Glycine: 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.GABA Agonists: Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).Receptors, Glycine: Cell surface receptors that bind GLYCINE with high affinity and trigger intracellular changes which influence the behavior of cells. Glycine receptors in the CENTRAL NERVOUS SYSTEM have an intrinsic chloride channel and are usually inhibitory.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.GABA Agents: Substances used for their pharmacological actions on GABAergic systems. GABAergic agents include agonists, antagonists, degradation or uptake inhibitors, depleters, precursors, and modulators of receptor function.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Glycine Agents: Substances used for their pharmacological actions on glycinergic systems. Glycinergic agents include agonists, antagonists, degradation or uptake inhibitors, depleters, precursors, and modulators of receptor function.GABA-A Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.Receptors, GABA-A: 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.Serotonin 5-HT1 Receptor Agonists: 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.GABA Modulators: Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here.GABA-B Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.Serotonin 5-HT2 Receptor Agonists: 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.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Glycine Plasma Membrane Transport Proteins: A family of sodium chloride-dependent neurotransmitter symporters that transport the amino acid GLYCINE. They differ from GLYCINE RECEPTORS, which signal cellular responses to GLYCINE. They are located primarily on the PLASMA MEMBRANE of NEURONS; GLIAL CELLS; EPITHELIAL CELLS; and RED BLOOD CELLS where they remove inhibitory neurotransmitter glycine from the EXTRACELLULAR SPACE.Receptors, GABA-B: A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.GABA Plasma Membrane Transport Proteins: A family of plasma membrane neurotransmitter transporter proteins that regulates extracellular levels of the inhibitory neurotransmitter GAMMA-AMINOBUTYRIC ACID. They differ from GABA RECEPTORS, which signal cellular responses to GAMMA-AMINOBUTYRIC ACID. They control GABA reuptake into PRESYNAPTIC TERMINALS in the CENTRAL NERVOUS SYSTEM through high-affinity sodium-dependent transport.Baclofen: 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.Rats, Sprague-Dawley: 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.Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.Muscimol: 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.Cannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.Glycine Dehydrogenase (Decarboxylating): A PYRIDOXAL PHOSPHATE dependent enzyme that catalyzes the decarboxylation of GLYCINE with the transfer of an aminomethyl group to the LIPOIC ACID moiety of the GLYCINE DECARBOXYLASE COMPLEX H-PROTEIN. Defects in P-protein are the cause of non-ketotic hyperglycinemia. It is one of four subunits of the glycine decarboxylase complex.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Strychnine: 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.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.GABA-A Receptor Antagonists: Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.Receptors, Opioid, kappa: 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.GABA Uptake Inhibitors: Compounds that suppress or block the plasma membrane transport of GAMMA-AMINOBUTYRIC ACID by GABA PLASMA MEMBRANE TRANSPORT PROTEINS.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.Histamine Agonists: Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.Neurons: 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.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Muscarinic Agonists: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.Excitatory Amino Acid Agonists: Drugs that bind to and activate excitatory amino acid receptors.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Patch-Clamp Techniques: An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.Nicotinic Agonists: Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.Neural Inhibition: The function of opposing or restraining the excitation of neurons or their target excitable cells.Glycine N-Methyltransferase: An enzyme that catalyzes the METHYLATION of GLYCINE using S-ADENOSYLMETHIONINE to form SARCOSINE with the concomitant production of S-ADENOSYLHOMOCYSTEINE.Phosphinic Acids: Inorganic or organic derivatives of phosphinic acid, H2PO(OH). They include phosphinates and phosphinic acid esters.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.Nipecotic AcidsPicrotoxin: 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.Synaptic Transmission: The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.Piperidines: A family of hexahydropyridines.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Receptors, Opioid, delta: A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.Quinpirole: A dopamine D2/D3 receptor agonist.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.GABA-B Receptor Antagonists: Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.Cells, Cultured: 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.Benzazepines: Compounds with BENZENE fused to AZEPINES.Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Receptors, Serotonin: Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.Serotonin: 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.Membrane Potentials: The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).Calcium: A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.Receptors, N-Methyl-D-Aspartate: A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.Naphthalenes: Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.Behavior, Animal: The observable response an animal makes to any situation.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.PyrrolidinesHippocampus: 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.Electrophysiology: 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.Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.Cholinergic Agonists: Drugs that bind to and activate cholinergic receptors.Betaine: A naturally occurring compound that has been of interest for its role in osmoregulation. As a drug, betaine hydrochloride has been used as a source of hydrochloric acid in the treatment of hypochlorhydria. Betaine has also been used in the treatment of liver disorders, for hyperkalemia, for homocystinuria, and for gastrointestinal disturbances. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1341)Benzoxazines: OXAZINES with a fused BENZENE ring.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Glycine Decarboxylase Complex H-Protein: A LIPOIC ACID-containing protein that plays the pivotal role in the transfer of methylamine groups and reducing equivalents between the three enzymatic components of the glycine decarboxylase complex.Aminobutyrates: 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.Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Dopamine Antagonists: Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.Receptors, Glucagon: Cell surface receptors that bind glucagon with high affinity and trigger intracellular changes which influence the behavior of cells. Activation of glucagon receptors causes a variety of effects; the best understood is the initiation of a complex enzymatic cascade in the liver which ultimately increases the availability of glucose to body organs.PyridazinesPurinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Ligands: A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)Dopamine: 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.N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).Glycine Decarboxylase Complex: A enzyme complex that catalyzes the oxidative DECARBOXYLATION and DEAMINATION of GLYCINE into CARBON DIOXIDE; AMMONIA; NADH; and N5N10-methylenetetrahydrofolate. It is composed of four different component protein components referred to as H, P, L, and T.Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.Cyclic AMP: An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.Receptor, Cannabinoid, CB2: A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.Inhibitory Postsynaptic Potentials: Hyperpolarization of membrane potentials at the SYNAPTIC MEMBRANES of target neurons during NEUROTRANSMISSION. They are local changes which diminish responsiveness to excitatory signals.Amino Acid Sequence: 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.Receptors, Metabotropic Glutamate: 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.Venoms: Poisonous animal secretions forming fluid mixtures of many different enzymes, toxins, and other substances. These substances are produced in specialized glands and secreted through specialized delivery systems (nematocysts, spines, fangs, etc.) for disabling prey or predator.Serotonin 5-HT3 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT3 RECEPTORS.Kinetics: The rate dynamics in chemical or physical systems.Receptors, Neurotransmitter: Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.Tetrahydronaphthalenes: Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.Soybeans: An annual legume. The SEEDS of this plant are edible and used to produce a variety of SOY FOODS.Purinergic P2X Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.Purinergic P2Y Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.Signal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Mice, Inbred C57BLTaurine: 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.Microinjections: The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.PiperazinesReceptor, Serotonin, 5-HT1B: A serotonin receptor subtype found at high levels in the BASAL GANGLIA and the frontal cortex. It plays a role as a terminal autoreceptor that regulates the rate of SEROTONIN release from nerve endings. This serotonin receptor subtype is closely related to and has similar drug binding properties as the 5-HT1D RECEPTOR. It is particularly sensitive to the agonist SUMATRIPTAN and may be involved in mediating the drug's antimigraine effect.Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.Bicyclo Compounds, Heterocyclic: A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)Receptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.QuinoxalinesXanthines: Purine bases found in body tissues and fluids and in some plants.Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Enkephalins: One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.Amino Acids: 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.Methylhistamines: Histamine substituted in any position with one or more methyl groups. Many of these are agonists for the H1, H2, or both histamine receptors.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Benzeneacetamides: Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.Receptors, sigma: A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.Bicyclo CompoundsMorpholinesReceptors, Serotonin, 5-HT4: A subtype of G-protein-coupled SEROTONIN receptors that preferentially couple to GS STIMULATORY G-PROTEINS resulting in increased intracellular CYCLIC AMP. Several isoforms of the receptor exist due to ALTERNATIVE SPLICING of its mRNA.Receptor, Serotonin, 5-HT1A: 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.Glutamate Decarboxylase: A pyridoxal-phosphate protein that catalyzes the alpha-decarboxylation of L-glutamic acid to form gamma-aminobutyric acid and carbon dioxide. The enzyme is found in bacteria and in invertebrate and vertebrate nervous systems. It is the rate-limiting enzyme in determining GAMMA-AMINOBUTYRIC ACID levels in normal nervous tissues. The brain enzyme also acts on L-cysteate, L-cysteine sulfinate, and L-aspartate. EC 4.1.1.15.Synapses: Specialized junctions at which a neuron communicates with a target cell. At classical synapses, a neuron's presynaptic terminal releases a chemical transmitter stored in synaptic vesicles which diffuses across a narrow synaptic cleft and activates receptors on the postsynaptic membrane of the target cell. The target may be a dendrite, cell body, or axon of another neuron, or a specialized region of a muscle or secretory cell. Neurons may also communicate via direct electrical coupling with ELECTRICAL SYNAPSES. Several other non-synaptic chemical or electric signal transmitting processes occur via extracellular mediated interactions.Binding, Competitive: 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.Indoles: 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.Neurotransmitter Agents: 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.Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Animals, Newborn: Refers to animals in the period of time just after birth.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Receptor, Adenosine A3: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Receptor, Adenosine A1: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Excitatory Postsynaptic Potentials: 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.Receptor, Serotonin, 5-HT2A: 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.Glycine Hydroxymethyltransferase: A pyridoxal phosphate enzyme that catalyzes the reaction of glycine and 5,10-methylene-tetrahydrofolate to form serine. It also catalyzes the reaction of glycine with acetaldehyde to form L-threonine. EC 2.1.2.1.Receptors, Dopamine: Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.4-Aminobutyrate Transaminase: An enzyme that converts brain gamma-aminobutyric acid (GAMMA-AMINOBUTYRIC ACID) into succinate semialdehyde, which can be converted to succinic acid and enter the citric acid cycle. It also acts on beta-alanine. EC 2.6.1.19.Receptors, Prostaglandin E: Cell surface receptors which bind prostaglandins with a high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin E receptors prefer prostaglandin E2 to other endogenous prostaglandins. They are subdivided into EP1, EP2, and EP3 types based on their effects and their pharmacology.Receptors, Histamine H3: A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)Isonicotinic Acids: Heterocyclic acids that are derivatives of 4-pyridinecarboxylic acid (isonicotinic acid).Structure-Activity Relationship: 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.Receptors, Histamine: Cell-surface proteins that bind histamine and trigger intracellular changes influencing the behavior of cells. Histamine receptors are widespread in the central nervous system and in peripheral tissues. Three types have been recognized and designated H1, H2, and H3. They differ in pharmacology, distribution, and mode of action.Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.CHO Cells: CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Receptors, Drug: Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.Dopamine Agents: Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Purinergic Agonists: Compounds that bind to and activate PURINERGIC RECEPTORS.Sodium Oxybate: The sodium salt of 4-hydroxybutyric acid. It is used for both induction and maintenance of ANESTHESIA.Amino Acid Transport Systems, Neutral: Amino acid transporter systems capable of transporting neutral amino acids (AMINO ACIDS, NEUTRAL).Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.Receptor, Serotonin, 5-HT2C: A serotonin receptor subtype found primarily in the CENTRAL NERVOUS SYSTEM and the CHOROID PLEXUS. This receptor subtype is believed to mediate the anorectic action of SEROTONIN, while selective antagonists of the 5-HT2C receptor appear to induce ANXIETY. Several isoforms of this receptor subtype exist, due to adenine deaminase editing of the receptor mRNA.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Sarcosine: An amino acid intermediate in the metabolism of choline.RNA, Messenger: RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.Protein Subunits: Single chains of amino acids that are the units of multimeric PROTEINS. Multimeric proteins can be composed of identical or non-identical subunits. One or more monomeric subunits may compose a protomer which itself is a subunit structure of a larger assembly.Xenopus laevis: 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.Cerebral Cortex: 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.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Acetylcholine: 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.Amphetamines: Analogs or derivatives of AMPHETAMINE. Many are sympathomimetics and central nervous system stimulators causing excitation, vasopressin, bronchodilation, and to varying degrees, anorexia, analepsis, nasal decongestion, and some smooth muscle relaxation.Disease Models, Animal: Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.Microdialysis: 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.Action Potentials: Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.Impromidine: A highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.Oligopeptides: Peptides composed of between two and twelve amino acids.Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.Hydrocarbons, FluorinatedImidazoles: Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).Corpus Striatum: 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.Substance P: An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.Anti-Anxiety Agents: Agents that alleviate ANXIETY, tension, and ANXIETY DISORDERS, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. ADRENERGIC BETA-ANTAGONISTS are commonly used in the symptomatic treatment of anxiety but are not included here.
GABA reuptake inhibitor Glycine reuptake inhibitor Excitatory amino acid receptor agonist Excitatory amino acid receptor ...
A1 receptor agonist has been shown to depress preBötC rhythmogenesis independent of the neurotransmitters GABA and glycine in ... Blocking this inhibition from Glycine or GABA causes it's neurons to be incapable of switching from the active phase to the ... Since many of these neurons express GABA, glutamate, serotonin and adenosine receptors, chemicals custom tailored to bind at ... The suppression of muscarinic receptors and the activation of nicotinic receptors due to prenatal exposure to nicotine have ...
It is an agonist for both central benzodiazepine receptors and to the peripheral-type benzodiazepine receptors found in rat ... It acts on benzodiazepine receptors in the brain which are associated with the GABA receptors, causing an enhanced binding of ... Nitrazepam causes a decrease in the cerebral contents of the amino acids glycine and alanine in the mouse brain. The decrease ... and long-acting benzodiazepine-receptor agonists with different receptor selectivity on motor coordination and muscle ...
Additional information on GABAB receptors has been reviewed elsewhere. GABA agonist GABA antagonist Kuffler SW, Edwards C ( ... Members of this superfamily, which includes nicotinic acetylcholine receptors, GABAA receptors, glycine and 5-HT3 receptors, ... Although the term "GABAС receptor" is frequently used, GABAС may be viewed as a variant within the GABAA receptor family. ... The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief ...
... at either the GABAA or glycine receptors, or ionotropic glutamate receptor agonists. Many other drugs may cause convulsions as ... also GABA antagonist) Sinomenine Strychnine Thebaine Tutin Ionotropic glutamate receptor agonists AMPA Domoic acid Kainic acid ... GABAA receptor antagonists, inverse agonists or negative allosteric modulators Bemegride Bicuculline Cicutoxin Cyclothiazide ... Tetramethylenedisulfotetramine Thujone GABA synthesis inhibitors 3-Mercaptopropionic acid Allylglycine Glycine receptor ...
... but rather through interaction with glycine and/or GABA receptors. As a polar compound, it has a limited ability to cross the ... Morphine-3-glucuronide is a metabolite of morphine produced by UGT2B7.[citation needed] It is not active as an opioid agonist, ... but does have some action as a convulsant, which does not appear to be mediated through opioid receptors, ...
4-Iodopropofol GABA receptor GABAB receptor GABAA-ρ receptor Gephyrin Glycine receptor GABAA receptor positive allosteric ... and the 5HT3 receptor. There are numerous subunit isoforms for the GABAA receptor, which determine the receptor's agonist ... GABA receptors A review of GABA and the receptors to which it binds. Tocris Cookson LTD. Enz R, Cutting GR (1998). "Molecular ... The ligand GABA is the endogenous compound that causes this receptor to open; once bound to GABA, the protein receptor changes ...
... the binding of glycine appears to be required for receptor activation. Because neither of these agonists alone can open this ... GABAA receptors are ligand-gated ion channels. GABA (gamma-aminobutyric acid), the endogenous ligand for these receptors, is ... which acts as a selective agonist at these receptors. When the NMDA receptor is activated by the binding of two co-agonists, ... The AMPA receptor GluA2 (GluR2) tetramer was the first glutamate receptor ion channel to be crystallized. Ligands: Agonists: ...
"Interaction of pitrazepin with the GABA/benzodiazepine receptor complex and with glycine receptors". European Journal of ... Murphy VF, Wann KT (November 1988). "The action of GABA receptor agonists and antagonists on muscle membrane conductance in ... Pitrazepin is a competitive GABAA and glycine receptor antagonist. It has been used to study insect and snail nervous systems ... Sattelle DB, Pinnock RD, Wafford KA, David JA (January 1988). "GABA receptors on the cell-body membrane of an identified insect ...
GABA) at GABAA receptor. Allopregnanolone has effects similar to those of other positive allosteric modulators of the GABA ... and glycine receptors. Unlike progesterone, allopregnanolone is inactive at the nuclear progesterone receptor (nPR). However, ... In addition, allopregnanolone has recently been found to be an agonist of the newly discovered membrane progesterone receptors ... In addition to its actions on GABA receptors, allopregnanolone, like progesterone, is known to be a negative allosteric ...
... taste receptor. Theanine increases serotonin, dopamine, GABA, and glycine levels in various areas of the brain, as well as BDNF ... the NMDA receptor. It acts as an antagonist of the former two sites and as an agonist of the latter site. Theanine also binds ... Specifically, it binds to ionotropic glutamate receptors in the micromolar range, including the AMPA and kainate receptors and ... and GABA, with possible improvement in specific memory and learning tasks. A research study in 2011 showed that regular brewed ...
... receptors have multiple binding sites just like ionotropic GABA receptors and can be influenced by co-agonists such the glycine ... Various metabotropic receptors can include certain glutamate receptors, muscarinic ACh receptors, GABAB receptors, and receptor ... Ionotropic glutamate receptors can include NMDA, AMPA, and kainate receptors. These receptors are named after agonists that ... Nicotinic, GABA, and Glutamate receptors are among some of the cell surface receptors regulated by ligand-gated ion channel ...
... s act as positive allosteric modulators, and at higher doses, as agonists of GABAA receptors. GABA is the principal ... the 5-HT3 receptor channel, and the glycine receptor channel. However, while GABAA receptor currents are increased by ... Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. In addition to this GABAergic effect, ... Taken together, the findings that barbiturates potentiate inhibitory GABAA receptors and inhibit excitatory AMPA receptors can ...
An important reflex initiated by cutaneous receptors and pain receptors is the flexor reflex. This reflex mechanism allows for ... When the agonist muscle is inhibited from contracting, the antagonist muscle contracts. ... Different neurotransmitters are released from different interneurons, but the two most common neurotransmitters are GABA, the ... where it establishes inhibition by expressing its inhibitory neurotransmitter glycine. However, some reports have indicated ...
... and GABA agonist tranquilizers (benzodiazepines). New endogenous chemicals are continually identified. Specific receptors have ... Another is the proposal of new routes of exploration for anti-psychotics such as glycine reuptake inhibitors.[9] Although the ... The plausible cause of HPPD is damage to the inhibitory GABA circuit in the visual pathway (GABA agonists such as midazolam can ... Many receptors are found to be pentameric clusters of five trans-membrane proteins (not necessarily the same) or receptor ...
The Cys-loop receptor superfamily includes inhibitory receptors (GABA A, GABA C, glycine receptors) and excitatory receptors ( ... at the water-lipid interface that play critical roles in protein functions and agonist binding may be disrupted by general ... "Sites of alcohol and volatile anaesthetic action on GABA(A) and glycine receptors". Nature. 389 (6649): 385-9. Bibcode: ... gated ion channels in synapse and G-protein coupled receptors altering their ion flux. Particularly Cys-loop receptors[42] are ...
... which includes nicotinic acetylcholine receptors, GABAA receptors, glycine and 5-HT3 receptors, possess a characteristic loop ... This mechanism is responsible for the sedative effects of GABAA allosteric agonists. In addition, activation of GABA receptors ... GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors); whereas GABAB receptors ... GABAB receptorEdit. Main article: GABAB receptor. A slow response to GABA is mediated by GABAB receptors,[40] originally ...
Hanley JG, Jones EM, Moss SJ (2000). "GABA receptor rho1 subunit interacts with a novel splice variant of the glycine ... 2005). "Mapping the rho1 GABA(C) receptor agonist binding pocket. Constructing a complete model". J. Biol. Chem. 280 (2): 1535- ... GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA receptors, which are ligand-gated ... May 1991). "Cloning of the gamma-aminobutyric acid (GABA) rho 1 cDNA: a GABA receptor subunit highly expressed in the retina". ...
Puil E. (Jan 2010). "R-Isovaline: a subtype-specific agonist at GABA(B)-receptors?". Neuroscience. 201: 85-95. doi:10.1016/j. ... The structure of isovaline is similar to the amino acids GABA and glycine, the chief inhibitory neurotransmitters in the ... Jun 28, 2012). "GABA(B) receptor-mediated selective peripheral analgesia by the non-proteinogenic amino acid, isovaline". ... Isovaline acts as an analgesic in mice by activating peripheral GABAB receptors. In a mouse model of osteoarthritis isovaline ...
Olsen RW, Betz H (2006). "GABA and glycine". In Siegel GJ, Albers RW, Brady S, Price DD (eds.). Basic Neurochemistry: Molecular ... They are defined as ligands able to directly activate a receptor by binding to an allosteric agonist binding site distinct from ... An ago-allosteric modulator acts as an agonist and an enhancer for endogenous agonists in increasing agonist potency (the dose ... Allosteric agonistsEdit. Allosteric agonists are to be distinguished from pure allosteric modulators. ...
... also acts as a glycine receptor antagonist and GABA receptor antagonist at very high concentrations. Levorphanol is 6 to 8 ... Levorphanol acts predominantly as an agonist of the μ-opioid receptor (MOR), but is also an agonist of the δ-opioid receptor ( ... DOR), κ-opioid receptor (KOR), and the nociceptin receptor (NOP), as well as an NMDA receptor antagonist and a serotonin- ... At the same time however, activation of this receptor as well as of the DOR have been determined to contribute to its analgesic ...
G protein-coupled receptor - G3P - GABA - GABA receptor - GABA-A receptor - gag-onc fusion protein - galanin - gamete - gamma- ... glucocorticoid receptor - glucose - glutamate - glutamate receptor - Glutamic acid - Glutamine - Glycerine - Glycine - glycine ... Inverse agonist - invertebrate peptide receptor - invertebrate photoreceptor - Ion channel - ion channel gating - Ionic bond - ... interleukin receptor - interleukin-1 receptor - interleukin-2 receptor - interleukin-3 - interleukin-3 receptor - intermediate ...
Glutamate-Gated Chloride Channels Which Likely Explain the Agonist Selectivity of the Vertebrate Glycine and GABAA-ρ Receptors ... Kehoe, JacSue; Vulfius, Catherine (2000-12-01). "Independence of and Interactions between GABA-, Glutamate-, and Acetylcholine- ... She determined that multiple receptors for a particular neurotransmitter could be found on a neuron, each receptor could change ... She discovered that one neurotransmitter can have multiple types of receptors, which could vary in level and type of response. ...
Recent research strongly supports the hypothesis that the N-arachidonoyl glycine (NAGly) receptor GPR18 is the molecular ... has not been reported with agonists that bind to cannabinoid receptors. THC, as well as the two major endogenous compounds ... from the depolarized post-synaptic neuron bind to CB1 receptors in the pre-synaptic neuron and cause a reduction in GABA ... Cannabinoid receptors are of a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of ...
Alcohol also modulates ionotropic GABA receptors. Metabotropic receptors, or G-protein-coupled receptors, do not use ion ... Glycine molecules and receptors work much in the same way in the spinal cord, brain, and retina. There are two types of ... When a high concentration of agonist is applied for an extended amount of time (fifteen minutes or more), hyperpolarization ... GABA is a very common neurotransmitter used in IPSPs in the adult mammalian brain and retina. GABA receptors are pentamers most ...
Receptor/signaling modulators GABAA receptor positive modulators GABA metabolism/transport modulators ... GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated ... GABA-A receptor activity. • transmembrane signaling receptor activity. • inhibitory extracellular ligand-gated ion channel ... GABA-A receptor complex. • postsynaptic membrane. • membrane. • synapse. • integral component of plasma membrane. • chloride ...
GABA(A) Receptor and Glycine Receptor Activation by Paracrine/Autocrine Release of Endogenous Agonists: More Than a Simple ... In addition, it is now established that both GABA receptors (GABARs) and glycine receptors (GlyRs) can be located ... such as GABA, glycine, and taurine. Recently, non-synaptic release of GABA, glycine, and taurine gained further attention with ... R and GlyR agonists. We then discuss the proposed non-synaptic release mechanisms and/or pathways for GABA, glycine, and ...
... receptor agonist (RS)-3,5-dihydroxyphenylglycine (DHPG) (100 microM, 10 min) induced long-term depression (LTD) of synaptic ... Excitatory Amino Acid Agonists / pharmacology* * Female * GABA-A Receptor Agonists * Glycine / analogs & derivatives* ... mGlu receptors or a combined group I and II agonist (30-100 microM (1S,3R)-ACPD) induced LTD. However, an agonist (1 mM CHPG) ... or by adding the GABA(A) receptor antagonist picrotoxin (29+/-2%). The N-methyl-D-aspartate (NMDA) receptor antagonist AP5 (100 ...
GABA, dopamine, glycine); an agonist of an inhibitory neurotransmitter (e.g., a GABA receptor agonist such as midazolam or ... an excitatory neurotransmitter agonist (e.g., glutamate receptor agonist, L-aspartic acid, N-methyl-D-aspartic acid (NMDA), ... Group II metabotropic glutamate receptor (mGluR) agonists such as DCG-IV); a local anesthetic agent (e.g., lidocaine); and/or ... Inhibition of inflammatory cytokine production by cholinergic agonists and vagus nerve stimulation. ...
GABA, dopamine, glycine); an agonist of an inhibitory neurotransmitter (e.g., a GABA receptor agonist such as midazolam or ... Group II metabotropic glutamate receptor (mGluR) agonists such as DCG-IV); a local anesthetic agent (e.g., lidocaine); and/or ... 2-hydroxy-GABA, nipecotic acid); an agent that decreases the level of an excitatory neurotransmitter (e.g., ...
GABA, dopamine, glycine); an agonist of an inhibitory neurotransmitter (e.g., a GABA receptor agonist such as midazolam or ... an excitatory neurotransmitter agonist (e.g., glutamate receptor agonist, L-aspartic acid, N-methyl-D-aspartic acid (NMDA), ... Alpha adrenergic receptor agonists for treatment of pain and/or inflammation. US8906360. 24 Jul 2006. 9 Dic 2014. The Board Of ... Beta adrenergic receptor agonists for treatment of pain and/or inflammation. US20090264489 *. 4 Mar 2009. 22 Oct 2009. Warsaw ...
GABA, dopamine, glycine); an agonist of an inhibitory neurotransmitter (e.g., a GABA receptor agonist such as midazolam or ... an excitatory neurotransmitter agonist (e.g., glutamate receptor agonist, L-aspartic acid, N-methyl-D-aspartic acid (NMDA), ... Group II metabotropic glutamate receptor (mGluR) agonists such as DCG-IV); a local anesthetic agent (e.g., lidocaine); and/or ...
This inhibitory action on fGDPs was mimicked by applying 2 μm glycine or 0.1 μm isoguvacine, a GABAA-receptor agonist. ... Glycine-mediated actions on NMDARs were excluded by 20 μm AP-5. GABAA and AMPA-kainate receptors were blocked by 1 μm SR 95531 ... 2002) Beta-alanine and taurine as endogenous agonists at glycine receptors in rat hippocampus in vitro. J Physiol 539:191-200, ... 2010) Glycine and glycine receptor signaling in hippocampal neurons: diversity, function and regulation. Prog Neurobiol 91:349- ...
Therefore, we propose that ES acts as a partial agonist at the picrotoxin GABA-blocking receptor. 4. MPS had no effect on GABA ... LY341495 and (2S,2R,3R)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV, a group II agonist) elicited negative and positive ... GABA) activates postsynaptic GABA(A) receptors but not pre- or postsynaptic GABA(B) receptors. Elevation of synaptic GABA ... Kinetic and pharmacological properties of GABA(A) receptors in single thalamic neurons and GABA(A) subunit expression JOURNAL ...
... whereas glycine was ineffective. [3H]Thiocolchicoside binding was also displaced by several GABA(A) receptor agonists and ... GABA) and [3H]strychnine binding, suggesting an interaction with both GABA and strychnine-sensitive glycine receptors. In order ... receptor. The different affinities for the GABA(A) receptor agonists and antagonists and sensitivity to neurosteroids obtained ... besides GABA(A) receptors, thiocolchicoside can bind to another unidentified site. Unlabelled thiocolchicoside, however, ...
... adenosine A1 receptor, and alpha and beta adrenoceptors. ... Volatile agents such as desflurane may activate GABA channels ... AGABA-A receptor (anion channel). positive allosteric modulator. Humans. AGlycine receptor subunit alpha-1. agonist ... The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride ... Desflurane also binds to and agonizes the GABA receptor, the large conductance Ca2+ activated potassium channel, the glycine ...
GABA) and glycine. Whereas GABAergic synapses are abundant in the cortex and cerebellum, glycine predominates... ... Goldinger A, Müller WE, Wollert U (1981) Inhibition of glycine and GABA receptor binding by several opiate agonists and ... Interactions between three pyridazinyl-GABA derivatives and central GABA and glycine receptors in the rat, an in vivo ... The glycine receptor deficiency of the mutant mouse spastic: evidence for normal glycine receptor structure and localization. J ...
It was shown that application of the TRPV1 agonist capsaicin increased the frequency of excitatory AMPA receptor- mediated as ... All neurons also responded to γ-aminobutyric acid (GABA) and glycine with currents mediated by GABAA receptors and glycine ... Currents evoked by GABA and glycine in acutely dissociated neurons from the rat medial preoptic nucleus. Karlsson, Urban Umeå ... the current decay in the presence of GABA or glycine was mainly due to a change in the chloride driving force and that receptor ...
Miller PS, Harvey RJ, and Smart TG (2004) Differential agonist sensitivity of glycine receptor alpha2 subunit splice variants. ... to yield receptors with properties of both GABAA and GABAC subtypes. Furthermore, GABAA and GABAB receptors, which differ ... The GABAA γ2S subunit also forms a complex with both GABABR1 and GABABR2 subunits to allow agonist-induced receptor ... ABBREVIATIONS: GABAR, GABA receptor; RDL, resistant to dieldrin; GRD, GABA receptor of Drosophila; TM, transmembrane; CACA, cis ...
Regarding receptor specificity of strychnine, the glycine, GABA and nicotinic receptors are homologous members of a receptor ... apparent affinity of an antagonist for the receptor. Kd apparent affinity of an agonist for the receptor. ... 1992) Antagonism of ligand-gated ion channel receptors: Two domains of the glycine receptor α subunit form the strychnine- ... 1) is a well-known competitive antagonist of glycine at glycine-gated Cl−channels (Saitoh et al., 1994), its binding to glycine ...
GABA reuptake inhibitor Glycine reuptake inhibitor Excitatory amino acid receptor agonist Excitatory amino acid receptor ...
A1 receptor agonist has been shown to depress preBötC rhythmogenesis independent of the neurotransmitters GABA and glycine in ... Blocking this inhibition from Glycine or GABA causes its neurons to be incapable of switching from the active phase to the ... Since many of these neurons express GABA, glutamate, serotonin and adenosine receptors, chemicals custom tailored to bind at ... The suppression of muscarinic receptors and the activation of nicotinic receptors due to prenatal exposure to nicotine have ...
... receptors, Serotonin (5-HT3) receptors, prostaglandin system, GABA receptors, and glycine receptors, so that why opioid-induced ... opioid agonist-antagonists, propofol, and nonsteroidal antiinflammatory drugs. ... Many medications have been used to treat this side effect included antihistamines, 5-HT3 (serotonin) receptor antagonists, ... mediated central µ opioid receptors, Dopamine (D2) ...
work on GABA-A receptors,. cause allosteric potentiation. Ex: benzodiazepines and barbiturates ... excitatory -- nicotine = agonist. - permeable to: Na+, K+, Ca++, Mg++. * in NMJ, autonomic ganglia, and CNS (esp. basal ... 2. glutamate GABA via GAD (Glutamine decarboxylase). * removed by reuptake*. 3. GABA Glutamate via GABA-transaminase. 4 ... Glycine receptor ionotropic receptor, most present in ventral spinal cord. - IPSP. * increases Cl- permeability in post- ...
Nicotinic acetylcholine receptors (nAChRs) belong to a family of neurotransmitter receptors that includes GABA-, glycine-, and ... Le Novere N, Grutter T, and Changeux J-P (2002) Models of the extracellular domain of the nicotinic receptors and of agonist- ... GABA receptors bind GABA at β-α interfaces (Smith and Olsen, 1995). In the α1β3 GABAA receptor, α1Glu137, α1His141 and β3Glu182 ... GABAA receptors also possess multiple Zn2+-binding sites. For clarity, it is important to remember that GABAA receptor β ...
acetylcholine, glycine, GABA =, histamine-gated chloride channels (what happens when the AChR receptor becomes excessively ... A new class of N-methyl-D-aspartic acid receptor agonists and antagonists--derivatives of imidazole-4,5- and pyrazole-3,4- ... acetylcholine, glycine, GABA =, histamine-gated chloride channels (what happens when the AChR receptor becomes "excessively" ... Histamine H3-receptor inverse agonists as novel antipsychotics. * see also Histidine, and Clozapine, an antihistaminic (also ...
acetylcholine, glycine, GABA =, histamine-gated chloride channels (what happens when the AChR receptor becomes "excessively" ... A new class of N-methyl-D-aspartic acid receptor agonists and antagonists--derivatives of imidazole-4,5- and pyrazole-3,4- ... Histamine H3-receptor inverse agonists as novel antipsychotics. * see also Histidine, and Clozapine, an antihistaminic (also ... "Histamine exerts its actions by combining with specific cellular histamine receptors. The four histamine receptors that have ...
Receptor-binding studies in vitro indicate that felbamate has weak inhibitory effects on GABA-receptor binding, benzodiazepine ... However, felbamate does interact as an antagonist at the strychnine-insensitive glycine recognition site of the NMDA receptor- ... is not effective in protecting chick embryo retina tissue against the neurotoxic effects of the excitatory amino acid agonists ... receptor binding, and is devoid of activity at the MK-801 receptor binding site of the NMDA receptor-ionophore complex. ...
Persistent peripheral inflammation changes AMPA receptor (AMPAR) trafficking in dorsal horn neurons by promoting ... Persistent peripheral inflammation changes AMPA receptor (AMPAR) trafficking in dorsal horn neurons by promoting ... GABAA, and glycine receptors, respectively. In addition, TTX (0.5 μM) and cadmium chloride (100 μM) were added to Krebs ... To prevent a desensitization of AMPARs during bath application of the agonist, we applied AMPA to the slices in the continuous ...
Orexins (also known as hypocretins) were identified as endogenous ligands for two orphan G-protein-coupled receptors in the ... Orexins (also known as hypocretins) were identified as endogenous ligands for two orphan G-protein-coupled receptors in the ... Orexin neurons are strongly inhibited by both a GABAA agonist, muscimol (Yamanaka et al., 2003b), and a GABAB receptor agonist ... it was also reported that orexin neurons express glycine receptors throughout adulthood and that glycine inhibits the electric ...
2011) Chloride ions in the pore of glycine and GABA channels shape the time course and voltage dependence of agonist currents. ... 2002) Openings of the rat recombinant α1 homomeric glycine receptor as a function of the number of agonist molecules bound. J ... 1994) Decreased agonist affinity and chloride conductance of mutant glycine receptors associated with human hereditary ... A prominent property of the flip mechanism fit to wild-type heteromeric glycine receptors is that agonist-binding affinity is ...
  • This will serve to update the most recent classification of GABA A receptors ( Pharmacol Rev 50:291-313, 1998) approved by the Nomenclature Committee of the International Union of Pharmacology. (aspetjournals.org)
  • Consistent with the emphasis of the Nomenclature Committee of the International Union of Pharmacology (IUPHAR), the receptors considered here are limited to mammalian species, with emphasis on humans. (aspetjournals.org)
  • Turecek, R & Trussell, LO 2002, ' Reciprocal developmental regulation of presynaptic ionotropic receptors ', Proceedings of the National Academy of Sciences of the United States of America , vol. 99, no. 21, pp. 13884-13889. (elsevier.com)
  • In vitro and in microiontophoresis, flibanserin behaves as a 5-HT1A agonist, a very weak partial agonist on dopamine D4 receptors, and a 5-HT2A antagonist. (scribd.com)
  • Flibanserin-induced reduction in firing rate in the cortex seems to be mediated through stimulation of postsynaptic 5-HT1A receptors, whereas the reduction of the number of active cells seems to be mediated through dopamine D4 receptor stimulation. (scribd.com)
  • For example, amphetamine, which increases dopamine production and D 2 occupancy, and LSD, which enhances dopaminergic transmission via 5-HT 2A receptor blockade, produce psychosis similar to the positive symptoms of schizophrenia. (cmeinstitute.com)
  • this includes partial dopamine agonists, such as aripiprazole and bifeprunox. (scribd.com)
  • 3) Dopamine-receptor density has been found postmortem to be increased in the brains of schizophrenics who have not been treated with antipsychotic drugs. (scribd.com)
  • 4) Some but not all post- mortem studies of schizophrenic subjects have reported increased dopamine levels and D2-receptor density in the nucleus accumbens, caudate, and putamen. (scribd.com)
  • 1. Central action: blocking of the synapses of the medullary interneurones and under cortical.No the effect on the junction myoneuronale nor on muscle fibre.Inhibit the reflexes polysynaptic, without touching with the arc reflexe elementary monosynaptic.Decrease the influence of the réticulée formation downward facilitatrice on the gamma activity, from where reduction in muscular hypertonicity.Would be a agonist Gabaergique:- Therapie 1981;36:95-102. (alibaba.com)
  • Altschuler RA, Betz H, Parakkal MH, Reeks KA, Wenthold RJ (1986) Identification of glycinergic synapses in the cochlear nucleus through immunocytochemical localization of the postsynaptic receptor. (springer.com)
  • In the central nervous system, melastatin transient receptor potential (TRPM) channels function as receptors for the neurosteroid pregnenolone sulfate (PregS). (eneuro.org)
  • Melastatin transient receptor potential (TRPM)3, a heat sensitive ion channel found throughout the CNS, also functions as a receptor for the neurosteroid pregnenolone sulfate (PregS). (eneuro.org)