Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.
Inorganic salts of HYDROGEN CYANIDE containing the -CN radical. The concept also includes isocyanides. It is distinguished from NITRILES, which denotes organic compounds containing the -CN radical.
A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.
An exocellulase with specificity for a variety of beta-D-glycoside substrates. It catalyzes the hydrolysis of terminal non-reducing residues in beta-D-glucosides with release of GLUCOSE.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
A kingdom of eukaryotic, heterotrophic organisms that live parasitically as saprobes, including MUSHROOMS; YEASTS; smuts, molds, etc. They reproduce either sexually or asexually, and have life cycles that range from simple to complex. Filamentous fungi, commonly known as molds, refer to those that grow as multicellular colonies.
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.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
Pregnane derivatives in which two side-chain methyl groups or two methylene groups in the ring skeleton (or a combination thereof) have been oxidized to keto groups.
Derivatives of the steroid androstane having three double bonds at any site in any of the rings.
A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.
The 5-beta-reduced isomer of ANDROSTERONE. Etiocholanolone is a major metabolite of TESTOSTERONE and ANDROSTENEDIONE in many mammalian species including humans. It is excreted in the URINE.
A biologically active 5-alpha-reduced metabolite of plasma PROGESTERONE. It is the immediate precursor of 5-alpha-pregnan-3-alpha-ol-20-one (ALLOPREGNANOLONE), a neuroactive steroid that binds with GABA(A) RECEPTOR.
The family of steroids from which the androgens are derived.
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.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
Cyclohexane ring substituted by one or more ketones in any position.
A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.
Unsaturated androstane derivatives which are substituted with two hydroxy groups in any position in the ring system.
Saturated derivatives of the steroid pregnane. The 5-beta series includes PROGESTERONE and related hormones; the 5-alpha series includes forms generally excreted in the urine.
An intermediate in TESTOSTERONE biosynthesis, found in the TESTIS or the ADRENAL GLANDS. Androstenediol, derived from DEHYDROEPIANDROSTERONE by the reduction of the 17-keto group (17-HYDROXYSTEROID DEHYDROGENASES), is converted to TESTOSTERONE by the oxidation of the 3-beta hydroxyl group to a 3-keto group (3-HYDROXYSTEROID DEHYDROGENASES).
An indole-dione that is obtained by oxidation of indigo blue. It is a MONOAMINE OXIDASE INHIBITOR and high levels have been found in urine of PARKINSONISM patients.
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.
Steroid derivatives formed by oxidation of a methyl group on the side chain or a methylene group in the ring skeleton to form a ketone.
Steroids that contain a ketone group at position 17.
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.
Metabolites or derivatives of PROGESTERONE with hydroxyl group substitution at various sites.
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.
Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.
Unsaturated derivatives of PREGNANES.
(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 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.
Steroids in which fission of one or more ring structures and concomitant addition of a hydrogen atom at each terminal group has occurred.
A class of chemicals that contain an anthracene ring with a naphthalene ring attached to it.
Enzymes that catalyze the transposition of double bond(s) in a steroid molecule. EC 5.3.3.
INDOLES which have two keto groups forming QUINONES like structures of the indole aromatic ring.
A class of ionotropic glutamate receptors characterized by their affinity for the agonist AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid).
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 non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
Piperazines with two keto oxygens.
An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
An anticonvulsant that is the active metabolite of TRIMETHADIONE.
Drugs that bind to and activate excitatory amino acid receptors.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
Compounds that inhibit AROMATASE in order to reduce production of estrogenic steroid hormones.
Unsaturated derivatives of the ESTRANES with methyl groups at carbon-13, with no carbon at carbon-10, and with no more than one carbon at carbon-17. They must contain one or more double bonds.
An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer.
A class of ionotropic glutamate receptors characterized by their affinity for KAINIC ACID.
Compounds with a five-membered heterocyclic ring with two nitrogens and a keto OXYGEN. Some are inhibitors of TNF-ALPHA production.
A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms.
A subclass of IMIDES with the general structure of pyrrolidinedione. They are prepared by the distillation of ammonium succinate. They are sweet-tasting compounds that are used as chemical intermediates and plant growth stimulants.
Hydrocarbon rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.
Substances used for the detection, identification, analysis, etc. of chemical, biological, or pathologic processes or conditions. Indicators are substances that change in physical appearance, e.g., color, at or approaching the endpoint of a chemical titration, e.g., on the passage between acidity and alkalinity. Reagents are substances used for the detection or determination of another substance by chemical or microscopical means, especially analysis. Types of reagents are precipitants, solvents, oxidizers, reducers, fluxes, and colorimetric reagents. (From Grant & Hackh's Chemical Dictionary, 5th ed, p301, p499)
Enzymes of the oxidoreductase class that catalyze the dehydrogenation of hydroxysteroids. (From Enzyme Nomenclature, 1992) EC 1.1.-.
The unspecified form of the steroid, normally a major metabolite of TESTOSTERONE with androgenic activity. It has been implicated as a regulator of gonadotropin secretion.
Six-carbon alicyclic hydrocarbons.
An amino acid formed by cyclization of leucine. It has cytostatic, immunosuppressive and antineoplastic activities.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
Compounds that inhibit the activity of DNA TOPOISOMERASES.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
A 21-carbon steroid, derived from CHOLESTEROL and found in steroid hormone-producing tissues. Pregnenolone is the precursor to GONADAL STEROID HORMONES and the adrenal CORTICOSTEROIDS.
The class of all enzymes catalyzing oxidoreduction reactions. The substrate that is oxidized is regarded as a hydrogen donor. The systematic name is based on donor:acceptor oxidoreductase. The recommended name will be dehydrogenase, wherever this is possible; as an alternative, reductase can be used. Oxidase is only used in cases where O2 is the acceptor. (Enzyme Nomenclature, 1992, p9)
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)
Compounds containing the PhCH= radical.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.
Unsaturated pregnane derivatives containing two keto groups on side chains or ring structures.
Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.
The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
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.
A genus of toxic herbaceous Eurasian plants of the Plantaginaceae which yield cardiotonic DIGITALIS GLYCOSIDES. The most useful species are Digitalis lanata and D. purpurea.
Carrier of aroma of butter, vinegar, coffee, and other foods.
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
A group of compounds that are derivatives of oxo-pyrrolidines. A member of this group is 2-oxo pyrrolidine, which is an intermediate in the manufacture of polyvinylpyrrolidone. (From Merck Index, 11th ed)
A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed)
A broad-spectrum excitatory amino acid antagonist used as a research tool.
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.
Compounds that contain the radical R2C=N.OH derived from condensation of ALDEHYDES or KETONES with HYDROXYLAMINE. Members of this group are CHOLINESTERASE REACTIVATORS.
Unsaturated derivatives of the steroid androstane containing at least one double bond at any site in any of the rings.
Pregnadienes which have undergone ring contractions or are lacking carbon-18 or carbon-19.
A metabolite of TESTOSTERONE or ANDROSTENEDIONE with a 3-alpha-hydroxyl group and without the double bond. The 3-beta hydroxyl isomer is epiandrosterone.
Electrical responses recorded from nerve, muscle, SENSORY RECEPTOR, or area of the CENTRAL NERVOUS SYSTEM following stimulation. They range from less than a microvolt to several microvolts. The evoked potential can be auditory (EVOKED POTENTIALS, AUDITORY), somatosensory (EVOKED POTENTIALS, SOMATOSENSORY), visual (EVOKED POTENTIALS, VISUAL), or motor (EVOKED POTENTIALS, MOTOR), or other modalities that have been reported.
The major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production. Progesterone, converted from PREGNENOLONE, also serves as an intermediate in the biosynthesis of GONADAL STEROID HORMONES and adrenal CORTICOSTEROIDS.
The relationship between the dose of an administered drug and the response of the organism to the drug.
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.
That portion of the electromagnetic spectrum from the UHF (ultrahigh frequency) radio waves and extending into the INFRARED RAYS frequencies.
Chemicals with two conjoined aromatic rings incorporating two nitrogen atoms and one of the carbons oxidized with a keto oxygen.
A synthetic progestin which is useful for the study of progestin distribution and progestin tissue receptors, as it is not bound by transcortin and binds to progesterone receptors with a higher association constant than progesterone.
An estrogenic steroid produced by HORSES. It has a total of five double bonds in the A- and B-ring. High concentration of equilenin is found in the URINE of pregnant mares.
The outer layer of the woody parts of plants.
Drugs used to prevent SEIZURES or reduce their severity.
Use of electric potential or currents to elicit biological responses.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.
A microanalytical technique combining mass spectrometry and gas chromatography for the qualitative as well as quantitative determinations of compounds.
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.
A pregnane found in the urine of pregnant women and sows. It has anesthetic, hypnotic, and sedative properties.
Chemicals that are used to oxidize pigments and thus effect whitening.
The rate dynamics in chemical or physical systems.
A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN RECEPTOR AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.
A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.
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).
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.
A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.
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.
Steroids in which one or more hydroxy groups have been substituted for hydrogen atoms either within the ring skeleton or on any of the side chains.
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.
The mahogany plant family of the order Sapindales, subclass Rosidae, class Magnoliopsida.
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.
A reagent that is highly selective for the modification of arginyl residues. It is used to selectively inhibit various enzymes and acts as an energy transfer inhibitor in photophosphorylation.
A 3-hydroxysteroid dehydrogenase which catalyzes the reversible reduction of the active androgen, DIHYDROTESTOSTERONE to 5 ALPHA-ANDROSTANE-3 ALPHA,17 BETA-DIOL. It also has activity towards other 3-alpha-hydroxysteroids and on 9-, 11- and 15- hydroxyprostaglandins. The enzyme is B-specific in reference to the orientation of reduced NAD or NADPH.
The most common inhibitory neurotransmitter in the central nervous system.
The study of the structure, preparation, properties, and reactions of carbon compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
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.
5-Bromo-2'-deoxycytidine. Can be incorporated into DNA in the presence of DNA polymerase, replacing dCTP.
A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.
Catalyze the oxidation of 3-hydroxysteroids to 3-ketosteroids.
The phenomenon whereby certain chemical compounds have structures that are different although the compounds possess the same elemental composition. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Compounds based on ANTHRACENES which contain two KETONES in any position. Substitutions can be in any position except on the ketone groups.
Cell-surface proteins that bind GAMMA-AMINOBUTYRIC ACID with high affinity and trigger changes that influence the behavior of cells. GABA-A receptors control chloride channels formed by the receptor complex itself. They are blocked by bicuculline and usually have modulatory sites sensitive to benzodiazepines and barbiturates. GABA-B receptors act through G-proteins on several effector systems, are insensitive to bicuculline, and have a high affinity for L-baclofen.
A species of gram-negative, aerobic rods formerly called Pseudomonas testosteroni. It is differentiated from other Comamonas species by its ability to assimilate testosterone and to utilize phenylacetate or maleate as carbon sources.
An oral anticoagulant that interferes with the metabolism of vitamin K. It is also used in biochemical experiments as an inhibitor of reductases.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.
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.
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.
Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
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.
The rotation of linearly polarized light as it passes through various media.
A flavoprotein that reversibly catalyzes the oxidation of NADH or NADPH by various quinones and oxidation-reduction dyes. The enzyme is inhibited by dicoumarol, capsaicin, and caffeine.
A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).
Methods used for the chemical synthesis of compounds. Included under this heading are laboratory methods used to synthesize a variety of chemicals and drugs.
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.
Drugs that inhibit 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE. They are commonly used to reduce the production of DIHYDROTESTOSTERONE.
Compounds based on reduced IMIDAZOLINES which contain no double bonds in the ring.
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.
A class of organic compounds containing three ring structures, one of which is made up of more than one kind of atom, usually carbon plus another atom. The heterocycle may be either aromatic or nonaromatic
The characteristic three-dimensional shape of a molecule.
Neodymium. An element of the rare earth family of metals. It has the atomic symbol Nd, atomic number 60, and atomic weight 144.24, and is used in industrial applications.
The conformation, properties, reaction processes, and the properties of the reactions of carbon compounds.
These compounds stimulate anabolism and inhibit catabolism. They stimulate the development of muscle mass, strength, and power.
A monoamine oxidase inhibitor with antihypertensive properties.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
A group of alicyclic hydrocarbons with the general formula R-C5H9.
A potent mutagen and carcinogen. It is a public health concern because of its possible effects on industrial workers, as an environmental pollutant, an as a component of tobacco smoke.
Determination of the spectra of ultraviolet absorption by specific molecules in gases or liquids, for example Cl2, SO2, NO2, CS2, ozone, mercury vapor, and various unsaturated compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.
Enzymes that regulate the topology of DNA by actions such as breaking, relaxing, passing, and rejoining strands of DNA in cells. These enzymes are important components of the DNA replication system. They are classified by their substrate specificities. DNA TOPOISOMERASE I enzymes act on a single strand of DNA. DNA TOPOISOMERASE II enzymes act on double strands of DNA.
An enzyme that catalyzes the reduction of TESTOSTERONE to 5-ALPHA DIHYDROTESTOSTERONE.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
A class of enzymes that catalyze geometric or structural changes within a molecule to form a single product. The reactions do not involve a net change in the concentrations of compounds other than the substrate and the product.(from Dorland, 28th ed) EC 5.
Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals.
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 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.
An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.
Derivatives of the steroid androstane having two double bonds at any site in any of the rings.
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.
A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.
Medicines that can be sold legally without a DRUG PRESCRIPTION.
A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.
Spectrophotometry in the infrared region, usually for the purpose of chemical analysis through measurement of absorption spectra associated with rotational and vibrational energy levels of molecules. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
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.
Substances that inhibit or prevent the proliferation of NEOPLASMS.
Catalyzes reversibly the oxidation of hydroxyl groups of prostaglandins.
A subclass of enzymes which includes all dehydrogenases acting on primary and secondary alcohols as well as hemiacetals. They are further classified according to the acceptor which can be NAD+ or NADP+ (subclass 1.1.1), cytochrome (1.1.2), oxygen (1.1.3), quinone (1.1.5), or another acceptor (1.1.99).
The imide of phthalic acids.
A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.
A pyrrolo-quinoline having two adjacent keto-groups at the 4 and 5 positions and three acidic carboxyl groups. It is a coenzyme of some DEHYDROGENASES.
A cell line derived from cultured tumor cells.
Compounds that interact with PROGESTERONE RECEPTORS in target tissues to bring about the effects similar to those of PROGESTERONE. Primary actions of progestins, including natural and synthetic steroids, are on the UTERUS and the MAMMARY GLAND in preparation for and in maintenance of PREGNANCY.
A genus of gram-negative, aerobic, rod-shaped bacteria widely distributed in nature. Some species are pathogenic for humans, animals, and plants.
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."
Artifactual vesicles formed from the endoplasmic reticulum when cells are disrupted. They are isolated by differential centrifugation and are composed of three structural features: rough vesicles, smooth vesicles, and ribosomes. Numerous enzyme activities are associated with the microsomal fraction. (Glick, Glossary of Biochemistry and Molecular Biology, 1990; from Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed)
A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.
Large collections of small molecules (molecular weight about 600 or less), of similar or diverse nature which are used for high-throughput screening analysis of the gene function, protein interaction, cellular processing, biochemical pathways, or other chemical interactions.
A basic science concerned with the composition, structure, and properties of matter; and the reactions that occur between substances and the associated energy exchange.
THIAZOLES with two keto oxygens. Members are insulin-sensitizing agents which overcome INSULIN RESISTANCE by activation of the peroxisome proliferator activated receptor gamma (PPAR-gamma).
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.
A bacterial genus of the order ACTINOMYCETALES.
An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.
The composition, conformation, and properties of atoms and molecules, and their reaction and interaction processes.
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.
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.
A major group of unsaturated cyclic hydrocarbons containing two or more rings. The vast number of compounds of this important group, derived chiefly from petroleum and coal tar, are rather highly reactive and chemically versatile. The name is due to the strong and not unpleasant odor characteristic of most substances of this nature. (From Hawley's Condensed Chemical Dictionary, 12th ed, p96)
An enzyme that catalyzes the desaturation (aromatization) of the ring A of C19 androgens and converts them to C18 estrogens. In this process, the 19-methyl is removed. This enzyme is membrane-bound, located in the endoplasmic reticulum of estrogen-producing cells of ovaries, placenta, testes, adipose, and brain tissues. Aromatase is encoded by the CYP19 gene, and functions in complex with NADPH-FERRIHEMOPROTEIN REDUCTASE in the cytochrome P-450 system.
62 (3): 405-96. doi:10.1124/pr.109.002451. PMC 2964903. PMID 20716669. Lin JW, Ju W, Foster K, Lee SH, Ahmadian G, Wyszynski M ... 41 (6): 730-6. doi:10.1016/S0028-3908(01)00135-6. PMID 11640927. S2CID 34373607. Lester RA, Quarum ML, Parker JD, Weber E, Jahr ... 36 (6): 787-95. doi:10.1016/0042-6989(95)00176-X. PMID 8736215. S2CID 17437312. Attwell PJ, Rahman S, Ivarsson M, Yeo CH ( ... 166 (2): 157-69. doi:10.1007/s00221-005-2349-z. PMID 16082536. S2CID 2352523. Traynelis SF, Wollmuth LP, McBain CJ, Menniti FS ...
2,3,4,5-tetrahydro-8-chloro-3-methyl-5-phenyl-1h-3-benzazepin-7-ol MeSH D03.438.079.800 - 2,3,4,5-tetrahydro-7,8-dihydroxy-1- ... 5-amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazole MeSH D03.383.312.649.290 - fanft MeSH D03.383.312.649.308 - furagin MeSH ... quinolizin-2-ol, 2-ethyl-1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy- MeSH D03.438.834.775 - sparteine MeSH D03.438. ... 5-amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazole MeSH D03.383.129.462.580.400 - 4-chloro-7-nitrobenzofurazan MeSH D03.383. ...
Learn more about 6-Cyano-7-nitroquinoxaline-2,3-dione. We enable science by offering product choice, services, process ... DuPont™ Tyvek® Micro-Clean® 2-1-2 Coveralls for Controlled Environments Coated on both sides with blue polymeric resin. Sterile ...
Owens DF, Kriegstein AR (2002) Is there more to GABA than synaptic inhibition? Nature Rev Neurosci 3:715-727CrossRefGoogle ... Lanthorn TH, Ganong AH, Cotman CW (1984) 2-Amino-4-phosphonobutyrate selectively blocks mossy fiber-CA3 responses in guinea pig ... Kamiya H, Shinozaki H, Yamamoto C (1996) Activation of metabotropic glutamate receptor type 2/3 suppresses transmission at rat ...
3 C and D ). The amplitude of the Ca2+ transients in nonexpanding spines was 8.9 ± 1.3% (n = 59), similar to the 8.4 ± 1.0% ... 3 E and F ). The lack of variation and slow time course of the Ca2+ transients in the nonexpanding spines suggest that they ... 3 A and B ). The average peak Ca2+ transient in expanding spines (50.4 ± 3.8%, n = 25) was significantly greater than that in ... 2D ).. To explore why only a small fraction of spines expanded, we imaged in the same spine both expansion and postsynaptic Ca ...
3. Presynaptic manipulations including increased stimulus strength gave the predicted changes in the value of mean 2/variance ( ... On the other hand, LTP did increase M2/sigma 2, although the increase was less than that predicted for a purely presynaptic ... M2/sigma 2). Moreover, postsynaptic manipulations that altered EPSC amplitude, including blockade of non-NMDA receptors by CNQX ... 2. Presynaptic manipulations, such as activation of presynaptic gamma-aminobutyric acid-B receptors by baclofen, blockade of ...
Eur J Neurosci. 1995 Nov 1;7(11):2308-21.. Receptive field properties of starburst cholinergic amacrine cells in the rabbit ... In darkness the cells displayed a tonic inward current that could be blocked by 100 microM APB and 2 microM CNQX. ... Light responses were completely suppressed during application of 100 microM D,L-2-amino-4-phosphonobutyric acid (APB), ... 1995 Nov 1;7(11):2308-21. Research Support, Non-U.S. Govt ...
JSTX-3 also prevented motor neuron death induced by the agonist, AMPA (5 μm), although not quite as effectively as 5 μm CNQX ( ... 3. JSTX-3, an inhibitor of Ca2+-permeable AMPA receptors, prevented motor neuron death induced by both AMPA and the G93A SOD-1 ... 7. Glutathione ethyl ester failed to protect motor neurons from toxicity of G93A SOD-1. A, 1 mmglutathione ethyl ester (GSH EE ... 7 A). However, inclusion of 1 mm glutathione ethyl ester in the culture medium had no significant effect on the viability of ...
DOI: 10.1016/0896-6273(95)90178-7 Abstract Contradictory hypotheses regarding the nature of synaptic transmission in the CNS ...
While the mechanisms responsible for LTP and LTD of excitatory synaptic responses mediated by AMPA receptors (AMPARs) have been extensively characterized, much less is known about the regulation of NMDA receptors (NMDARs) by synaptic activity. In hippocampal CA1 cells, prolonged low frequency affere …
FIGURE 6. FIGURE 6. Niflumic acid did not change the ratio of IPSCs at pair-pulse stimulation. (A,B) Traces of glycinergic ... FIGURE 2. FIGURE 2. Effect of NFA on sIPSCs recorded from "neonatal" HMs. (A) Trace of continuous whole-cell recording of ... FIGURE 3. FIGURE 3. Effect of NFA on sIPSCs in "juvenile" HMs. (A) Representative traces of sIPSCs whole-cell recordings in ... Figure 2 illustrates the effect of NFA on the MN in neonatal slice (P3) at Vhold = -70 mV. Addition of NFA caused decrease in ...
2A,B). In contrast, the Ihold potentiation by EtOH (100 mm) was lost as early as 1 h after EtOH intoxication, but gradually ... 7C). At 1 h after a single EtOH dose, DZ potentiation of Itonic was unaffected, but maximal decreases occurred at 2 d after ... Figure 7. Time course of changes in diazepam sensitivity of synaptic and tonic GABAAR-currents after EtOH treatment. A, Traces ... Figure 2. Changes in acute EtOH sensitivity of synaptic and tonic GABAAR-currents after EtOH intoxication. A, Traces are ...
ς2. variance. pS. picosiemens. TTX. tetrodotoxin. VR. reversal potential of the agonist response. VH. membrane holding ... α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid. CNQX. 6-cyano-7-nitroquinoxaline-2,3-dione. cGMP. 3′,5′ cyclic guanosine ... 3′,5′ cyclic 8-bromo-guanosine monophosphate. FUDR. the mitotic inhibitors 5-fluoro-2′-deoxyuridine and uridine. LTD. long-term ... 2) The shape of kainate current-voltage (I-V) curves and their reversal potentials were unchanged in cGMP. 3) Neither the ...
6-cyano-7-nitroquinoxaline-2,3-dione. KAT II. kynurenine aminotransferase II. K-S. Kolmogorov-Smirnov. KYNA. kynurenic acid. ... 2 and 3) may be caused by the ability of MLA to block some heteromeric α7 or non-α7 nAChRs. The α7 nAChR currents in ... 2, B and C).. The frequency of GABAergic PSCs was also significantly lower in slices that had been incubated for 1 h in ACSF ... 7. Effect of the admixture of kynurenine and α-BGT on the frequency of PSCs. A, mean frequency of PSCs recorded 1) after 1-h ...
... scanning photostimulation revealed that NCAM deletion increased the strength of close-in inhibitory connections to layer 2/3 ... scanning photostimulation revealed that NCAM deletion increased the strength of close-in inhibitory connections to layer 2/3 ... 2. *. (. 1. −. exp. (. −. (. I. −. I. break. ). /. I. rate. ). ). +. (. F. 0. +. F. 1. ). (. 1. ). ... FIGURE 2. Figure 2. Comparisons of firing rates of interneurons between wild type (WT) and NCAM-null mice in ACC. (A) ...
3G). Notably, the A/N ratio of naïve neurons before TBS was larger in Mecp2 KO neurons (WT n = 11/5 and Mecp2-/y n = 13/7; P = ... 7C). On the other hand, spine volume did not change after TBS in Mecp2 KO neurons (Mecp2-/y Ctl n = 862/32/7/3 and Mecp2-/y TBS ... 2 E and F and Fig. S2 A and B). The intensity of individual GluA1 puncta in the dendritic and somatic layers of area CA1 and ... 3 C and E, Bottom). Because naïve Mecp2 KO slices showed a steeper I-O of EPSC amplitude (Fig. 1C), we monitored the change of ...
6, C and D). The EC50 for increased SCOs frequency was 2.33 μM (1.30-4.18 μM, 95% CI), and the IC50 value for 4-AP attenuation ... 6A, traces 3-6) with an EC50 of 1.76 μM (1.21 to 2.54 μM; 95% CI). Unlike either kainate or pilocarpine, 4-AP produced a long- ... 6-cyano-7-nitroquinoxaline-2,3-dione. DIV. days in vitro. FLIPR. fluorescent imaging plate reader. FWHM. full width at half ... 6. 4-AP alters Ca2+ dynamics and SCO in 10 DIV HN cultures. (A) Representative traces of 4-AP-triggered Ca2+ responses in HN ...
2003 Sep;6(5):648-57. View Article. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3 ... 1996 Feb;49(2):311-8. View Article. Luna-Tortos C, Fedrowitz M, Loscher W: Several major antiepileptic drugs are substrates for ... 2005 Oct;6(5):451-72. View Article. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell ... 2005 Oct;6(5):451-72. View Article. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell ...
Kemp, J.A., Foster, A.C., Leeson,P.D., Priestley, T., Tridgett, R., Iversen, L.L. and Woodruff, G.N. (1988). 7-Chlorokynurenic ... Harris, M.K and Miller, J.R. (1989). CNQX (6-cyano-7-nitroquinoxalone-2,3-elione) antagonizes NMDA-evoked (3H)GABA release from ... Neuman, R.S., Ben-Ari, Y., Gho, M. and Cherubini, E. (1988a). Blockage of excitatory synaptic transmission by 6-cyano-7- ... nitroquinoxaline-2,3-dione (CNQX) in the hippocampus in vitro. Neurosci. Lett. 92, 64-68.PubMedCrossRefGoogle Scholar ...
2.Center for Computational ScienceUniversity of MiamiCoral GablesUSA. *3.Department of Computer ScienceUniversity of MiamiCoral ... 2). This is a unique feature of NMDAR: they are the only iGluR subtype with more than one orthologous copy present before the ... 2).. Within vertebrates there are two ancient paralogs with a total of five kainate genes. The three paralogs GRIK_A1-3 form ... 3 Conserved motifs in Aplysia and H. sapiens. Boxed region denotes SYTANLAAFL motif vital for formation of the channel pore and ...
ABBREVIATIONS: ACSF, artificial cerebrospinal fluid, APV, dl-2-amino-5-phosphonopentanoic acid; CNQX, 6-cyano-7- ... nitroquinoxaline-2,3-dione; IPSC, inhibitory postsynaptic current; mIPSC, miniature inhibitory postsynaptic current; sIPSC, ... Molecular Pharmacology September 1, 2007, 72 (3) 780-787; DOI: ... Molecular Pharmacology September 1, 2007, 72 (3) 780-787; DOI: ...
Data are shown as the mean ± SEM (hM3Dq: n = 6 mice; mCherry: n = 4 mice). *p,0.05, ***p,0.001, (d) two-way ANOVA followed by ... c) Summary of experiments in (b). Blue light 5 Hz (n = 7 cells), 10 Hz (n = 8 cells), 20 Hz (n = 9 cells), and yellow light 20 ... Blue light stimulation of 6.8 mW/mm2 increased the firing up to 674 ± 174% (n = 5 cells, p=0.004 vs both pre and post, one-way ... DAPI (4′,6-diamidino-2-phenylindole) staining was used to label nuclear DNA and also to assist understanding of the anatomical ...
62 (3): 405-96. doi:10.1124/pr.109.002451. PMC 2964903. PMID 20716669. Lin JW, Ju W, Foster K, Lee SH, Ahmadian G, Wyszynski M ... 41 (6): 730-6. doi:10.1016/S0028-3908(01)00135-6. PMID 11640927. S2CID 34373607. Lester RA, Quarum ML, Parker JD, Weber E, Jahr ... 36 (6): 787-95. doi:10.1016/0042-6989(95)00176-X. PMID 8736215. S2CID 17437312. Attwell PJ, Rahman S, Ivarsson M, Yeo CH ( ... 166 (2): 157-69. doi:10.1007/s00221-005-2349-z. PMID 16082536. S2CID 2352523. Traynelis SF, Wollmuth LP, McBain CJ, Menniti FS ...
... cyano7nitroquinoxaline2,3dione (CNQX; 20 microMs), and kynurenate (1mM) had no effect on the glutamate‐evoked current. 8. ... dione (CNQX; 20 microMs), and kynurenate (1mM) had no effect on the glutamate‐evoked current. 8. The voltage dependence, cation ... nitroquinoxaline2,3‐ ... 2. L‐Glutamate evoked an inward current at membrane potentials ... 2. L‐Glutamate evoked an inward current at membrane potentials between ‐140 and +50 mV. The current was larger at more negative ...
7. The rise time for the NMDA component was 8-20 ms and the time constant for decay ranged from 60-150 ms. 8. During increased ... 6. For those synapses that were close to the soma the time constant for decay for the non-NMDA component, which was voltage ... 3. The voltage-dependent component was abolished by the N-methyl-D-aspartate (NMDA) receptor antagonist DL-2-amino-5- ... 2. Excitatory postsynaptic currents (EPSCs) had a fast component whose amplitude was voltage insensitive and a slow component ...
AUDITORY AND VISUAL MAPS OF SPACE IN THE OPTIC TECTUM OF THE OWL JOURNAL OF NEUROSCIENCE Knudsen, E. I. 1982; 2 (9): 1177-1194 ... THE HEARING OF THE BARN OWL SCIENTIFIC AMERICAN Knudsen, E. I. 1981; 245 (6): 113-? View details for Web of Science ID ... SUPERVISED LEARNING IN THE BRAIN JOURNAL OF NEUROSCIENCE Knudsen, E. I. 1994; 14 (7): 3985-3997 View details for Web of Science ... Selective attention in birds. Current biology Sridharan, D., Schwarz, J. S., Knudsen, E. I. 2014; 24 (11): R510-3 Abstract. The ...
Controlling brain states. Neuron Bennett, C., Arroyo, S., Hestrin, S. 2014; 83 (2): 260-261 Abstract. Neurons in mouse V1 ... Layer 6 corticothalamic neurons activate a cortical output layer, layer 5a. journal of neuroscience Kim, J., Matney, C. J., ... 6. No shift of the tau K-V and the gK-V relations was observed when the internal potassium was reduced from 150 to 50 mM. 7. ... In layer 5/6 (L5/6), we recorded from two or three FS and/or pyramidal (PYR) neurons to study the development of electrical and ...
Abbreviations: CNQX, 6-cyano-7-nitroquinoxaline-2, 3-dione; DMSO, dimethyl sulfoxide; PBS, phosphate buffered saline; EPSP, ... Would the Department of Finance consider expanding the exclusion in subsection 47(3) so that shares acquired from either an ... Abbreviations: AC, adenylate cyclase; AMPA, a-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate; AP, action potential; CaM, ...
8-Hydroxy-2-(di-n-propylamino)-tetralin inhibits food intake in fasted rats by an action at 5-HT1A ... ... Efforts to address the food effect issue led us to explore and discover compounds in series 2 as orally active CRF 1 receptor ... A molecular form known as chicken GnRH II ([His(5) Trp(7) Tyr(8)] GnRH, cGnRH II) is widely distributed in vertebrates, and has ... The effects of the 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) on food intake were investigated in food- ...
View ORCID ProfileCarlos B. Duarte1,7,*. *. 1CNC-Center for Neuroscience and Cell Biology, University of Coimbra, 3004-504 ... 6 BDNF-induced increase in synaptic expression of GluN2B-containing NMDAR is mediated by activation of Pyk2.. (A to C) ... 3, C and D), as well as in the respective diffusion coefficient (Fig. 3, E and F). Together, the observed alterations in the ... Plasmids (2 μg per coverslip) were diluted in tris-EDTA transfection buffer [10 mM tris-HCl and 2.5 mM EDTA (pH 7.3)], and a ...
Figure 6shows that neither intrathecal administration of NMDA or non-NMDA receptor antagonists nor local application of aCSF to ... Figure 2. Time-course changes in root mean square (RMS) and mean power frequency (MPF) values of electromyographic signals ... Figure 2. Time-course changes in root mean square (RMS) and mean power frequency (MPF) values of electromyographic signals ... Figure 3. Time-course changes in root mean square (RMS) and mean power frequency (MPF) values of electromyographic signals ...
... dione (CNQX; Sigma-Aldrich Japan), tetrodotoxin (TTX; Wako, Osaka, Japan), and N-methyl-DL-aspartic acid (NMDA; Wako). APB was ... dione (CNQX), tetrodotoxin (TTX), and N-methyl-DL-aspartic acid (NMDA) were injected intravitreally. Digital subtraction of the ... Figure 3. Comparisons of the amplitudes of ON-component and OFF-component between WT and Tg rabbits at 18 months of age. ON- ... Figure 3. Comparisons of the amplitudes of ON-component and OFF-component between WT and Tg rabbits at 18 months of age. ON- ...
  • However, recruitment of additional synaptic release sites by increasing stimulus strength and antagonism of non-N-methyl-D-aspartate (NMDA) glutamate receptors by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) failed to alter PPF. (
  • Moreover, postsynaptic manipulations that altered EPSC amplitude, including blockade of non-NMDA receptors by CNQX, or changing the holding potential of the postsynaptic cell, gave little change in M2/sigma 2, as would be predicted for manipulations resulting in a uniform postsynaptic change. (
  • In darkness the cells displayed a tonic inward current that could be blocked by 100 microM APB and 2 microM CNQX. (
  • KAR competitive antagonist CNQX [6-cyano-7-nitroquinoxaline-2,3-dione] (1-10 µ M) normalized Ca 2+ dynamics to the prekainate pattern. (
  • CNQX (6-cyano-7-nitroquinoxalone-2,3-elione) antagonizes NMDA-evoked (3H)GABA release from cultured cortical neurons via an inhibitory action at the strychnine-insensitive glycine site. (
  • CNQX or cyanquixaline (6-cyano-7-nitroquinoxaline-2,3-dione) is a competitive AMPA/kainate receptor antagonist. (
  • CNQX is an antagonist of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptors (AMPARs). (
  • Furthermore, D-AP5 and 7-CIK did not affect the frequency of spontaneous inhibitory postsynaptic currents, proving that the action of NMDA receptors do not account for the effects of CNQX. (
  • To block different retinal pathways, 2-amino-4-phosphonobutyric acid (APB), 6-cyano-7-nitroquinoxaline-2, 3 (1H,4H)-dione (CNQX), tetrodotoxin (TTX), and N-methyl-DL-aspartic acid (NMDA) were injected intravitreally. (
  • The available AMPA antagonistic compounds such as 6-cyano-7-nitroquinoxaline-2, 3-dione (CNQX) , 6, 7-dinitroquinoxalone-2, 3-dione (DNQX) , or earlier compounds such as glutamic acid diethyl ester (GDEE) had very little antagonist activity in vivo due to their lack of affinity. (
  • However, microinjection of 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX, a selective AMPA/kainate receptor antagonist, 2 mM, 100 nl) into the RVLM after intravenous MK-801 abolished the hypoxia evoked sympathoexcitatory response. (
  • Validation of the synaptic processes was achieved with the use of the synaptic blockers 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and 2-amino-5-phosphonovaleric acid (APV). (
  • Riluzole also attenuated nonexcitotoxic oxidative injury induced by exposure to FeCl 3 in the presence of MK-801 and CNQX. (
  • A non-NMDA glutamate receptor antagonist, 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), reduced vestibular CAPs significantly but only at the highest concentration tested (1 mM). (
  • Blockade of excitatory synaptic transmission by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) in the hippocampus in vitro. (
  • European Journal of Pharmacology , 557 (2-3), 106-114. (
  • 6-Cyano-7-nitroquinoxaline-2,3-dione--pharmacology;Analysis of Variance;Behavior, Addictive--physiopathology;Conditioning, Operant--drug effects;Cues;Dopamine Antagonists--pharmacology;Dose-Response Relationship, Drug;Excitatory Amino Acid. (
  • The high concentration of actin in dendritic spines led to the proposal that activity-dependent changes in spine shape could modify synaptic efficacy ( 6 , 7 ). (
  • Several mechanisms have been proposed to underlie these deficits, including altered composition of synaptic NMDA receptors, sparse connectivity through weak synapses, and LTP saturation ( 6 , 10 , 11 ). (
  • Experience-dependent synaptic plasticity is a fundamental feature of neural networks involved in storing information [1] - [3] . (
  • The importance of inhibitory inputs to PVN neurons is highlighted by anatomical data, which show that ∼50% of all synaptic connections made in the PVN are GABAergic in nature ( 7 ) and serve to mediate peripheral cardiovascular- and energy balance-related signals to this hypothalamic nucleus ( 27 , 31 ). (
  • The blockade of glutamatergic excitatory synaptic transmission by preincubation of the slices with the amino-3-hydroxy-5-methyl-4-isoxazolpropionic acid receptor antagonist 6-cyano-7-nitroquinoxaline-2,3-dione (10 μM), but not with theN-methyl-d-aspartate receptor antagonistd-2-amino-5-phosphonovaleric acid (50/μM), prevented the induction of epileptiform activity by 1,3-dipropyl-8-cyclopentylxanthine. (
  • 3 4 5 These α-Bgtx-sensitive nicotinic receptors have a high permeability to calcium and have been shown to enhance synaptic transmission via presynaptic mechanisms. (
  • also known as Arg3.1) is an immediate early gene (IEG) that is rapidly induced in the brain by synaptic activity ( 6 , 7 ). (
  • Facing the cytoplasmic aspect of the CAZ are numerous synaptic vesicles that are enmeshed in a fine matrix of proteins comprised primarily of microfilaments and the synaptic vesicle-associated protein Synapsin, which are thought to hold them together and keep them at the presynaptic region [5,6]. (
  • Conversely, uridine (at all concentrations tested) had a negligible effect on PPF and basal synaptic transmission, which is mediated primarily by α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs). (
  • Synaptic response mediated by the N-methyl-D-aspartate (NMDA) receptor (EPSPnmda) was isolated pharmacologically by application of a solution containing non-NMDA receptor antagonist 6-cyano-7-nitroquinoxaline-2,3-dione (10 μmol/l) and γ-aminobutyric acid A receptor antagonist bicuculline (20 μmol/l). (
  • Using patch clamp recordings in acute slices, we examined the effects of the ACh receptor (AChR) agonist carbachol on the excitatory synaptic drive onto BCs or ChCs in layers 2 to 6 of mouse PFC. (
  • The effects of extracellularly applied 3′-5′ cyclic guanosine monophosphate (cGMP) on kainate responses from cultured cerebellar granule and Purkinje neurons were investigated using whole-cell and outside-out patch recording modes. (
  • Using the methyl-CpG-binding protein 2 (Mecp2) knockout (KO) mouse model of Rett syndrome, we show that naïve excitatory synapses onto hippocampal pyramidal neurons of symptomatic mice have all of the hallmarks of potentiated synapses. (
  • Layer 6 corticothalamic neurons activate a cortical output layer, layer 5a. (
  • Layer 6 corticothalamic neurons are thought to modulate incoming sensory information via their intracortical axons targeting the major thalamorecipient layer of the neocortex, layer 4, and via their long-range feedback projections to primary sensory thalamic nuclei. (
  • However, anatomical reconstructions of individual layer 6 corticothalamic (L6 CT) neurons include examples with axonal processes ramifying within layer 5, and the relative input of the overall population of L6 CT neurons to layers 4 and 5 is not well understood. (
  • 3 Usually, remodeling in RP eyes has features that take place earlier and more severely among cells directly connected to the photoreceptors, that is, bipolar cells, and less severely on the other inner retinal neurons. (
  • Under current-clamp conditions, NPVF and NPFF caused depolarization (6-9 mV) of neurons that persisted in the presence of TTX but was abolished in the presence of bicuculline. (
  • In the brain, NPFF has been shown to influence the secretion of vasopressin from the hypothalamus and activate neurons of cardiovascular centers in the brain stem that regulate sympathetic autonomic outflow ( 2 , 16 ). (
  • The PVN is a bilateral periventricular structure in the hypothalamus that contains separate populations of neurons that 1 ) regulate the secretion of hormones from the posterior pituitary (magnocellular neurons), 2 ) project to the median eminence to control adenohypophyseal hormone release (parvocellular neurons), and 3 ) send projections to the caudal brain stem and spinal cord autonomic centers for control of sympathetic outflow (parvocellular neurons) ( 36 ). (
  • Activation or suppression of single PV neurons modified visual responses of postsynaptic Pyr cells in 6 of 7 pairs whereas that of single SOM neurons showed no significant modification in 8 of 11 pairs, suggesting that PV neurons can act solo whereas most of SOM neurons may act in chorus on Pyr cells. (
  • The activation/inactivation of single PV neurons modified visual responses of postsynaptic Pyr cells in 6 of the 7 pairs whereas that of single SOM neurons did not induce such a modification in 8 of the 11 pairs, suggesting that the operation mode of the two major subtypes of interneurons is different. (
  • Initially we analyzed inhibitory postsynaptic currents (IPSCs) of Pyr cells evoked by action potentials of presynaptic PV or SOM neurons in vivo in layer 2/3 of the visual cortex of mice in which each subtype of interneurons expressed channelrhodopsin-2 (ChR2). (
  • Low conductance would facilitate the contribution of the intrinsic response properties of postsynaptic neurons to cell and network dynamics ( 6 - 9 ). (
  • 5-HT 1B receptors play a crucial role in regulating serotonin neurotransmission, as they serve as both autoreceptors on serotonin-containing neurons originating from the raphe nuclei and heteroreceptors on several neurons that do not contain serotonin ( 6 , 7 ). (
  • The present study demonstrates that nicotine has at least 3 sites of action to increase the activity of vagal cardiac neurons. (
  • In rats (6 to 12 days old), the heart was exposed in an initial surgery with a right thoracotomy, and rhodamine (XRITC, Molecular Probes) was injected into the pericardial sac and applied to the terminals of preganglionic parasympathetic cardiac neurons located mostly in the fat pads at the base of the heart. (
  • This released glutamate activates ionotropic glutamate receptors such as α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid and N -methyl-d-aspartate (NMDA) receptors in the postsynaptic membrane of the DH neurons, causing membrane depolarization and the firing of action potentials. (
  • These results indicate that transplantation of X-box-binding protein 1-transfected neural stem cells can promote stem cell survival and differentiation into dopaminergic neurons, increase dopamine and 3,4-dihydroxyphenylacetic acid levels, reduce α-synuclein aggregation in the substantia nigra, and improve the symptoms of Parkinson's disease in rats. (
  • A single pulse delivered to the VPM via bipolar electrode induced an EPSC with short latency (2 ms), as well as EPSCs with long latency (120 ms) in the cortical neurons. (
  • Using the fluorescent dye 2',7'-dichlorodihydrofluorescein (DCF-H2) we investigated the role of glutamate in the production of reactive oxygen species (ROS) in cultured neurons from fetal rat forebrain. (
  • p = 0.0007), but not in non-dopaminergic neurons (2 ± 4% inhibition). (
  • 2. Presynaptic manipulations, such as activation of presynaptic gamma-aminobutyric acid-B receptors by baclofen, blockade of presynaptic adenosine receptors by theophylline, blockade of presynaptic potassium channels by cesium, and increasing the Ca(2+)-Mg2+ ratio in the external recording solution, each reliably changed PPF in a fashion reciprocal to the change in the EPSC amplitude. (
  • During learning, two subtypes of iGluR, α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPAR) and N-methyl-D-aspartate receptors (NMDAR), are dynamically regulated postsynaptically in vertebrates. (
  • 5 , 6 On the other hand, glutamate activates the depolarizing kainate/AMPA-type ionotropic receptors (iGluR) on OFF-cone bipolar cells. (
  • In this study, we examined the possible involvement of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)/kainate receptors in the RVLM on sympathetic chemoreceptor reflex in pentobarbitone anaesthetised, vagotomised and artificially ventilated rats. (
  • For NPFF and related peptides, two G protein-coupled receptors, designated NPFF1 and NPFF2, have been identified in human and rat central nervous system (CNS) tissues ( 6 , 39 ). (
  • Third, the hypothalamic PVN is enriched in NPFF binding sites and receptors ( 6 , 11 ). (
  • The effects on brain function of drugs acting on GABA A receptors show that it is not necessary to silence a cell type to alter network properties or behavior: a modest modulation of inhibitory postsynaptic currents (IPSCs) is sufficient 6 - 8 . (
  • The ability of alpha4beta2 nicotinic acetylcholine receptors to modulate dopaminergic (DA) cell activity in the ventral tegmental area (VTA) in rat midbrain slices was assessed using a selective alpha4beta2 receptor agonist, TC-2559 ((E)-N-methyl-4-[3-(5-ethoxypyridin)y1]-3-buten-1-amine). (
  • The selectivity of TC-2559 was characterized across 6 recombinant human nicotinic receptors (alpha4beta2, alpha2beta4, alpha4beta4, alpha3beta4, alpha3beta2 and alpha7) stably expressed in mammalian cell lines. (
  • Glutamate receptor antagonists (6-cyano-7-nitroquinoxaline-2,3-dione and D(-)-2-amino-5-phosphonopentanoic acid) did not reduce TC-2559-induced responses, suggesting that the increase in DA cell firing induced by TC-2559 is caused by direct postsynaptic depolarisation via the activation of alpha4beta2 receptors and not by enhancement of glutamate release. (
  • There are 14 different serotonin receptors ( 2 ), some of which have multiple splice variants that enable binding of distinct sets of intracellular proteins ( 5 ). (
  • Pharmacologic and genetic studies have suggested a role for 5-HT 1B receptors in the pathophysiology of obsessive compulsive disorder, drug addiction, depression, anxiety, aggression, and sleep ( 1 , 7 , 8 ). (
  • p11 interacted with 5-HT 1B receptors, but not with 5-HT 1A , 5-HT 2A , 5-HT 5A , 5-HT 6 , dopamine D 1 or D 2 receptors, two irrelevant baits (CΔ115 and pRP21), or the empty plasmid, which showed the specificity of this interaction ( Fig. 1A ). (
  • 2 Some of these nicotinic receptors, especially those that contain the α7 gene product, which are selectively blocked by α-bungarotoxin (α-Bgtx), are preferentially localized, and clustered, at presynaptic sites. (
  • Although MOR internalization has been thought to play a role in acute opioid tolerance, 3 the exposure of MORs to morphine does not cause internalization and down-regulation of these receptors, as occurs with other more potent and selective μ-opioid agonists. (
  • 4-6 Prolonged MOR activation results in desensitization of the receptors through G-protein uncoupling and subsequent neuronal excitation. (
  • 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]. (
  • The role of (+/-)-alpha-amino-3-hydroxy-5-methyl-isoxazole-4-propionic acid (AMPA)-kainate and N-methyl-D-aspartate (NMDA) receptors in the rostral ventrolateral medulla (RVLM) and caudal ventrolateral medulla (CVLM) on the central respiratory drive (CRD)-related activity of splanchnic sympathetic nerve activity (SNA) was examined in rats. (
  • 3. At agonist concentrations less than or equal to 1 mM, kainate receptors, with a 20-pS conductance, did not desensitize. (
  • At kainate concentrations greater than or equal to 1 mM, though, kainate receptors desensitized to a low steady-state conductance within approximately 200 ms. Resensitization of all channels required as long as 3 s, which could render kainate receptors inexcitable during high-frequency activation. (
  • These responses were prevented by 6-cyano-7-nitroquinoxaline-2,3-dione, a selective antagonist for non-N-methyl-D-aspartate receptors, by L-type Ca 2+ channel blockers such as nifedipine, or by omitting Ca 2+ or Na + in the medium. (
  • Nucleus Accumbens;Cocaine;Receptors, AMPA;Cocaine-Related Disorders;Dopamine;Glutamic Acid;alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid;Drug-Seeking Behavior;Craving;Microinjections;Dopamine Antagonists;Receptors, Glutamate;Excitatory. (
  • 2-Hydroxy-saclofen: an improved antagonist at central and peripheral GABAB receptors. (
  • SHANK3 is a protein in the core of the postsynaptic density (PSD) and has a critical role in recruiting many key functional elements to the PSD and to the synapse, including components of α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionic acid (AMPA), metabotropic glutamate (mGlu) and N -methyl-D-aspartic acid (NMDA) glutamate receptors, as well as cytoskeletal elements. (
  • GKAP is a PSD-95-binding protein that forms an important component of the postsynaptic density (PSD), where protein-protein interactions between scaffolding proteins and receptors are a key mechanism in assembling a functional synapse [ 2 ]. (
  • GKAP mediates the binding of Shanks to N -methyl-D-aspartic acid (NMDA) and α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionic acid (AMPA) receptors [ 8 ]. (
  • In this study, we showed that δ-cells express GluR4c-flip, a newly identified splicing variant of GluR4, an (RS)-α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type ionotropic glutamate receptor of rat. (
  • In consequence, AMPA-R antagonists have been reported to be effective in the therapy of neurodegenerative disorders such as ischemic stroke, epilepsy, head trauma, and Alzheimer's disease [ 6 , 7 ]. (
  • In the literature are described different series of AMPA receptor antagonistic, one of which is based on the quinoxaline-2, 3-dione structure, which have high affinity and selectivity. (
  • The effects of NMDA and α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) on endogenous acetylcholine release from rat striatal slices and synaptosomes were investigated. (
  • Tetrodotoxin (0.5 μM) prevented the facilitatory effect of 3 μM NMDA and AMPA, but left unchanged that of 30 μM NMDA and 100 μM AMPA. (
  • In addition, the AMPA selective quinoxalinedione, 2,3-dihydroxy-6-nitro-7-sulfamoylbenzo (F) quinoxaline (NBQX) has been shown to be neuroprotective in cerebral ischemia models [31]. (
  • Glutamate (1 mM) as well as α-amino-3-hydroxy-5- methyl-4-isoxazole propionic acid (AMPA), a glutamate agonist, significantly reduced auditory CAPs (AMPA EC 50 =100 μM). (
  • 2. L‐Glutamate evoked an inward current at membrane potentials between ‐140 and +50 mV. (
  • 3. The glutamate‐evoked current was activated by external cations with relative efficacies: Na+ much greater than Li+ greater than K+ greater than Cs+, choline. (
  • 6. The uptake blocker threo‐3‐hydroxy‐DL‐aspartate (30 microM) reduced the glutamate‐evoked current, but also generated a current itself. (
  • 9. In addition to glutamate, the uptake carrier can also transport aspartate and threo‐3‐hydroxy‐DL‐aspartate, but not dihydrokainate. (
  • 10,11 ] Similarly, glutamate-like immunoreactivity [ 12 ] and NMDA, kainate, and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid binding sites [ 13 ] are present in the dorsal and ventral horn of the spinal cord. (
  • The glutamate-dependent somatostatin secretion was Ca2+ dependent and blocked by 6-cyano-7-nitroquinoxaline-2,3-dione. (
  • The "L-MAN" EPSPs were blocked by the N-methyl-D-aspartate (NMDA) receptor antagonist D-(-)-2-amino-5-phosphonovaleric acid (D-APV) as well as the broad-spectrum glutamate receptor antagonist kynurenic acid but were relatively unaffected by the non-NMDA receptor blocker 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX). (
  • Pretreatment with the glutamate receptor antagonists (DL-2-amino-5-phosphonovaleric acid and 6-cyano-7-nitroquinoxaline-2,3-dione disodium) also did not alter phase shifts to NPY. (
  • 2. Long burst activities were elicited by 4-aminopyridine in the presence of ionotropic glutamate receptor and GABAA receptor blockers (6-cyano-7-nitroquinoxaline-2,3-dione and 3-(RS-2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid, and picrotoxin). (
  • Similarly, kynurenic acid (4-hydroxyquinoline-2- carboxylic acid, 1 mM), a glutamate antagonist, significantly reduced auditory but not vestibular CAPs. (
  • In the presence of Ca 2+ and Na + , (RS)-α-amino-3-hydroxy-5-methyl- 4-isoxazolepropionic acid or kainate evoked glutamate secretion from the cultured cells, which was prevented by 6-cyano-7-nitroquinoxaline-2,3-dione, L-type Ca 2+ channel blockers, type E or B botulinum neurotoxin, or incubation at 2+ channels. (
  • 5. The late EPSCs in granule cells from fluid percussion-injured rats were not blocked by the NMDA receptor antagonist 2-amino-5-phosphonovaleric acid (APV), but were eliminated by both the non-NMDA glutamate receptor antagonist 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and the AMPA receptor antagonist GYKI 53655. (
  • The addition of an excitotoxic concentration of glutamate (100 microM) produced a generalized decrease in cellular DCF fluorescence accompanied by local areas of increased fluorescence around the margins of the cell body that could be observed within 2-4 min of glutamate exposure. (
  • Light responses were completely suppressed during application of 100 microM D,L-2-amino-4-phosphonobutyric acid (APB), consistent with activation exclusively through rod bipolar cells (on) and ON-cone bipolar cells. (
  • Quinoxaline-2, 3-dione obtained from cyclocondensation reaction of o-phenylene diamine with oxalic acid was reacted with three different ketones and formaldehyde to give the corresponding Mannich bases in satisfactory yield. (
  • Thus, cyclocondensation of o-phenylene diamine (1) with oxalic acid in presence of hydrochloric acid afforded quinoxaline 2, 3-dione (2) by both conventional and microwave irradiation method. (
  • A rabbit model of traumatic optic nerve injury, established by occlusion of the optic nerve using a vascular clamp, was used to investigate the effects of alpha-amino-3-hydroxy-5-methyl-4- isoxazolepropionic acid receptor antagonist GYKI 52466 on apoptosis of retinal ganglion cells following nerve injury. (
  • The results demonstrate that following acute optic nerve injury, apoptosis of retinal ganglion cells is a programmed process, which can be inhibited by the alpha-amino-3-hydroxy-5-methyl-4- isoxazolepropionic acid receptor antagonist. (
  • Moreover, dopamine and 3,4-dihydroxyphenylacetic acid levels in the substantia nigra were significantly increased, α-synuclein expression was decreased, and neurological behaviors were significantly ameliorated in rats following transplantation of X-box-binding protein 1-transfected neural stem cells. (
  • Consistent with this observation, the presence of (RS)-α-amino-3-hydroxy-5-methyl-4- isoxazolepropionic acid or kainate, non-N-methyl-D-aspartate receptor agonists, transiently stimulated increased the intracellular Ca 2+ concentration of cultured pinealocytes, whereas N-methyl-D-aspartate did not. (
  • Taurine (2-amino-ethane sulfonic acid) is one of the most plentiful free amino-acids in humans [ 1 , 2 ]. (
  • Bath application of the highly selective adenosine A1 receptor antagonist 1,3-dipropyl-8-cyclopentylxanthine at concentrations up to 100 nM induced both spontaneous and stimulus-evoked epileptiform burst discharges. (
  • The effect of TC-2559 was blocked by 2 microM dihydro-beta-erythroidine (an alpha4beta2-preferring antagonist), but not by 10 nM methyllycaconitine (an alpha7 antagonist). (
  • This study investigated the effects of daily intraperitoneal injections of N-methyl-D-aspartate receptor antagonist MK-801 and nitric oxide synthase inhibitor nitro-L-arginine (L-NA) on the survival of retinal ganglion cells (RGCs) at 1 and 2 weeks after unilateral optic nerve transection in adult hamsters. (
  • 3. Dentate granule cells following trauma showed enhanced action potential discharges, and longer-lasting depolarizations, in response to perforant path stimulation, in the presence of the GABAA receptor antagonist bicuculline. (
  • The potentiation of sEPSCs in layers 3-6 BCs was prevented by the Na + channel blocker tetrodotoxin and was abolished by the M1-selective muscarinic AChR antagonist pirenzepine. (
  • 6. For those synapses that were close to the soma the time constant for decay for the non-NMDA component, which was voltage insensitive, ranged from 4-8 ms. 7. (
  • Carotid chemoreceptor stimulation with brief N2 inhalation increased splanchnic sympathetic nerve activity and arterial pressure in animals that had received an intravenous injection of the non-competitive NMDA receptor blocker, MK-801 (2 mg/kg). (
  • 6,7-Dinitro-quinoxaline-2,3-dion and 6-nitro,7-cyano-quinoxaline-2,3-dion antagonise responses to NMDA in the rat spinal cord via an action at the strychnine-insensitive glycine receptor. (
  • 3. Presynaptic manipulations including increased stimulus strength gave the predicted changes in the value of mean 2/variance (M2/sigma 2). (
  • On the other hand, LTP did increase M2/sigma 2, although the increase was less than that predicted for a purely presynaptic mechanism. (
  • The plastic GABA A R changes were gradually and fully reversible by 2 weeks after single EtOH dosing, but unexplainably persisted long after withdrawal from chronic intermittent ethanol treatment, which leads to signs of alcohol dependence. (
  • doi: 10.1016/0896-6273(95)90178-7. (
  • Irons-Brown, SR & Jones, TA 2004, ' Effects of selected pharmacological agents on avian auditory and vestibular compound action potentials ', Hearing Research , vol. 195, no. 1-2, pp. 54-66. (
  • Long-term potentiation (LTP), a cellular correlate of learning and memory ( 5 ), is impaired at hippocampal CA1 excitatory synapses of symptomatic Mecp2 knockout (KO) mice ( 6 , 7 ), mice that express nonfunctional MeCP2 ( Mecp2 308 ) ( 8 ), and mice with a STOP codon before Mecp2 exon 3 ( Mecp2 stop ) ( 9 , 10 ). (
  • Quinoxaline-2, 3-dione derivatives are important classes of nitrogen-containing heterocycles, as they constitute useful intermediates in organic synthesis [ 1 ]. (
  • Since these compounds are based on quinoxaline-2, 3-dione, we were planning to synthesize some novel quinoxaline dione derivatives and to evaluate their antagonistic action through neuroprotection. (
  • There is also morphological evidence that hippocampal slices undergo a spontaneous and rapid increase in synapses within 2 hr after slicing [13] . (
  • Taurine-mediated responses were partially blocked by picrotoxin (50 μ M) and almost completely blocked by strychnine (2 μ M), suggesting that taurine-mediated responses are via glycine receptor (GlyR) activation. (
  • 2. The percentage decrease in the number of hilar interneurones labelled with either GAD67 or parvalbumin mRNA probes following trauma was not different from the decrease in the total population of hilar cells, indicating no preferential survival of interneurones with respect to the non-GABAergic hilar cells, i.e. the mossy cells. (
  • 2003), The nicotinic alpha 4 beta 2 receptor selective. (
  • The nicotinic alpha 4 beta 2 receptor selective agonist, TC -2559, increases dopamine neuronal activity in the ventral tegmental area of rat midbrain slices. (
  • 2. Excitatory postsynaptic currents (EPSCs) had a fast component whose amplitude was voltage insensitive and a slow component whose amplitude was voltage dependent with a region of negative slope resistance in the range of -70 to -30 mV. 3. (
  • 6. In addition, the late EPSCs were not present in low (0.5 mM) extracellular calcium, and they were also eliminated by the removal of the dentate hilus from the slice. (
  • Carbachol increased the frequency and amplitude of spontaneous EPSCs (sEPSCs) recorded from PV + BCs in layers 3-6, but not in BCs from layer 2. (
  • We demonstrate that cell death (93+/-2 vs. 46+/-1.6%) as well as fragmentation of nuclear DNA induced by low extracellular potassium were prevented by addition of ouabain (0.1 mM), a specific inhibitor of the Na(+),K(+)-ATPase. (
  • Caffeine pretreatment prevented these effects of PGE1, and the adenosine A2A receptor inhibitor MSX-3 had similar preventative effects. (
  • 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. (
  • Transverse hippocampal slices (400 μm) were prepared from 4- to 8-week-old transgenic C57BL/6 mice (line M) expressing enhanced GFP (EGFP) ( 26 ). (
  • Loss-of-function mutations in the transcriptional regulator methyl-CpG-binding protein 2 ( MECP2 ) occur in 95% of RTT individuals ( 3 ), and Mecp2 -deficient mice recapitulate several neurological features of RTT, including impaired hippocampal-dependent learning and memory ( 4 ). (
  • The behavioural effects of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) in mice. (
  • RTT individuals develop typically until 6-18 mo, when neurological symptoms begin, including intellectual disability, autistic features, deficits in motor control and sensory perception, breathing irregularities, and epilepsy disorders ( 2 ). (
  • Would the Department of Finance consider expanding the exclusion in subsection 47(3) so that shares acquired from either an EPSP or an RSU are not subject to the requirement to average the cost of shares received from such plans with identical share holdings? (
  • 3 Department of Biomedical Sciences and Padova Neuroscience Center, University of Padova, 35131 Padova, Italy. (
  • Cells with high-noise kainate responses had average channel conductances of 5 to 7 picoseimens, whereas the average conductances of low-variance noise responses were 0.3 to 2.0 picoseimens. (
  • The 2(1H)-quinoxalinone (Qu) significantly reduced depressive-like responses as evaluated in FST, whereas no anxiolytic-like effect was found as measured by open field test (OF). (
  • For example, patients with migraine exhibit increased cortical responses to noxious and non-noxious sensory stimuli during the interictal period ( 6 , 7 ). (
  • 7. Mossy hilar cells in the traumatic dentate gyrus responded with significantly enhanced, prolonged trains of action potential discharges to perforant path stimulation. (
  • The generation of the burst discharges was independent of the membrane potential, and the amplitude of the slow component of the paroxysmal depolarization shift increased with hyperpolarization, indicating that the 1,3-dipropyl-8-cyclopentylxanthine-induced bursts were synaptically mediated events. (
  • Both 1,3-dipropyl-8-cyclopentylxanthine and the adenosine-degrading enzyme adenosine deaminase produced an apparently irreversible depolarization of the membrane potential by about 20 mV. (
  • Adult male Wistar rats, weighing 250-300 g (n = 32), were housed under a constant temperature (22 °C) and illuminated 7:00 a.m. to 7:00 p.m., with food pellets and water available ad libitum. (
  • Whole body plethysmography was used to assess the HVR and apnea incidence in neonatal rats 2 h following a single bolus intraperitoneal injection of PGE1 with and without prior caffeine treatment. (
  • Submitted for publication February 2, 1996. (
  • 2) The shape of kainate current-voltage (I-V) curves and their reversal potentials were unchanged in cGMP. (
  • 3) Neither the estimated conductance nor the kinetics of the kainate-activated channels was affected by cGMP. (
  • Here, we describe altered cortical physiology in a genetic mouse model of familial hemiplegic migraine type 2 (FHM2), with reduced expression of astrocytic Na + ,K + -ATPases. (
  • Defective neuron-astrocyte interactions have been implicated in the establishment and development of several neurological disorders ( 1 - 3 ). (
  • Laser scanning photostimulation revealed that NCAM deletion increased the strength of close-in inhibitory connections to layer 2/3 pyramidal cells of the ACC. (
  • Further, application of taurine at different doses (10 μ M to 3 mM) showed a concentration dependent depolarizations and inward currents with the EC 50 of 84.3 μ M and 723 μ M, respectively. (
  • This review compares, across Classes of vertebrates, the functional and anatomical characteristics of 1) the neural pathways that process visual information about objects, and 2) stimulus selection pathways that determine the objects to which an animal attends. (