NMDA receptors are voltage-dependent ligand-gated ion channels that requires simultaneous binding of glutamate and a co-agonist ... and the biosynthetic enzyme aromatic amino acid decarboxylase (AADC). Broadley KJ (March 2010). "The vascular effects of trace ... phenethylamine is produced directly from L-phenylalanine by the aromatic amino acid decarboxylase (AADC) enzyme, which converts ...
... monoaminergic and dopamine agonists, progesterone, aminosteroids, excitatory amino acid reuptake inhibitors, beta-2 antagonists ... Willis, C.; Lybrand, S.; Bellamy, N. (2004). "Excitatory amino acid inhibitors for traumatic brain injury". The Cochrane ... Bailes JE, Mills JD, Hadley K (January 2011). "Dietary Supplementation with the Omega-3 Fatty Acid Docosahexaenoic Acid in ... "Changes in cortical extracellular levels of energy-related metabolites and amino acids following concussive brain injury in ...
... is an excitatory amino acid analogue of glutamate; a neurotransmitter in the brain that activates glutamate ... In addition there is a synergistic effect with endogenous glutamate and N-Methyl-D-aspartate receptor agonists that contribute ... Domoic acid is a structural analog of kainic acid, proline, and endogenous excitatory neurotransmitter glutamate.[8] Ohfune and ... "Domoic Acid Toxicity". The Marine Mammal Center. Retrieved 2 April 2015.. *^ "Domoic Acid Poisoning". Northwest Fisheries ...
Cudkowicz has also led clinical trials for the use of ceftriaxone, an excitatory amino acid transporter, to minimize glutamate ... a potassium channel agonist, in phase II clinical trials. In 2019, Cudkowicz started to test the efficacy of autologous bone ...
... α-Decarboxylation of excitatory amino acids can produce derivatives with inhibitory effects. Indeed, unlike quisqualic acid, ... properties and appears to act predominantly as an agonist of the GABAA receptor and also to a lesser extent as an agonist of ... a novel gamma-aminobutyric acid (GABA) related depressant amino acid". The Journal of Pharmacy and Pharmacology. 30 (6): 364-7 ... Quisqualic acid Muscimol Evans RH, Francis AA, Hunt K, Martin MR, Watkins JC (June 1978). "Quisqualamine, ...
... and is responsible for the majority of fast excitatory amino acid neurotransmission in the central nervous system (CNS). ... Moreover, whereas AMPAR agonists activate all AMPARs, AMPAR PAMs can show selectivity for specific subpopulations of AMPARs. ... Similarly to AMPAR agonists, high-impact AMPAR PAMs can cause convulsions and neurotoxicity in sufficiently high doses. ... However, low doses of AMPAR activators may nonetheless be useful, and AMPAR PAMs, which, unlike agonists, show selectivity for ...
... see also Excitatory amino acid receptor agonist, Excitatory amino acid receptor antagonist, Ionotropic glutamate receptor, ... Ampakine, NMDA receptor antagonist Nicotinic receptor: see also Nicotinic agonist, Ganglionic blocker and Neuromuscular- ... see also GABA receptor agonist, GABA receptor antagonist Glutamate receptor: ...
This may be achieved by regulating the excitatory amino acid systems that are responsible for changes in the strength of ... Atypical μ-opioid receptor agonist[edit]. In 2014, tianeptine was found to be a μ-opioid receptor (MOR) full agonist using ... 7-[(3-Chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid ... This seems to be because of the unique C3 amino heptanoic acid side chain of tianeptine, which, in contrast to other TCAs, is ...
... agonists AMPA Domoic acid Kainic acid NMDA Quinolinic acid Quisqualic acid Tetrazolylglycine Acetylcholine receptor agonists ... "Excitatory aminoacids and epileptic seizures in immature brain". Physiological Research. 53 Suppl 1: S115-24. PMID 15119942. ... Most convulsants are antagonists (or inverse agonists) at either the GABAA or glycine receptors, or ionotropic glutamate ... GABAA receptor antagonists, inverse agonists or negative allosteric modulators Bemegride Bicuculline Cicutoxin Cyclothiazide ...
... are stimulated most strongly by the excitatory amino acid analog L-quisqualic acid. Stimulating the receptors causes the ... has been found to cause more damage to neurons in the presence of group I mGluR agonists. On the other hand, agonists of group ... Like all glutamate receptors, mGluRs bind with glutamate, an amino acid that functions as an excitatory neurotransmitter. The ... "Presynaptic inhibitory action of metabotropic glutamate receptor agonist on excitatory transmission in visual cortical neurons ...
Glutamate is one of two primary excitatory amino acid neurotransmitters, along with aspartate. Glutamate receptors are one of ... The function of NMDA receptors depend on glycine receptor binding as a co-agonist within the channel pore. NMDA receptors do ... Dopamine is synthesized from the amino acid tyrosine. Tyrosine is catalyzed into levadopa (or L-DOPA) by tyrosine hydroxlase, ... Glutamate is synthesized from the amino acid glutamine by the enzyme glutamate synthase. Dopaminergic neurons-dopamine. ...
Excitatory Amino Acids include Glutamate, whereas inhibitory Amino Acids include GABA and Glycine. Additionally, catecholamines ... Inverse agonists bind to receptors and elicit the opposite effect that an agonist would. The spectrum of drug continuum also ... Agonists bind to receptors and elicit the same effects as an endogenous neurotransmitter. For example, morphine is an agonist ... Because drugs range widely in their potency and efficacy, drugs have been categorized on the spectrum of agonists and ...
Zhang W, Han XY, Wong SM, Takeuchi H (January 1997). "Pharmacologic characteristics of excitatory gamma-amino-butyric acid ( ... Murphy VF, Wann KT (November 1988). "The action of GABA receptor agonists and antagonists on muscle membrane conductance in ... Takeuchi H (September 1992). "Sensitivities of Achatina giant neurones to putative amino acid neurotransmitters". Comparative ...
Malenka RC, Nestler EJ, Hyman SE (2009). "Chapter 5: Excitatory and Inhibitory Amino Acids". In Sydor A, Brown RY (eds.). ... Methamphetamine is also an agonist of the alpha-2 adrenergic receptors and sigma receptors with a greater affinity for σ1 than ... benzoic acid, hippuric acid, norephedrine, and phenylacetone, the metabolites of amphetamine.[2][112][113] Among these ... σ Receptor agonists have been shown to facilitate dopamine release, through both σ-1 and σ-2 receptors [11-14].. ...
They include excitatory amino acid receptor agonists and excitatory amino acid receptor antagonists. Christensen, Inge T.; ... Excitatory amino acid receptor ligands are ligands of excitatory amino acid receptors (EAARs), also known as glutamate ... "Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to ... homoibotenic acid". Journal of Medicinal Chemistry. 35 (19): 3512-3519. doi:10.1021/jm00097a008. v t e v t e. ...
Glutamatergic GABA reuptake inhibitor Glycine reuptake inhibitor Excitatory amino acid receptor agonist Excitatory amino acid ... An excitatory amino acid reuptake inhibitor (EAARI) is a type of drug which inhibits the reuptake of the excitatory ... Media related to Excitatory amino acid reuptake inhibitors at Wikimedia Commons Glutamate (EAAT) Transporters - Tocris ... neurotransmitters glutamate and aspartate by blocking one or more of the excitatory amino acid transporters (EAATs). Examples ...
Kynurenic acid Memantine Nitrous oxide Perampanel Phencyclidine Excitatory amino acid receptor agonist Excitatory amino acid ... An excitatory amino acid receptor antagonist, or glutamate receptor antagonist, is a chemical substance which antagonizes one ... reuptake inhibitor N-methyl-D-aspartate receptor antagonist MeSH list of agents 82018691 Excitatory+amino+acid+antagonists at ...
Bellesi M, Conti F (2010). "The mGluR2/3 agonist LY379268 blocks the effects of GLT-1 upregulation on prepulse inhibition of ... Excitatory amino acid transporter 2 (EAAT2) also known as solute carrier family 1 member 2 (SLC1A2) and glutamate transporter 1 ... The glutamate transporter 1 (GLT1)/ excitatory amino acid transporter 2 (EAAT2) is responsible for the reuptake of more than 90 ... "DL-threo-b-Benzyloxyaspartate, A Potent Blocker of Excitatory Amino Acid Transporters" (PDF). Molecular Pharmacology.CS1 maint ...
... acid Kainic acid N-Methyl-D-aspartic acid Quisqualic acid Excitatory amino acid receptor antagonist Excitatory amino acid ... An excitatory amino acid receptor agonist, or glutamate receptor agonist, is a chemical substance which agonizes one or more of ... reuptake inhibitor Excitatory+amino+acid+agonists at the US National Library of Medicine Medical Subject Headings (MeSH) MeSH ...
Malenka RC, Nestler EJ, Hyman SE (2009). "Chapter 5: Excitatory and Inhibitory Amino Acids". In Sydor A, Brown RY (eds.). ... Ligands: Agonists: Glutamate, AMPA, 5-Fluorowillardiine, Domoic acid, Quisqualic acid, etc. Antagonists: CNQX, Kynurenic acid, ... Primary endogenous co-agonists: glutamate and either D-serine or glycine Other agonists : aminocyclopropanecarboxylic acid; D- ... The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, or quisqualate receptor) is a ...
Shirasaki, Y; Sugimura, M; Sato, T (September 2010). "Bromocriptine, an ergot alkaloid, inhibits excitatory amino acid release ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) ... Agonists: Ergolines (e.g., 2-Br-LSD (BOL-148), ergotamine, LSD) ... Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, ...
... excitatory amino acid agents MeSH D27.505.519.625.190.200 - excitatory amino acid agonists MeSH D27.505.519.625.190.300 - ... excitatory amino acid agents MeSH D27.505.696.577.190.200 - excitatory amino acid agonists MeSH D27.505.696.577.190.300 - ... excitatory amino acid antagonists MeSH D27.505.519.625.240 - gaba agents MeSH D27.505.519.625.240.200 - gaba agonists MeSH ... excitatory amino acid antagonists MeSH D27.505.696.577.240 - gaba agents MeSH D27.505.696.577.240.200 - gaba agonists MeSH ...
... is an acid that naturally occurs in some seaweed. Kainic acid is a potent neuroexcitatory amino acid agonist that acts by ... ISBN 978-0-205-23939-9. Moloney, Mark G. (1998). "Excitatory amino acids". Natural Product Reports. 15 (2): 205-219. doi: ... Kainic acid is an agonist for kainate receptors, a type of ionotropic glutamate receptor. Kainate receptors likely control a ... Kainic acid is a direct agonist of the glutamic kainate receptors and large doses of concentrated solutions produce immediate ...
Excitatory amino acid receptor agonists. *Glycine receptor agonists. *Peripherally selective drugs. *Chelating agents ... R1-amino acid + R2-α-ketoacid ⇌ R1-α-ketoacid + R2-amino acid. A very common α-keto acid is α-ketoglutarate, an intermediate in ... A key process in amino acid degradation is transamination, in which the amino group of an amino acid is transferred to an α- ... Glutamic acid (symbol Glu or E)[4] is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins ...
The amino acid L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic ... Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities. ... CHPG (2-amino-2-(2-chloro-5-hydroxyphenyl)acetic acid) Monellin Glutamate Lithium LY-344,545 Mavoglurant Remeglurant SIB-1893 ( ... Receptor density versus agonist concentration". The Journal of Biological Chemistry. 277 (39): 35947-60. doi:10.1074/jbc. ...
Its chemical structure is similar to the amino acid phenylalanine. Caramboxin is an agonist of both NMDA and AMPA glutamatergic ... ionotropic receptors with potent excitatory, convulsant, and neurodegenerative properties. Due to a possible interaction ... Caramboxin is a non-proteinogenic amino acid that stimulates the glutamate receptors in neurons. ... between caramboxin and oxalic acid in starfruit leading to both neurotoxic and nephrotoxic effects, eating starfruit or ...
... amino acids, and chemical signals, such as adenosine, GABA, and glycine. The pre-Bötzinger complex produces two types of ... Several synthetic compounds have been shown to act on neurons specific to the preBötC, most being selective agonists or ... This is due to the reduction of excitatory synaptic transmission in a nucleus and increased excitability in motor neurons ... However, the generation of respiratory rhythm requires other excitatory components, such as glutamate, in order to produce a ...
Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-Aminobutyric acid (GABA) ... S(-) form of barbiturate have shown more depressant activity while the R(+) isomers have an excitatory effect.[28] ... pyrimidinone and 3-amino-1,2,4-triazole derivatives". Bioorganic & Medicinal Chemistry. 23 (3): 480-7. doi:10.1016/j.bmc. ... Valerian constituents (e.g., isovaleric acid, isovaleramide, valerenic acid, valerenol). *Unsorted benzodiazepine site positive ...
Excitatory amino acid agonist) (AMPA(英語:Ampakine)). *Glutamate receptor antagonist(英語:Excitatory amino acid antagonist) (NMDA(英 ... Acetylcholine receptor agonist(英語:Parasympathomimetic_drug) (Muscarinic(英語:Muscarinic agonist) ... 腎上腺素受體激動藥 (α(英語:Alpha-adrenergic agonist) ... 多巴胺受體激動劑(英語:Dopamine agonist) ... Glutamate reuptake inhibitor(英語
... results in an amino acid switch: valine to methionine exchange at codon 66, Val66Met, which is in the prodomain of BDNF.[39][38 ... Tropomyosin receptor kinase B § Agonists. References[edit]. *^ a b c GRCh38: Ensembl release 89: ENSG00000176697 - Ensembl, May ... Levels of both BDNF mRNA and BDNF protein are known to be up-regulated in epilepsy.[86] BDNF modulates excitatory and ... as the amino acid change occurs on the portion of the prodomain where sortilin binds; and sortilin is essential for normal ...
In ALS, there are decreased levels of excitatory amino acid transporter 2 (EAAT2), which is the main transporter that removes ... Bartus RT, Bétourné A, Basile A, Peterson BL, Glass J, Boulis NM (January 2016). "β2-Adrenoceptor agonists as novel, safe and ... "G93A" means that the 93rd amino acid residue in the SOD1 protein has been changed from glycine to alanine. ... It may work by decreasing release of the excitatory neurotransmitter glutamate from pre-synaptic neurons.[10] The most common ...
Amino acid-derived. Major excitatory/inhibitory systems. Glutamate system. *Agmatine. *Aspartic acid (aspartate) ... Agonists (abridged; see here for more): 2-AG. *2-AGE (noladin ether) ...
At high concentrations, it had no effect on spontaneous or potassium evoked amino acid release.[45] ... two of the dominant excitatory neurotransmitters in the CNS.[61] It is generally accepted to be a member of the sodium channel ... Early studies of lamotrigine's mechanism of action examined its effects on the release of endogenous amino acids from rat ... Lamotrigine is inactivated by glucuronidation in the liver.[72] Lamotrigine is metabolized predominantly by glucuronic acid ...
Taurine is a non-protein sulfur amino acid that is found in high concentrations in human milk. It has been shown to have ... GABAB agonist: baclofen[edit]. Baclofen (β-p-chlorophenyl-GABA) has some analgesic properties and has been traditionally used ... simultaneously releasing excitatory neurotransmitters onto motor neurons. Because the number and function of GABAB receptors ... The GABAB antagonist CGP-35348 (3-amino-propyl-(diethoxymethyl) phosphinic acid) has been used in Aldh5a1-/- mice with strong ...
NMDA receptor agonists. *Excitatory amino acid reuptake inhibitors. Hidden categories: *Articles with incomplete citations from ... derived from the related proteinogenic L-amino acid glutamic acid. Theanine is an analog of this amino acid, and its primary ... is an amino acid analogue of the proteinogenic amino acids L-glutamate and L-glutamine and is found primarily in particular ... Not to be confused with threonine, a distinct amino acid, or theine, an archaic synonym of caffeine. ...
... another GABAB receptor agonist, γ-hydroxybutyric acid (GHB), has been associated with euphoria, abuse, and addiction.[13] These ... inhibiting the release of excitatory neurotransmitters. However, baclofen does not have significant affinity for the GHB ... RS)-4-Amino-3-(4-chlorophenyl)butanoic acid. CAS Number. *1134-47-0 Y ... Chemically, baclofen is a derivative of the neurotransmitter γ-aminobutyric acid (GABA). It is believed to work by activating ( ...
Amino acid-derived. Major excitatory/inhibitory systems. Glutamate system. *Agmatine. *Aspartic acid (aspartate) ... Glycine receptor agonists. *Nervous system drug stubs. Hidden categories: *ECHA InfoCard ID from Wikidata ... In the cysteine sulfinic acid pathway, cysteine is first oxidized to its sulfinic acid, catalyzed by the enzyme cysteine ... Kalir, Asher; Kalir, Henry H. "Biological activity of sulfinic acid derivatives" in Chemistry of Sulphinic Acids, Esters Their ...
... increases biogenic amine and excitatory neurotransmitter activity in the brain, with its most pronounced effects targeting the ... "Miscellaneous Sympathomimetic Agonists". In Brunton LL, Chabner BA, Knollmann BC (eds.). Goodman & Gilman's Pharmacological ... 2-Amino-1,2-dihydronaphthalene. *2-Aminoindane. *5-(2-Aminopropyl)indole. *2-Aminotetralin ...
Homocysteic acid - endogenous glutamate site agonist. *Ibotenic acid - naturally occurring glutamate site agonist found in ... This has revealed a common fold with amino acid-binding bacterial proteins and with the glutamate-binding module of AMPA- ... The excitatory postsynaptic potential (EPSP) produced by activation of an NMDA receptor increases the concentration of Ca2+ in ... Homoquinolinic acid - synthetic glutamate site partial agonist. *N-Methyl-D-aspartic acid (NMDA) - synthetic glutamate site ...
Ibotenic acid - a naturally occurring agonist found in Amanita muscaria. *Quisqualic acid - a naturally occurring agonist found ... The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor ... This direct inhibition of excitatory neurotransmission by decanoic acid in the brain contributes to the anticonvulsant effect ... Domoic acid - a naturally occurring agonist that causes amnesic shellfish poisoning. *Glutamic acid (glutamate) - the ...
Rothman, S., J. Thurston, and R. Hauhart (1987) "Delayed Neurotoxicity of Excitatory Amino Acids In Vitro." Neuroscience, 22 (2 ... Agonist: Inverzni agonist • Ireverzibilni agonist • Parcijalni agonist • Superagonist • Fiziološki agonist. Antagonist: ... Meldrum, B., and J. Garthwaite (1990) "Excitatory Amino Acid Neurotoxicity and Neurodegenerative Disease." Trends in ... "Lesion of Striatal Neurons with Kainic Acid Provides a Model for Huntington's Chorea." Nature, 246: 244-46. ...
Amino acid-derived. *Major excitatory/inhibitory systems: Glutamate system: Agmatine. *Aspartic acid (aspartate) ... Chiodera P, Volpi R, Capretti L, Caffarri G, Magotti MG, Coiro V (April 1996). "Different effects of the serotonergic agonists ... 1-({(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-16-(4-hydroxybenzyl)-13-[(1S)-1- ... Oxytocin is a peptide of nine amino acids (a nonapeptide) in the sequence cysteine-tyrosine-isoleucine-glutamine-asparagine- ...
... in part by upregulating the expression of excitatory amino acid transporter 2 (EAAT2), a.k.a. glutamate transporter 1 (GLT1), ... Sarcosine; Polyamine site agonists: Neomycin. *Spermidine. *Spermine; Other positive allosteric modulators: 24S- ... glutathione has been found to bind to and activate ionotropic receptors that are different from any other excitatory amino acid ... is correlated with a persistent reduction in the expression of excitatory amino acid transporter 2 (EAAT2) in the nucleus ...
R1-amino acid + R2-α-ketoacid ⇌ R1-α-ketoacid + R2-amino acid. A very common α-keto acid is α-ketoglutarate, an intermediate in ... Acute infusion of the drug LY354740 (also known as eglumegad, an agonist of the metabotropic glutamate receptors 2 and 3) ... It is also an excitatory neurotransmitter, in fact the most abundant one, in the vertebrate nervous system. It serves as the ... A key process in amino acid degradation is transamination, in which the amino group of an amino acid is transferred to an α- ...
Amino acid-derived. Major excitatory /. inhibitory systems. Glutamate system. *Agmatine. *Aspartic acid (aspartate) ... Orthosteric Agonist Muscimol,[59] GABA,[59] gaboxadol (THIP),[59] isoguvacine, progabide, piperidine-4-sulfonic acid (partial ... "amino acid", when used without a qualifier, refers specifically to an alpha amino acid. GABA is not an alpha amino acid, ... gamma-Aminobutyric acid, or γ-aminobutyric acid /ˈɡæmə əˈmiːnoʊbjuːˈtɪrɪk ˈæsɪd/, or GABA /ˈɡæbə/, is the chief inhibitory ...
Amino acid-derived. Major excitatory/inhibitory systems. Glutamate system. *Agmatine. *Aspartic acid (aspartate) ... Glycine is a required co-agonist along with glutamate for NMDA receptors. In contrast to the inhibitory role of glycine in the ... is an amino acid that has a single hydrogen atom as its side chain. It is the simplest amino acid (since carbamic acid is ... With acid chlorides, one obtains the amidocarboxylic acid, such as hippuric acid[23] and acetylglycine.[24] With nitrous acid, ...
It differs from Con-R mainly in the C-terminal amino acids and, like Con-R, it induces sleep-like symptoms in young mice, with ... Con-G blocks NMDAR-mediated excitatory postsynaptic currents (EPSCs). Con-G reduces the strength of excitotoxic intracellular ... Sarcosine; Polyamine site agonists: Neomycin. *Spermidine. *Spermine; Other positive allosteric modulators: 24S- ... Rigby AC, Baleja JD, Li L, Pedersen LG, Furie BC, Furie B (December 1997). "Role of gamma-carboxyglutamic acid in the calcium- ...
39-43 amino acids in length, called amyloid beta (Aβ). Aβ is a fragment from the larger amyloid precursor protein (APP). APP is ... Glutamate is an excitatory neurotransmitter of the nervous system, although excessive amounts in the brain can lead to cell ... and GLP-1 receptor agonists". Annals of the New York Academy of Sciences. 1035: 290-315. doi:10.1196/annals.1332.018. PMID ... Omega-3 fatty acid supplements from plants and fish, and dietary docosahexaenoic acid (DHA), do not appear to benefit people ...
... /orphanin FQ (N/OFQ), a 17-amino acid neuropeptide, is the endogenous ligand for the nociceptin receptor (NOP, ORL-1 ... "Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor". Nature. 377 (6549): 532-5. doi: ... as it is excitatory for rodents yet inhibitory for sheep.[5] ... Agonists (abridged; see here for a full list): 3-HO-PCP. *7- ...
Amino acid reuptake inhibitor *Excitatory amino acid reuptake inhibitor (or glutamate-aspartate reuptake inhibitor) ... Inverse agonist. *Positive allosteric modulator (PAM). *Negative allosteric modulator (NAM). *♦ Transporter [Reuptake vs Efflux ... "The involvement of sodium and calcium ions in the release of amino acid neurotransmitters from mouse cortical slices elicited ... γ-aminobutyric acid (GABA),[3] glycine,[4] adenosine,[5] choline (the precursor of acetylcholine),[6] and the endocannabinoids, ...
Amino acid-derived. *Major excitatory/inhibitory systems: Glutamate system: Agmatine. *Aspartic acid (aspartate) ... Agonists: 2-Pyridylethylamine. *Betahistine. *Histamine. *HTMT. *UR-AK49. *Antagonists: First-generation: 4- ...
... derived from the related proteinogenic L-amino acid glutamic acid. Theanine is an analog of this amino acid, and its primary ... Theanine is structurally similar to the excitatory neurotransmitter glutamate, and in accordance, binds to glutamate receptors ... and as an agonist of the latter site.[19] Theanine also binds to group I mGluRs.[15][20] In addition, it inhibits glutamine ... is an amino acid analogue of the proteinogenic amino acids L-glutamate and L-glutamine and is found primarily in particular ...
Although it is a full agonist at CB2 and a partial agonist at CB1, it behaves as a CB1 antagonist in vivo. In rats, virodhamine ... "N-(1-amino-3-methyl-1-oxobutan-2-yl)-1-(cyclohexylmethyl)-1H-indazole-3-carboxamide(AB-CHMINACA), N-(1-amino-3-methyl-1- ... cannabinolic acid-C4. A and/or B. Δ9-THCA-C4 A and/or B ... On the converse, when release of the excitatory ... cannabinolic acid B. Δ9-THCA-C5 B Δ9-Tetrahydro- ... Cannabigerolic acid A. (E)-CBGA-C5 A Cannabigerolic acid A. ...
... -A is 33 amino acid residues long and has two intrachain disulfide bonds; orexin-B is a linear 28 amino acid residue ... Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D2 ... There are two types of orexin: orexin-A and -B (hypocretin-1 and -2). They are excitatory neuropeptides with approximately 50% ... Other dietary nutrients, amino acids, also can activate orexin neurons, and they can suppress the glucose response of orexin ...
... acid Kainic acid N-Methyl-D-aspartic acid Quisqualic acid Excitatory amino acid receptor antagonist Excitatory amino acid ... An excitatory amino acid receptor agonist, or glutamate receptor agonist, is a chemical substance which agonizes one or more of ... reuptake inhibitor Excitatory+amino+acid+agonists at the US National Library of Medicine Medical Subject Headings (MeSH) MeSH ...
... agonist action of excitatory amino acids on mouse spinal cord neurones under voltage clamp., The Journal of Physiology" on ... agonist action of excitatory amino acids on mouse spinal cord neurones under voltage clamp.. Mixed‐agonist action of excitatory ... Mixed‐agonist action of excitatory amino acids on mouse spinal cord neurones under voltage clamp.. Mayer, M L; Westbrook, G L ... "Mixed‐agonist action of excitatory amino acids on mouse spinal cord neurones under voltage clamp.." The Journal of Physiology ...
The release of amino acids from rat neostriatum and substantia nigra in vivo: a dual microdialysis probe analysis.. ... The effect of 6-hydroxydopamine lesions on the release of amino acids in the direct and indirect pathways of the basal ganglia ...
... excitatory synapses, but their functional interactions are unclear. We found that mGluR1 agonist-induced currents and [Ca2+]i ... Metabotropic gamma-aminobutyric acid type B (GABAB) and glutamate receptors (mGluRs) are postsynaptically co-expressed at ... Excitatory Amino Acid Agonists / pharmacology * Excitatory Amino Acid Antagonists / pharmacology * Excitatory Postsynaptic ... Low-concentration baclofen, a GABAB agonist, augmented mGluR1-mediated excitatory synaptic current produced by stimulating PFs ...
Excitatory amino acid antagonists as well as GABA agonists cause barbiturate-like anesthesia in rats. Article date: 1989/1/1 ... Excitatory amino acid antagonists as well as GABA agonists cause barbiturate-like anesthesia in rats.. Article date: 1989/1/1 ... Amino Acids, Receptors, Cell Surface, Receptors, Amino Acid, Receptors, Neurotransmitter, Phenobarbital, Receptors, GABA-A, ... Substances mentioned in the article: Amino Acids; Receptors, Amino Acid; Receptors, Cell Surface; Receptors, GABA-A; Receptors ...
Excitatory Amino Acid Antagonists. Excitatory Amino Acid Agents. To Top. *For Patients and Families ... Adrenergic alpha-2 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter ...
... glutamate exocytosis from astrocytes of the rat hippocampal dentate molecular layer enhances synaptic strength at excitatory ... Excitatory Amino Acid Agonists / pharmacology * Excitatory Amino Acid Antagonists / pharmacology * Exocytosis / drug effects ... Correspondingly, we identify NMDA receptor 2B subunits on the extrasynaptic portion of excitatory nerve terminals. The receptor ... glutamate exocytosis from astrocytes of the rat hippocampal dentate molecular layer enhances synaptic strength at excitatory ...
Excitatory Amino Acid Agonists. Excitatory Amino Acid Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological ... Drug Information available for: Aspartic acid Ornithine Magnesium aspartate Genetic and Rare Diseases Information Center ... will be measured with in vitro NMR spectroscopy to assess for biomarkers of treatment response and to determine the amino acids ...
Excitatory Amino Acid Agonists. Excitatory Amino Acid Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological ...
The interaction of agonists and noncompetitive antagonists at the excitatory amino acid receptors in rat retinal ganglion cells ...
Systemic injection of kainic acid (KA) in the rat produces an animal model of human temporal lobe epilepsy. We examined the ... 0/Amino Acid Transport System X-AG; 0/Excitatory Amino Acid Agonists; 0/Excitatory Amino Acid Transporter 3; 0/Glutamate Plasma ... Excitatory Amino Acid Agonists / toxicity*. Excitatory Amino Acid Transporter 3. Glutamate Plasma Membrane Transport Proteins. ... We examined the temporal expression of the sodium-dependent neuronal glutamate transporter, excitatory amino acid carrier 1 ( ...
Pharmacological Actions : Excitatory Amino Acid Agonists. [+] Schisandra may protect against glutamate-induced toxicity. May 01 ... Problem Substances : Aspartame, Brilliant Blue FCF, L-glutamic Acid, Quinoline Yellow. Adverse Pharmacological Actions : ... Aspartame and L-glutamic acid work synergistically with food coloring agents to induce neurotoxicity.Mar 01, 2006. ... Curcumin and tannic acid protect against glutamate-induced excitotoxicity. Aug 01, 2006. ...
Excitatory Amino Acid Agonists. 7. 4. Vascular smooth muscle cell (VSMC) inhibitor. 7. 5. ...
0 (Excitatory Amino Acid Agonists); 0 (Excitatory Amino Acid Antagonists); 0 (Receptors, Metabotropic Glutamate); 0 ( ... 0 (Amino Acid Transport System ASC); 0 (Minor Histocompatibility Antigens); 0 (Protein Kinase Inhibitors); 0 (SLC1A5 protein, ... cycle intermediates and glutamine-derived non-essential amino acids. This reduces the building blocks required for rapid growth ... Agonistas de Amino cidos Excitat rios/administra o & dosagem. Glutamina/administra o & dosagem. Infarto do Mioc rdio/preven o ...
... which is raised against the amino acids 91-105 mapping with the amino terminal domain of mouse c-Jun p39, i ... 0/Excitatory Amino Acid Agonists; 0/Proto-Oncogene Proteins c-jun; 0/Transcription Factor AP-1; 487-79-6/Kainic Acid ... Excitatory Amino Acid Agonists / toxicity*. Female. Gene Expression Regulation / drug effects*, radiation effects*. ... which is raised against the amino acids 91-105 mapping with the amino terminal domain of mouse c-Jun p39, is simultaneously ...
... the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), and the neuromodulator noradrenaline (NA) have been found to be ... Excitatory Amino Acid Membrane Potential Change Inositol Phospholipid GABAB Receptor Agonist NMDA Response These keywords were ... The excitatory neurotransmitter glutamate, the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), and the ... aim of the study reported here was to analyze the influence of NA and GABA on the action of the glutamate subreceptor agonist N ...
1988) Excitatory amino acid receptors expressed in Xenopus oocytes: agonist pharmacology. Mol Pharmacol 34:298-307. pmid: ... a gain-of-function model that exploits the fact that astrocytes take up neurotransmitter amino acids via excitatory amino acid ... we selected the amino acid D-aspartic acid (Danbolt, 2001, DAniello, 2007) because, interestingly, it is a selective agonist ... 2007) D-Aspartic acid: an endogenous amino acid with an important neuroendocrine role. Brain Res Rev 53:215-234. doi:10.1016/j. ...
NMDA receptor agonist An excitatory amino acid agonist which binds to NMDA receptors and triggers a response. ... NMDA receptor agonist An excitatory amino acid agonist which binds to NMDA receptors and triggers a response. ... quinolinic acid (CHEBI:16675) is a pyridinedicarboxylic acid (CHEBI:36112) quinolinic acid (CHEBI:16675) is conjugate acid of ... quinolinic acid (CHEBI:16675) has role Escherichia coli metabolite (CHEBI:76971) quinolinic acid (CHEBI:16675) has role human ...
NMDA receptor agonist An excitatory amino acid agonist which binds to NMDA receptors and triggers a response. ... NMDA receptor agonist An excitatory amino acid agonist which binds to NMDA receptors and triggers a response. ... glycine (CHEBI:15428) is a α-amino acid (CHEBI:33704) glycine (CHEBI:15428) is a proteinogenic amino acid (CHEBI:83813) glycine ... serine family amino acid (CHEBI:26650) glycine (CHEBI:15428) is conjugate acid of glycinate (CHEBI:32508) glycine (CHEBI:15428 ...
The excitatory potency of the acidic amino acids glutamate and aspartate in various regions of the central nervous system (CNS ... Garthwaite G, Garthwaite J. Neurotoxicity of excitatory amino acid receptor agonists in rat cerebellar slices: dependence on ... Neurotoxicity of excitatory amino acids. In: McGeer EG, Olney JW, McGeer PL, eds. Kainic acid as a Tool in Neurobiology. New ... Structure-function studies on N-oxalyldiamino-dicarboxylic acids and excitatory amino acid receptors: evidence that beta-L-ODAP ...
l-Glutamate is the most abundant of a group of endogenous amino acids in the mammalian central nervous system which presumably ... function as excitatory neurotransmitters and under abnormal conditions... ... Garthwaite G, Garthwaite J (1986) Neurotoxicity of excitatory amino acid receptor agonists in rat cerebellar slices. Dependence ... Structure-activity relationships in the development of excitatory amino acid receptor agonists and competitive antagonists. ...
Excitatory Amino Acid AgonistsIBA 02/2004. Therapy/Procedure. 1. Traditional Medicine (Folk Remedies) 01/2011. ...
Lesion-Induced Relative Supersensitivity to an Excitatory Amino Acid Agonist in the Cat Dorsal Lateral Geniculate Nucleus ...
They are conditional because they were evoked by excitatory amino acid agonists (MacLean et al., 1997; Schmidt et al., 1998; ... acid kynurenic (1.5 mm), N-methyl-dl-aspartic acid (NMA) (15 μm), 5-hydroxytryptamine creatinine sulfate (5-HT) (5 μm), TTX ( ... Ipsilaterally projecting excitatory interneurons have been hypothesized to be the source of rhythm generation in the locomotor ... 2007) Intrinsic bursters increase the robustness of rhythm generation in an excitatory network. J Neurophysiol 97:1515-1526. ...
They include excitatory amino acid receptor agonists and excitatory amino acid receptor antagonists. Christensen, Inge T.; ... Excitatory amino acid receptor ligands are ligands of excitatory amino acid receptors (EAARs), also known as glutamate ... "Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to ... homoibotenic acid". Journal of Medicinal Chemistry. 35 (19): 3512-3519. doi:10.1021/jm00097a008. v t e v t e. ...
Domoic acid is an excitatory amino acid analogue of glutamate; a neurotransmitter in the brain that activates glutamate ... In addition there is a synergistic effect with endogenous glutamate and N-Methyl-D-aspartate receptor agonists that contribute ... Domoic acid is a structural analog of kainic acid, proline, and endogenous excitatory neurotransmitter glutamate.[8] Ohfune and ... "Domoic Acid Toxicity". The Marine Mammal Center. Retrieved 2 April 2015.. *^ "Domoic Acid Poisoning". Northwest Fisheries ...
Excitatory Amino Acid Agonists: 1 study in 1 result : IBA. *Cholinergic Antagonists (Anticholinergics): 1 study in 1 result : ... Excitatory Amino Acid Antagonists: 3 outcomes 1 study in 11 results : IBA ... Amino Acid Transport System X-AG (Glutamate Transporter): 17 results : IBA. *Ketoglutarate Dehydrogenase Complex (Oxoglutarate ... Glycine (Aminoacetic Acid): 1 outcome in 8 results : FDA 23 Generic. *Aspirin (Acetylsalicylic Acid): 1 outcome in 8 results : ...
Smith, D. H. et al., "Traumatic Brian Injury and Excitatory Amino Acids," 107:1445-1458. cited by other.. Akman et al. " ... By way of background, gamma-aminobutyric acid (GABA) and glutamic acid are major neurotransmitters which are involved in the ... amino acid addition salts, esters, amides, and prodrugs of the compounds of the present invention which are, within thescope of ... This class of drugs are strong GABA agonists which are effective on both GABA-B and GABA-A receptors.. One specific benzylidene ...
Excitatory Amino Acid Antagonists. Excitatory Amino Acid Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Adrenergic alpha-2 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. ...
Increased calbindin-D28K immunoreactivity in rat cerebellar Purkinje cell with excitatory amino acids agonists is not dependent ...
  • An excitatory amino acid receptor agonist, or glutamate receptor agonist, is a chemical substance which agonizes one or more of the glutamate receptors. (wikipedia.org)
  • L‐glutamic and L‐homocysteic acid responses behaved as though due to simultaneous activation of both NMDA and either kainate or quisqualate receptors. (deepdyve.com)
  • We suggest that L‐glutamate acts as a mixed agonist at both NMDA and non‐NMDA receptors. (deepdyve.com)
  • Metabotropic gamma-aminobutyric acid type B (GABAB) and glutamate receptors (mGluRs) are postsynaptically co-expressed at cerebellar parallel fiber (PF)-Purkinje cell (PC) excitatory synapses, but their functional interactions are unclear. (nih.gov)
  • We found that mGluR1 agonist-induced currents and [Ca2+]i increases in PCs were enhanced following co-activation of GABAB receptors. (nih.gov)
  • These results indicate that postsynaptic GABAB receptors functionally interact with mGluR1 and enhance mGluR1-mediated excitatory transmission at PF-PC synapses. (nih.gov)
  • Results of this study indicate that paeoniflorin-induced inhibition of excitatory amino acid agonist- and high-dose morphine-induced nociceptive behaviors might be due to modulation of NMDA receptors, specifically the NR2B subunit. (biomedcentral.com)
  • The excitation of glutamate is partially mediated through the ionotropic glutamate receptors (iGluRs) including N -methyl-D-aspartate (NMDA), α-amino-3-hydroxy-5-methylisoxazole-4- propionic acid (AMPA), and kainate receptors [ 8 , 9 ]. (biomedcentral.com)
  • An excitatory amino acid agonist which binds to NMDA receptors and triggers a response. (ebi.ac.uk)
  • The effects of domoic acid have been attributed to several mechanisms, but the one of concern is through glutamate receptors . (wikipedia.org)
  • Domoic acid has a very strong affinity for these receptors, which results in excitotoxicity initiated by an integrative action on ionotropic glutamate receptors at both sides of the synapse, coupled with the effect of blocking the channel from rapid desensitization. (wikipedia.org)
  • Excitatory amino acid receptor ligands are ligands of excitatory amino acid receptors (EAARs), also known as glutamate receptors. (wikipedia.org)
  • Classical cannabinoid agonists (structures shown in Table 1 ) bind to and activate cannabinoid receptors 1 and 2 (CB1, CB2) that modulate signal transduction cascades to produce various physiological and pathological outcomes. (frontiersin.org)
  • Although excitatory amino acid (FAA) receptors have been investigated extensively in the limbic system and neocortex, less is known of the function of EAA receptors in the brainstem. (springer.com)
  • A number of biochemical and electrophysiological studies suggest that the synapse between the ipsilateral vestibular (VIIIth) nerve and the brainstem vestibular nucleus (VN) is mediated by an EAA acting predominantly on kainate or α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors. (springer.com)
  • Collingridge G. L. and Lester R. A. J. (1989) Excitatory amino acid receptors in the vertebrate central nervous system. (springer.com)
  • [6] [13] It has been found to act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors . (wikipedia.org)
  • By fast application of agonists to isolated neurons, it was first demonstrated that all neurons responded to glutamate with currents mediated by α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, and a majority of neurons also with currents mediated by N-Methyl-D-aspartate (NMDA) receptors. (diva-portal.org)
  • All neurons also responded to γ-aminobutyric acid (GABA) and glycine with currents mediated by GABAA receptors and glycine receptors, respectively. (diva-portal.org)
  • Glutamate is the major excitatory neurotransmitter in the mammalian central nervous system and exerts its action through multiple ionotropic and metabotropic receptors. (asahq.org)
  • Watkins et al (1990) Experiments with kainate and quisqualate agonists and antagonists in relation to the sub-classification of non-NMDA receptors. (tocris.com)
  • The glutamate receptor class is a class of excitatory amino acid neurotransmitter receptors. (collaborativedrug.com)
  • There are AMPA receptors, kainate receptors, and NMDA receptors, named after selective agonists, pharmacology going back into the 80s. (collaborativedrug.com)
  • High-resolution-MS and NMR ( 1 H, 13 C, COSY, heteronuclear sequential quantum correlation, heteronuclear multiple bond correlation) analysis identified the paralytic compound as quisqualic acid (C 5 H 7 N 3 O 5 ), a known but rare agonist of excitatory amino acid receptors. (pnas.org)
  • However, the role of excitatory and inhibitory amino acid receptors and their interaction with α7-nAChR in physiological and glaucomatous events remains unknown. (arvojournals.org)
  • Highly selective agonist for group ii mGluRs and has no effect on ionotropic excitatory amino acid receptors. (agscientific.com)
  • 1S,3R)-homo-ACPD are the first agonist to show selectivity for mGlu receptors over iGlu receptors. (agscientific.com)
  • 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. (umassmed.edu)
  • GABA B receptors as potential targets for drugs able to prevent excessive excitatory amino acid transmission in the spinal cord. (rndsystems.com)
  • Blockade of GABA B receptors facilitates muscarinic agonist-induced epileptiform activity in immature rat piriform cortex in vitro. (rndsystems.com)
  • Consequently, there is much interest in the modulation of glutamate receptors, especially the N-methyl-Daspartate (NMDA) and α-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) subtypes [22]. (scirp.org)
  • A similar pattern of an initial general vasoconstriction followed by hindquarter vasodilation can be seen after stimulation of S -α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors in the NTS ( 9 ). (physiology.org)
  • The pharmacological actions of L-proline on excitatory and inhibitory amino acid receptors have been characterized under voltage-clamp conditions, using cultured dissociated neurons from the dorsal horn of the rat spinal cord. (aspetjournals.org)
  • Our results using dorsal horn neurons grown in culture indicate that L-proline is a weak agonist at strychnine-sensitive glycine receptors and at both NMDA and non-NMDA glutamate receptors. (aspetjournals.org)
  • Furthermore, the ability of L-proline to stimulate Ca2+ entry after activation of excitatory amino acid receptors implicates L-proline as a potential endogenous excitotoxin. (aspetjournals.org)
  • Excitatory amino acid antagonists as well as GABA agonists cause barbiturate-like anesthesia in rats. (muscimol.xyz)
  • Watkins JC, Krogsgaard LP, Honore T. Structure-activity relationships in the development of excitatory amino acid receptor agonists and competitive antagonists. (springer.com)
  • Schwarcz R, Meldrum B. Excitatory aminoacid antagonists provide a therapeutic approach to neurological disorders. (springer.com)
  • They include excitatory amino acid receptor agonists and excitatory amino acid receptor antagonists. (wikipedia.org)
  • Davies et al (1984) Phosphonodipeptides and piperazine derivatives as antagonists of amino acid-induced and synaptic excitation in mammalian and amphibian spinal cord. (tocris.com)
  • Evans et al (1987) A comparison of excitatory amino acid antagonists acting at primary afferent C fibres and motoneurones of the isolated spinal cord of the rat. (tocris.com)
  • Clozapine, but not haloperidol, produces bursts of excitatory postsynaptic potentials (EPSPs), which are blocked by glutamate receptor antagonists, suggesting that these EPSPs are the result of increasing release of excitatory amino acids. (selleckchem.com)
  • At a holding potential of -62 mV, millimolar concentrations of L-proline elicited an inward current that was partially antagonized by D-(-)-2-amino-5-phosphonopentanoic acid (APV), 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), and strychnine and was virtually abolished (97% block) by a combination of all three antagonists. (aspetjournals.org)
  • The results confirm that astrocytes can act as excitatory nodes that can influence neurons over a significant range in a number of brain regions. (jneurosci.org)
  • Curtis D.R., Watkins J.C. The excitation and depression of spinal neurons by structurally related amino acids. (springer.com)
  • DHEA (100 nM) protected cultured neurons against the neurotoxic actions of either AMPA (25 μM) or kainic acid (1 mM) as well. (pnas.org)
  • Cochran S., Kasik P., and Precht W. (1987) Pharmacological aspects of excitatory synaptic transmission to second-order vestibular neurons in the frog. (springer.com)
  • These findings show that fast-acting excitatory and inhibitory amino-acid transmitters are most likely important for communication between hypothalamic neurons. (diva-portal.org)
  • Application of agonists to isolated neurons revealed cross-talk, detected as an apparent cross-desensitization, between the responses to GABA and those to glycine. (diva-portal.org)
  • Neurons pretreated with TNF alpha exhibited increased intracellular Ca2+ concentrations following membrane depolarization but reduced intracellular Ca2+ concentration responses to excitatory amino acids, compared with neurons in untreated control cultures or cultures cotreated with kappaB decoy DNA. (nih.gov)
  • Administration of excitatory amino acids may be toxic for retinal cells and block axonal transport in retinal neurons. (nii.ac.jp)
  • The D-form may act selectively on retinal neurons, suggesting that it may be an agonist of an excitatory amino acid receptor. (nii.ac.jp)
  • N‐methyl‐D‐aspartate (NMDA) and L‐aspartic acid responses had a negative slope conductance at membrane potentials more negative than ‐30 mV. (deepdyve.com)
  • In the presence of the NMDA receptor antagonist (+/‐)‐2‐aminophosphonovaleric acid (2‐APV) the response to L‐glutamate became less voltage sensitive and resembled responses evoked by kainate or quisqualate. (deepdyve.com)
  • Correspondingly, we identify NMDA receptor 2B subunits on the extrasynaptic portion of excitatory nerve terminals. (nih.gov)
  • Antisense oligodeoxynucleotides of NMDA receptor subunits NR1, NR2A, NR2B significantly enhanced the inhibition of paeoniflorin on excitatory amino acid-and high-dose morphine-induced nociception. (biomedcentral.com)
  • The aim of the study reported here was to analyze the influence of NA and GABA on the action of the glutamate subreceptor agonist N-methyl-D-aspartate (NMDA). (springer.com)
  • We have found that DHEA(S) can prevent or reduce the neurotoxic actions in the hippocampus of the glutamate agonists N -methyl- d -aspartic acid (NMDA) both in vitro and in vivo or α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and kainic acid in vitro . (pnas.org)
  • Using patch clamp techniques, the GABA-elicited membrane current and miniature excitatory postsynaptic currents (mEPSCS) of RGCs and the NMDA-gated current (INMDA) were detected in rat retinal slices. (arvojournals.org)
  • The α7-nAChR specific agonist PNU-282987 enhanced the amplitude of currents elicited by GABA and reduced the amplitude of currents elicited by NMDA. (arvojournals.org)
  • L-AP4 (10 mM, 30 nl) produced sympathoinhibitory responses that were abolished by the NMDA receptor antagonist 2-amino-5-phosphonovaleric acid (AP-5, 10 mM) but were unaffected by the non-NMDA antagonist 6-nitro-7-sulfamobenzoquinoxaline-2,3-dione (NBQX, 2 mM). (elsevier.com)
  • Each of the excitatory amino acid agonists, quisqualate, NMDA and kainate, inhibited [ 3 H]inositol phospholipid synthesis, but only quisqualate affected [ 3 H]inositol phospholipids available to the α 1 -adrenergic receptor. (elsevier.com)
  • This paper is a review of data concerning the role of excitatory amino acids in the processes of learning and memory and in the pathogenesis and treatment of disorders thereof. (springer.com)
  • Low-concentration baclofen, a GABAB agonist, augmented mGluR1-mediated excitatory synaptic current produced by stimulating PFs. (nih.gov)
  • Here we show that glutamate exocytosis from astrocytes of the rat hippocampal dentate molecular layer enhances synaptic strength at excitatory synapses between perforant path afferents and granule cells. (nih.gov)
  • We applied the group-I metabotropic glutamate (mGlu) receptor agonist, 3,5-dihydroxyphenylglycine (DHPG), to neonatal or adult rat hippocampal slices at concentrations (10 microM) that induced a short-term depression (STD) of excitatory synaptic transmission at the Schaffer collateral/CA1 synapses. (bath.ac.uk)
  • Addition of clustered EphB1/Fc alone to the slices induced a small but nondecremental depression of excitatory synaptic transmission, which differed from the depression induced by 10 microM DHPG. (bath.ac.uk)
  • Presynaptic plasma membrane Ca2+ ATPase isoform 2a regulates excitatory synaptic transmission in rat hippocampal CA3. (rndsystems.com)
  • Jope, RS & Xiaohua, L 1989, ' Inhibition of inositol phospholipid synthesis and norepinephrine-stimulated hydrolysis in rat brain slices by excitatory amino acids ', Biochemical Pharmacology , vol. 38, no. 4, pp. 589-596. (elsevier.com)
  • Domoic acid is a structural analog of kainic acid , proline , and endogenous excitatory neurotransmitter glutamate . (wikipedia.org)
  • Several lines of evidence suggest that endogenous excitatory amino acids contribute to the pathophysiology of neuronal injury in major neurological disorders. (ahajournals.org)
  • 3. The effects of (-)-baclofen, a gamma-aminobutyric acid (GABA)B receptor agonist, were studied on the cortically evoked DPSPs. (nih.gov)
  • 2 h) did not alter Ca2+ current or glutamate receptor agonist-induced currents. (nih.gov)
  • Selective group I metabotropic glutamate receptor agonist which activates both mGluR1 and mGluR5. (axonmedchem.com)
  • Although quiescent at 4 days in vitro (DIV), HN acquired distinctive SCO patterns as they matured to form extensive dendritic networks by 16 DIV. Challenge with kainate, a kainate receptor (KAR) agonist, 4-aminopyridine (4-AP), a K + channel blocker, or pilocarpine, a muscarinic acetylcholine receptor agonist, caused distinct changes in SCO dynamics. (aspetjournals.org)
  • The excitatory neurotransmitter glutamate, the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), and the neuromodulator noradrenaline (NA) have been found to be involved in the pathophysiology of several neuropsychiatric disorders, especially schizophrenia and epilepsy (cf. (springer.com)
  • It was shown that application of the TRPV1 agonist capsaicin increased the frequency of excitatory AMPA receptor- mediated as well as inhibitory GABAA receptor-mediated postsynaptic currents. (diva-portal.org)
  • This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. (tocris.com)
  • GZFLc instead exhibited direct inhibitory effect against COX2, a critical enzyme that catalyzes arachidonic acid conversion to prostaglandins. (hindawi.com)
  • Gamma-aminobutyric acid receptor type A (GABA A ) and glycine receptor systems are thought to be the major inhibitory systems in the CNS. (asahq.org)
  • 7. Application of the GABA uptake inhibitor nipecotic acid (100-300 microM) clearly reduced the amplitude of both kynurenate-and bicuculline-sensitive DPSPs evoked at low frequencies of stimulation (0.01-0.3 Hz), but had lower effects at higher stimulation rates (1-3 Hz). (nih.gov)
  • Application of nipecotic acid increased the duration of membrane responses to exogenously applied GABA. (nih.gov)
  • Presynaptic modulation of γ-aminobutyric acid (GABA) release by an alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist promotes retinal ganglion cell (RGC) survival and function, as suggested by a previous study on a chronic glaucomatous model from our laboratory. (arvojournals.org)
  • Microinjection of S -α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) in the nucleus of the solitary tract (NTS) of conscious rats causes hypertension, bradycardia, and vasoconstriction in the renal, mesenteric, and hindquarter vascular beds. (physiology.org)
  • The membrane-bound protein is the principal transporter that clears the excitatory neurotransmitter glutamate from the extracellular space at synapses in the central nervous system. (genecards.org)
  • [4] Clozapine is a full agonist at the muscarinic M4 receptor (EC50 = 11 nM), producing inhibition of forskolin-stimulated cAMP accumulation. (selleckchem.com)
  • Inhibition by excitatory amino acid agonists of norepinephrine (NE)-stimulated phosphoinositide hydrolysis was studied in rat brain slices. (elsevier.com)
  • Consumption of about 5 ng of l -quisqualic acid (thought to mimic the neurotransmitter l -glutamic acid), equivalent to one or two petals, is sufficient to paralyze the beetles. (sciencemag.org)
  • Glutamic acid decarboxylase mRNA in rat brain: regional distribution and effects of intrastriatal kainic acid. (umassmed.edu)
  • Neurotoxicity of excitatory amino acids. (springer.com)
  • Garthwaite G, Garthwaite J. Amino acid neurotoxicity: intracellular sites of calcium accumulation associated with the onset of irreversible damage to rat cerebellar neurones in vitro. (springer.com)
  • Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose. (umassmed.edu)
  • Intraperitoneal injection of kainic acid at convulsant doses to the adult rat produces cell death with morphological features of necrosis, together with the appearance of cells with fine granular chromatin degeneration and small numbers of apoptotic-like cells, in the entorhinal and piriform cortices, basal amygdala, certain thalamic nuclei, and CA1 region of the hippocampus. (biomedsearch.com)
  • In the brain, domoic acid especially damages the hippocampus and amygdaloid nucleus. (wikipedia.org)
  • Mixed‐agonist action of excitatory amino acids on mouse spinal cord neurones under voltage clamp. (deepdyve.com)
  • Antinociceptive actions of mGluR3 agonists have been demonstrated in the periphery, spinal cord, and amygdale. (asahq.org)
  • Ceramide, an intracellular messenger that activates the transcription factor NF-kappaB, mimicked the actions of TNFs on Ca2+ current density and currents induced by glutamate receptor agonists. (nih.gov)
  • Cotreatment with kappaB decoy DNA abolished the effects of TNF alpha on Ca2+ current and excitatory amino acid-induced currents, demonstrating a requirement for NF-kappaB activation in the actions of TNF alpha. (nih.gov)
  • The frequency and the amplitude of glutamate receptor-mediated miniature glutamatergic excitatory postsynaptic currents (mEPSCs) were not significantly different between the control and glaucomatous RGCs. (arvojournals.org)
  • Translocation of glutamate transporter subtype excitatory amino acid carrier 1 protein in kainic acid-induced rat epilepsy. (biomedsearch.com)
  • Glutamate transporters, also known as excitatory amino acid transporters (EAATs), are sodium- and potassium-dependent members of the solute carrier family 6 (SLC1), widely distributed throughout the brain. (genecards.org)
  • Today, L-glutamate is accepted as the predominant fast excitatory neurotransmitter in the vertebrate brain. (springer.com)
  • Intraventricular kainic acid preferentially destroys hippocampal pyramidal cells. (springer.com)
  • Accordingly, neuropathological findings after postnatal hypoxia/ischemia are similar to those induced by exogenous glutamate agonists. (ahajournals.org)
  • This phenomenon was replicated by exogenous preexposure to the amino acid D-aspartate (D-Asp). (jneurosci.org)
  • In addition to providing caution concerning the use of nicotinic agonists in the improvement of cognitive function in people with schizophrenia taking these drugs, this led us to try 5HT2 antagonist treatment to reduce nicotine self-administration. (duke.edu)
  • This cardioprotective effect was mimicked by the mGluR1 agonist, DHPG (10 M), and abolished when glutamate was coinjected with the mGluR1 antagonist YM298198 (100 nM). (bireme.br)
  • mGluR1 and mGluR5 agonist (rac. (axonmedchem.com)
  • The excitatory potency of the acidic amino acids glutamate and aspartate in various regions of the central nervous system (CNS) has been recognized since the 1960 s. 1,2 Nevertheless, the earlier findings that these amino acids are ( 1 ) constituents of intermediary metabolism and are ( 2 ) located in the brain ubiquitously in high concentrations rendered them unlikely candidates as neurotransmitters. (springer.com)
  • In addition there is a synergistic effect with endogenous glutamate and N-Methyl-D-aspartate receptor agonists that contribute to the excitotoxicity. (wikipedia.org)
  • Using the alpha7 and beta2(*) nAChR-selective agonists (R)-N-(1-azabicyclo[2.2.2]-oct-3-yl)(5-(2-pyridyl)thiophene-2-carboxamide) (compound A) and 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine (5-iodo-A-85380), respectively, in conjunction with inhibitors of voltage-operated Ca(2+) channels (VOCCs) and intracellular Ca(2+) stores, we show that [(3)H]d-aspartate release evoked by activation of beta2(*) nAChRs occurs via VOCCs. (unboundmedicine.com)
  • Sodium-dependent, high-affinity amino acid transporter that mediates the uptake of L-glutamate and also L-aspartate and D-aspartate (PubMed:7521911, PubMed:14506254, PubMed:15265858, PubMed:26690923). (genecards.org)
  • Excitatory amino acids and neuronal plasticity. (tocris.com)
  • The current‐voltage relation of responses evoked by brief pressure applications of excitatory amino acids was examined over a membrane potential range of ‐100 to +70 mV. (deepdyve.com)
  • Responses to kainic and quisqualic acids were relatively linear within +/‐ 20 mV of the resting potential. (deepdyve.com)
  • In contrast, over the same potential range the slope conductance of responses evoked by L‐glutamic and L‐homocysteic acids was close to zero. (deepdyve.com)
  • a much weaker voltage sensitivity was observed for responses evoked by kainic and quisqualic acids. (deepdyve.com)
  • Clozapine potently antagonizes agonist-induced responses at the other four muscarinic receptor subtypes. (selleckchem.com)
  • Previous studies have demonstrated that microinjection of the putative group III metabotropic glutamate receptor (mGluR) agonist, L(+)-2-amino-4- phosphonobutyric acid (L-AP4), into the nucleus tractus solitarius (NTS) produces depressor and sympathoinhibitory responses. (elsevier.com)
  • Estimates of relative potency were obtained, however, by comparison with responses elicited by selective agonists. (aspetjournals.org)
  • Aims of this present study were to investigate effects of paeoniflorin on excitatory amino acid agonist- or high-dose morphine-induced nociceptive behaviors in mice. (biomedcentral.com)
  • An earlier report indicated that PF reduced formalin- and acetic acid-induced nociception in mice [ 32 ]. (biomedcentral.com)
  • The protective effect of berberine agonist significantly recovered learning and memory skills, attenuated brain edema and inhibited matrix metalloproteinase‑3 and ‑9 protein expression in mice with severe TBI. (spandidos-publications.com)
  • Berberine agonist significantly reduced inflammation, oxidative stress and apoptosis levels in mice with severe TBI. (spandidos-publications.com)
  • In endotoxin-treated mice, the activity of indoleamine-2,3-dioxygenase(IDO), the first enzyme of the kynurenine pathway that synthesizes QUIN, is increased in several extrahepatic tissues, plasma L-kynurenine (L-KYN) is elevated [4], and QUIN, 3-hydroxykynurenine L-TRP and 5-hydroxyindoleacetic acid (5-HIAA) concentrations are increased in cerebral cortex [5, 61. (docme.ru)
  • have shown that opioids [especially μ-opioid receptor (MOR) agonists] can be effective in treating neuropathic pain. (aspetjournals.org)
  • These conflicting data may result from differences in the type of nerve injury, route of drug administration, potency and receptor selectivity of the particular opioid agonist, and the methods of measuring neuropathic pain. (aspetjournals.org)
  • [16] μ-Opioid receptor agonists typically induce euphoria , and in accordance, tianeptine does so at high doses well above the normal therapeutic range. (wikipedia.org)
  • This finding links to further injections of excitatory amino acid receptor agonists opioid antagonist and melanocortin 1 receptor genes. (healmyptsd.com)
  • Moreover, brain structures which are considered anatomical substrata for learning and memory may be particularly vulnerable to the neurotoxic actions of these excitatory amino acids, especially in the elderly who are also the segment of the population most susceptible to impairments of mnemonic function. (springer.com)
  • Geranium-derived and synthetic l -quisqualic acid demonstrated the same positive paralytic dose-response. (pnas.org)
  • A traditional Chinese medicine, Shih-chun-tze, used to treat infections with the large parasitic nematode Ascaris has as its active ingredient l -quisqualic acid, a known but rare agonist of excitatory amino acids. (sciencemag.org)
  • In the present study, the neuroprotective effect of berberine agonist rescue learning and memory in severe traumatic brain injury (TBI), and the possible mechanism underlying these observations was explored. (spandidos-publications.com)
  • Collectively, results of the present study revealed that the neuroprotective effect of berberine agonist rescues learning and memory skills in severe TBI. (spandidos-publications.com)
  • Aprikyan GV, Gekchyan KG (1988) Release of neurotransmitter amino acids from rat brain synaptosomes. (springer.com)
  • These include the excitatory amino acid glutamate, the neuropeptide substance P, and the brain-derived neurotrophic factor. (aspetjournals.org)
  • In this study we evaluate the ability of triflusal (2-acetoxy-4-trifluoromethylbenzoic acid), an antiplatelet agent inhibitor of NF-κB activation, to improve lesion outcome after excitotoxic damage to the immature brain. (ahajournals.org)
  • Kainic acid is utilized in primary neuronal cell cultures and acute brain slice preparations to study the physiological effect of excitotoxicity and assess the neuroprotective capabilities of potential therapeutics. (agscientific.com)
  • l -Glutamate is the most abundant of a group of endogenous amino acids in the mammalian central nervous system which presumably function as excitatory neurotransmitters and under abnormal conditions may behave as neurotoxins. (springer.com)
  • Radiation-induced apoptosis in developing rats and kainic acid-induced excitotoxicity in adult rats are associated with distinctive morphological and biochemical c-Jun/AP-1 (N) expression. (biomedsearch.com)
  • In recent years there have been significant advances in our understanding of the contribution of excitatory glutamatergic transmission to seizures. (iospress.com)
  • Banay-Schwartz M, Lajtha A, Palkovits M (1989) Changes with ageing in the levels of amino acids in rat CNS structural elements. (springer.com)
  • In the present study, inoculation of macaques with D/ l/California, an immunosuppressive serotype 1 type D retrovirus, was associated with acute and chronic increases in CSF and serum quinolinic acid concentrations in macaques that had developed SAIDS, a simian disease analogous to AIDS in humans-particularly macaques with demonstrable opportunistic infections. (docme.ru)
  • In this review we summarize data from studies performed in humans and animals and focus on iono- and metabotropic excitatory amino acid receptor-mediated events in seizures and epilepsy. (iospress.com)
  • Systemic injection of kainic acid (KA) in the rat produces an animal model of human temporal lobe epilepsy. (biomedsearch.com)
  • Intracerebral or systemic administration of glutamate receptor agonists has become a popular way to induce seizures in rodents. (iospress.com)
  • Although these levels are not correlated with encephalitis severity, quinolinic acid may be an etiologic agent in HIV-1-related neuropathology. (acnp.org)
  • Increased ratio of quinolinic acid to kynurenic acid in cerebrospinal fluid of D retrovirusЧinfected rhesus macaques Relationship to clinical and viral status. (docme.ru)
  • Increased Ratio of Quinolinic Acid to Kynurenic Acid in Cerebrospinal Fluid of D Retrovirus-infected Rhesus Macaques: Relationshp to Clinical and Viral Status Melvyn P. Heyes, PhD," Ivan N. Mefford, PhD,t Bonnie J. Quearry, BS," Manish Dedhia," and Andrew Lackner, DVMS. (docme.ru)
  • Increased concentrations of excitotoxin quinolinic acid in cerebrospinal fluid (CSF) are associated with infection with the human immunodeficiency virus (HIV-1) and have been implicated in the pathogenesis of the acquired immune deficiency syndrome (AIDS) dementia complex. (docme.ru)
  • quinolinic acid, 15.6fold). (docme.ru)
  • CSF quinolinic acid, but not kynurenic acid, was also increased in viremic macaques with SAIDS-related complex (2.4-fold) and asymptomatic virus positive carriers (3.4-fold). (docme.ru)
  • Macaques that had recovered from D/ Kalifornia infection and were antibody positive and virus negative had normal CSF quinolinic acid and kynurenic acid concentrations. (docme.ru)
  • Macaques infected with D/ l/California may provide a primate model for investigation of the mechanisms involved in increases in CSF quinolinic acid in retrovirus and other infectious diseases, including HIV-1. (docme.ru)
  • It remains to be determined whether the increased CSF quinolinic acid concentrations and the increased ratio of quinolinic acid to kynurenic acid have neurological significance or are a useful "marker" of infection. (docme.ru)
  • Heyes MP, Mefford IN, Quearry BJ, Dedhia M, Lackner A. Increased ratio of quinolinic acid to kynurenic acid in cerebrospinal fluid of D retrovirus-infected rhesus macaques: relationship to clinical and viral status. (docme.ru)
  • Glutamate is an excitatory amino acid (EAA) and a crucial neurotransmitter involved in nociceptive signaling and pain modulation in the central nervous system [ 1 - 5 ]. (biomedcentral.com)
  • The BTB/kelch protein KRIP6 binds within a 58 amino acid segment of GluR6 proximal to the plasma membrane. (thebiogrid.org)
  • The membrane potential‐chord conductance relation of the ionic mechanism activated by excitatory amino acids, derived using the driving force for ionic current, showed two types of behaviour. (deepdyve.com)
  • In situ injection of kainic acid: A new method for selectively lesioning neural cell bodies while sparing axons of passage. (springer.com)