Receptors gaba a. Medical search

Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).

Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.

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.

The most common inhibitory neurotransmitter in the central nervous system.

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.

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.

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.

A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.

Compounds that suppress or block the plasma membrane transport of GAMMA-AMINOBUTYRIC ACID by GABA PLASMA MEMBRANE TRANSPORT PROTEINS.

Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.

Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.

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.

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.

An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.

Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.

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.

Inorganic or organic derivatives of phosphinic acid, H2PO(OH). They include phosphinates and phosphinic acid esters.

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.

Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.

The function of opposing or restraining the excitation of neurons or their target excitable cells.

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.

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.

Hyperpolarization of membrane potentials at the SYNAPTIC MEMBRANES of target neurons during NEUROTRANSMISSION. They are local changes which diminish responsiveness to excitatory signals.

An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.

The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.

A 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.

An analogue of GAMMA-AMINOBUTYRIC ACID. It is an irreversible inhibitor of 4-AMINOBUTYRATE TRANSAMINASE, the enzyme responsible for the catabolism of GAMMA-AMINOBUTYRIC ACID. (From Martindale The Extra Pharmacopoeia, 31st ed)

A family of vesicular neurotransmitter transporter proteins that sequester the inhibitory neurotransmitters GLYCINE; GAMMA-AMINOBUTYRIC ACID; and possibly GAMMA-HYDROXYBUTYRATE into SECRETORY VESICLES.

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.

Heterocyclic acids that are derivatives of 4-pyridinecarboxylic acid (isonicotinic acid).

A pregnane found in the urine of pregnant women and sows. It has anesthetic, hypnotic, and sedative properties.

A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.

A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.

Derivatives of 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.

Specialized junctions at which a neuron communicates with a target cell. At classical synapses, a neuron's presynaptic terminal releases a chemical transmitter stored in synaptic vesicles which diffuses across a narrow synaptic cleft and activates receptors on the postsynaptic membrane of the target cell. The target may be a dendrite, cell body, or axon of another neuron, or a specialized region of a muscle or secretory cell. Neurons may also communicate via direct electrical coupling with ELECTRICAL SYNAPSES. Several other non-synaptic chemical or electric signal transmitting processes occur via extracellular mediated interactions.

A group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring.

Neurons whose primary neurotransmitter is GAMMA-AMINOBUTYRIC ACID.

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.

Proteins involved in the transport of organic anions. They play an important role in the elimination of a variety of endogenous substances, xenobiotics and their metabolites from the body.

Most generally any NEURONS which are not motor or sensory. Interneurons may also refer to neurons whose AXONS remain within a particular brain region in contrast to projection neurons, which have axons projecting to other brain regions.

The sodium salt of 4-hydroxybutyric acid. It is used for both induction and maintenance of ANESTHESIA.

A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug.

Drugs that inhibit the transport of neurotransmitters into axon terminals or into storage vesicles within terminals. For many transmitters, uptake determines the time course of transmitter action so inhibiting uptake prolongs the activity of the transmitter. Blocking uptake may also deplete available transmitter stores. Many clinically important drugs are uptake inhibitors although the indirect reactions of the brain rather than the acute block of uptake itself is often responsible for the therapeutic effects.

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).

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 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.

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.

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 benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.

The distal terminations of axons which are specialized for the release of neurotransmitters. Also included are varicosities along the course of axons which have similar specializations and also release transmitters. Presynaptic terminals in both the central and peripheral nervous systems are included.

Derivatives of BUTYRIC ACID that include a double bond between carbon 2 and 3 of the aliphatic structure. Included under this heading are a broad variety of acid forms, salts, esters, and amides that include the aminobutryrate structure.

The relationship between the dose of an administered drug and the response of the organism to the drug.

Depolarization of membrane potentials at the SYNAPTIC MEMBRANES of target neurons during neurotransmission. Excitatory postsynaptic potentials can singly or in summation reach the trigger threshold for ACTION POTENTIALS.

A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.

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.

Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.

Substances that act in the brain stem or spinal cord to produce tonic or clonic convulsions, often by removing normal inhibitory tone. They were formerly used to stimulate respiration or as antidotes to barbiturate overdose. They are now most commonly used as experimental tools.

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.

Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.

Use of electric potential or currents to elicit biological responses.

Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.

Refers to animals in the period of time just after birth.

An inhibitor of glutamate decarboxylase. It decreases the GAMMA-AMINOBUTYRIC ACID concentration in the brain, thereby causing convulsions.

Projection neurons in the CEREBRAL CORTEX and the HIPPOCAMPUS. Pyramidal cells have a pyramid-shaped soma with the apex and an apical dendrite pointed toward the pial surface and other dendrites and an axon emerging from the base. The axons may have local collaterals but also project outside their cortical region.

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.

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.

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.

A group of pyrido-indole compounds. Included are any points of fusion of pyridine with the five-membered ring of indole and any derivatives of these compounds. These are similar to CARBAZOLES which are benzo-indoles.

A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.

The part of brain that lies behind the BRAIN STEM in the posterior base of skull (CRANIAL FOSSA, POSTERIOR). It is also known as the "little brain" with convolutions similar to those of CEREBRAL CORTEX, inner white matter, and deep cerebellar nuclei. Its function is to coordinate voluntary movements, maintain balance, and learn motor skills.

Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.

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.

Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS.

Agents that inhibit SODIUM-POTASSIUM-CHLORIDE SYMPORTERS which are concentrated in the thick ascending limb at the junction of the LOOP OF HENLE and KIDNEY TUBULES, DISTAL. They act as DIURETICS. Excess use is associated with HYPOKALEMIA and HYPERGLYCEMIA.

A clear, colorless liquid rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in ALCOHOLIC BEVERAGES.

Na-K-Cl transporter ubiquitously expressed. It plays a key role in salt secretion in epithelial cells and cell volume regulation in nonepithelial cells.

Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.

Neurotransmitter receptors located on or near presynaptic terminals or varicosities. Presynaptic receptors which bind transmitter molecules released by the terminal itself are termed AUTORECEPTORS.

Membrane proteins whose primary function is to facilitate the transport of molecules across a biological membrane. Included in this broad category are proteins involved in active transport (BIOLOGICAL TRANSPORT, ACTIVE), facilitated transport and ION CHANNELS.

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.

Drugs used to prevent SEIZURES or reduce their severity.

Female germ cells derived from OOGONIA and termed OOCYTES when they enter MEIOSIS. The primary oocytes begin meiosis but are arrested at the diplotene state until OVULATION at PUBERTY to give rise to haploid secondary oocytes or ova (OVUM).

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.

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.

An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.

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.

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.

A group of compounds that are derivatives of methoxybenzene and contain the general formula R-C7H7O.

Pinched-off nerve endings and their contents of vesicles and cytoplasm together with the attached subsynaptic area of the membrane of the post-synaptic cell. They are largely artificial structures produced by fractionation after selective centrifugation of nervous tissue homogenates.

The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.

Therapeutic introduction of ions of soluble salts into tissues by means of electric current. In medical literature it is commonly used to indicate the process of increasing the penetration of drugs into surface tissues by the application of electric current. It has nothing to do with ION EXCHANGE; AIR IONIZATION nor PHONOPHORESIS, none of which requires current.

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."

An enzyme that plays a role in the GLUTAMATE and butanoate metabolism pathways by catalyzing the oxidation of succinate semialdehyde to SUCCINATE using NAD+ as a coenzyme. Deficiency of this enzyme, causes 4-hydroxybutyricaciduria, a rare inborn error in the metabolism of the neurotransmitter 4-aminobutyric acid (GABA).

Compounds that contain the radical R2C=N.OH derived from condensation of ALDEHYDES or KETONES with HYDROXYLAMINE. Members of this group are CHOLINESTERASE REACTIVATORS.

An amino acid formed in vivo by the degradation of dihydrouracil and carnosine. Since neuronal uptake and neuronal receptor sensitivity to beta-alanine have been demonstrated, the compound may be a false transmitter replacing GAMMA-AMINOBUTYRIC ACID. A rare genetic disorder, hyper-beta-alaninemia, has been reported.

A very loosely defined group of drugs that tend to reduce the activity of the central nervous system. The major groups included here are ethyl alcohol, anesthetics, hypnotics and sedatives, narcotics, and tranquilizing agents (antipsychotics and antianxiety agents).

The largest portion of the CEREBRAL CORTEX in which the NEURONS are arranged in six layers in the mammalian brain: molecular, external granular, external pyramidal, internal granular, internal pyramidal and multiform layers.

Extensions of the nerve cell body. They are short and branched and receive stimuli from other NEURONS.

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.

The representation of the phylogenetically oldest part of the corpus striatum called the paleostriatum. It forms the smaller, more medial part of the lentiform nucleus.

Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.

An inhibitor of glutamate decarboxylase and an antagonist of GAMMA-AMINOBUTYRIC ACID. It is used to induce convulsions in experimental animals.

The action of a drug that may affect the activity, metabolism, or toxicity of another drug.

Amino derivatives of caproic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the amino caproic acid structure.

Cell membrane glycoproteins that form channels to selectively pass chloride ions. Nonselective blockers include FENAMATES; ETHACRYNIC ACID; and TAMOXIFEN.

Agents that are capable of inducing a total or partial loss of sensation, especially tactile sensation and pain. They may act to induce general ANESTHESIA, in which an unconscious state is achieved, or may act locally to induce numbness or lack of sensation at a targeted site.

The voltages across pre- or post-SYNAPTIC MEMBRANES.

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.

The ten-layered nervous tissue membrane of the eye. It is continuous with the OPTIC NERVE and receives images of external objects and transmits visual impulses to the brain. Its outer surface is in contact with the CHOROID and the inner surface with the VITREOUS BODY. The outer-most layer is pigmented, whereas the inner nine layers are transparent.

The modification of the reactivity of ENZYMES by the binding of effectors to sites (ALLOSTERIC SITES) on the enzymes other than the substrate BINDING SITES.

INTERNEURONS of the vertebrate RETINA containing two processes. They receive inputs from the RETINAL PHOTORECEPTOR CELLS and send outputs to the RETINAL GANGLION CELLS. The bipolar cells also make lateral connections in the retina with the RETINAL HORIZONTAL CELLS and with the AMACRINE CELLS.

A technique for maintenance or growth of animal organs in vitro. It refers to three-dimensional cultures of undisaggregated tissue retaining some or all of the histological features of the tissue in vivo. (Freshney, Culture of Animal Cells, 3d ed, p1)

Drugs that bind to and activate excitatory amino acid receptors.

One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.

A region in the MESENCEPHALON which is dorsomedial to the SUBSTANTIA NIGRA and ventral to the RED NUCLEUS. The mesocortical and mesolimbic dopaminergic systems originate here, including an important projection to the NUCLEUS ACCUMBENS. Overactivity of the cells in this area has been suspected to contribute to the positive symptoms of SCHIZOPHRENIA.

Low molecular weight, calcium binding muscle proteins. Their physiological function is possibly related to the contractile process.

(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 chemicals derived from barbituric acid or thiobarbituric acid. Many of these are GABA MODULATORS used as HYPNOTICS AND SEDATIVES, as ANESTHETICS, or as ANTICONVULSANTS.

A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.

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.

The opening and closing of ion channels due to a stimulus. The stimulus can be a change in membrane potential (voltage-gated), drugs or chemical transmitters (ligand-gated), or a mechanical deformation. Gating is thought to involve conformational changes of the ion channel which alters selective permeability.

The observable response an animal makes to any situation.

The electrical properties, characteristics of living organisms, and the processes of organisms or their parts that are involved in generating and responding to electrical charges.

Agents that induce various degrees of analgesia; depression of consciousness, circulation, and respiration; relaxation of skeletal muscle; reduction of reflex activity; and amnesia. There are two types of general anesthetics, inhalation and intravenous. With either type, the arterial concentration of drug required to induce anesthesia varies with the condition of the patient, the desired depth of anesthesia, and the concomitant use of other drugs. (From AMA Drug Evaluations Annual, 1994, p.173)

A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)

Transport proteins that carry specific substances in the blood or across cell membranes.

INTERNEURONS of the vertebrate RETINA. They integrate, modulate, and interpose a temporal domain in the visual message presented to the RETINAL GANGLION CELLS, with which they synapse in the inner plexiform layer.

Histochemical localization of immunoreactive substances using labeled antibodies as reagents.

Branch-like terminations of NERVE FIBERS, sensory or motor NEURONS. Endings of sensory neurons are the beginnings of afferent pathway to the CENTRAL NERVOUS SYSTEM. Endings of motor neurons are the terminals of axons at the muscle cells. Nerve endings which release neurotransmitters are called PRESYNAPTIC TERMINALS.

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)

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 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.

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.

GRAY MATTER situated above the GYRUS HIPPOCAMPI. It is composed of three layers. The molecular layer is continuous with the HIPPOCAMPUS in the hippocampal fissure. The granular layer consists of closely arranged spherical or oval neurons, called GRANULE CELLS, whose AXONS pass through the polymorphic layer ending on the DENDRITES of PYRAMIDAL CELLS in the hippocampus.

One of four subsections of the hippocampus described by Lorente de No, located furthest from the DENTATE GYRUS.

Neural tracts connecting one part of the nervous system with another.

The ability of a substrate to allow the passage of ELECTRONS.

Postsynaptic potentials generated from a release of neurotransmitters from a presynaptic nerve terminal in the absence of an ACTION POTENTIAL. They may be m.e.p.p.s (miniature EXCITATORY POSTSYNAPTIC POTENTIALS) or m.i.p.p.s (miniature INHIBITORY POSTSYNAPTIC POTENTIALS).

An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.

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.

The output neurons of the cerebellar cortex.

An organochlorine insecticide whose use has been cancelled or suspended in the United States. It has been used to control locusts, tropical disease vectors, in termite control by direct soil injection, and non-food seed and plant treatment. (From HSDB)

An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.

Cell membranes associated with synapses. Both presynaptic and postsynaptic membranes are included along with their integral or tightly associated specializations for the release or reception of transmitters.

Common name for Carassius auratus, a type of carp (CARPS).

Membrane transporters that co-transport two or more dissimilar molecules in the same direction across a membrane. Usually the transport of one ion or molecule is against its electrochemical gradient and is "powered" by the movement of another ion or molecule with its electrochemical gradient.

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.

Almond-shaped group of basal nuclei anterior to the INFERIOR HORN OF THE LATERAL VENTRICLE of the TEMPORAL LOBE. The amygdala is part of the limbic system.

An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).

Toluenes in which one hydrogen of the methyl group is substituted by an amino group. Permitted are any substituents on the benzene ring or the amino group.

Ventral part of the DIENCEPHALON extending from the region of the OPTIC CHIASM to the caudal border of the MAMMILLARY BODIES and forming the inferior and lateral walls of the THIRD VENTRICLE.

A subclass of symporters that specifically transport SODIUM CHLORIDE and/or POTASSIUM CHLORIDE across cellular membranes in a tightly coupled process.

Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.

A group of peptide antibiotics from BACILLUS brevis. Gramicidin C or S is a cyclic, ten-amino acid polypeptide and gramicidins A, B, D are linear. Gramicidin is one of the two principal components of TYROTHRICIN.

A class of drugs that act by inhibition of sodium influx through cell membranes. Blockade of sodium channels slows the rate and amplitude of initial rapid depolarization, reduces cell excitability, and reduces conduction velocity.

Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.

The capacity of the NERVOUS SYSTEM to change its reactivity as the result of successive activations.

Elements of limited time intervals, contributing to particular results or situations.

Amino acids with uncharged R groups or side chains.

The lower portion of the BRAIN STEM. It is inferior to the PONS and anterior to the CEREBELLUM. Medulla oblongata serves as a relay station between the brain and the spinal cord, and contains centers for regulating respiratory, vasomotor, cardiac, and reflex activities.

A sulfamyl diuretic.

Theoretical representations that simulate the behavior or activity of the neurological system, processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment.

A childhood seizure disorder characterized by rhythmic electrical brain discharges of generalized onset. Clinical features include a sudden cessation of ongoing activity usually without loss of postural tone. Rhythmic blinking of the eyelids or lip smacking frequently accompanies the SEIZURES. The usual duration is 5-10 seconds, and multiple episodes may occur daily. Juvenile absence epilepsy is characterized by the juvenile onset of absence seizures and an increased incidence of myoclonus and tonic-clonic seizures. (Menkes, Textbook of Child Neurology, 5th ed, p736)

An outbred strain of rats developed in 1915 by crossing several Wistar Institute white females with a wild gray male. Inbred strains have been derived from this original outbred strain, including Long-Evans cinnamon rats (RATS, INBRED LEC) and Otsuka-Long-Evans-Tokushima Fatty rats (RATS, INBRED OLETF), which are models for Wilson's disease and non-insulin dependent diabetes mellitus, respectively.

Changes in the amounts of various chemicals (neurotransmitters, receptors, enzymes, and other metabolites) specific to the area of the central nervous system contained within the head. These are monitored over time, during sensory stimulation, or under different disease states.

GRAY MATTER located in the dorsomedial part of the MEDULLA OBLONGATA associated with the solitary tract. The solitary nucleus receives inputs from most organ systems including the terminations of the facial, glossopharyngeal, and vagus nerves. It is a major coordinator of AUTONOMIC NERVOUS SYSTEM regulation of cardiovascular, respiratory, gustatory, gastrointestinal, and chemoreceptive aspects of HOMEOSTASIS. The solitary nucleus is also notable for the large number of NEUROTRANSMITTERS which are found therein.

Ultrashort-acting anesthetics that are used for induction. Loss of consciousness is rapid and induction is pleasant, but there is no muscle relaxation and reflexes frequently are not reduced adequately. Repeated administration results in accumulation and prolongs the recovery time. Since these agents have little if any analgesic activity, they are seldom used alone except in brief minor procedures. (From AMA Drug Evaluations Annual, 1994, p174)

A meshlike structure composed of interconnecting nerve cells that are separated at the synaptic junction or joined to one another by cytoplasmic processes. In invertebrates, for example, the nerve net allows nerve impulses to spread over a wide area of the net because synapses can pass information in any direction.

Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.

A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.

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.

Several groups of nuclei in the thalamus that serve as the major relay centers for sensory impulses in the brain.

A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.

The physical activity of a human or an animal as a behavioral phenomenon.

Gated, ion-selective glycoproteins that traverse membranes. The stimulus for ION CHANNEL GATING can be due to a variety of stimuli such as LIGANDS, a TRANSMEMBRANE POTENTIAL DIFFERENCE, mechanical deformation or through INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS.

A region extending from the PONS & MEDULLA OBLONGATA through the MESENCEPHALON, characterized by a diversity of neurons of various sizes and shapes, arranged in different aggregations and enmeshed in a complicated fiber network.

An aquatic genus of the family, Pipidae, occurring in Africa and distinguished by having black horny claws on three inner hind toes.

The black substance in the ventral midbrain or the nucleus of cells containing the black substance. These cells produce DOPAMINE, an important neurotransmitter in regulation of the sensorimotor system and mood. The dark colored MELANIN is a by-product of dopamine synthesis.

Ovoid body resting on the CRIBRIFORM PLATE of the ethmoid bone where the OLFACTORY NERVE terminates. The olfactory bulb contains several types of nerve cells including the mitral cells, on whose DENDRITES the olfactory nerve synapses, forming the olfactory glomeruli. The accessory olfactory bulb, which receives the projection from the VOMERONASAL ORGAN via the vomeronasal nerve, is also included here.

The rate dynamics in chemical or physical systems.

A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.

A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.

Laboratory mice that have been produced from a genetically manipulated EGG or EMBRYO, MAMMALIAN.

An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.

A species of the family Ranidae which occurs primarily in Europe and is used widely in biomedical research.

Transmitter receptors on or near presynaptic terminals (or varicosities) which are sensitive to the transmitter(s) released by the terminal itself. Receptors for the hormones released by hormone-releasing cells are also included.

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.

The parts of a macromolecule that directly participate in its specific combination with another molecule.

Region of hypothalamus between the ANTERIOR COMMISSURE and OPTIC CHIASM.

The rostral part of the frontal lobe, bounded by the inferior precentral fissure in humans, which receives projection fibers from the MEDIODORSAL NUCLEUS OF THE THALAMUS. The prefrontal cortex receives afferent fibers from numerous structures of the DIENCEPHALON; MESENCEPHALON; and LIMBIC SYSTEM as well as cortical afferents of visual, auditory, and somatic origin.

The part of the brain that connects the CEREBRAL HEMISPHERES with the SPINAL CORD. It consists of the MESENCEPHALON; PONS; and MEDULLA OBLONGATA.

A family of inwardly-rectifying potassium channels that are activated by PERTUSSIS TOXIN sensitive G-PROTEIN-COUPLED RECEPTORS. GIRK potassium channels are primarily activated by the complex of GTP-BINDING PROTEIN BETA SUBUNITS and GTP-BINDING PROTEIN GAMMA SUBUNITS.

A convulsant primarily used in experimental animals. It was formerly used to induce convulsions as a alternative to electroshock therapy.

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.

Why are there so few resistance-associated mutations in insecticide target genes? (1/3892)

The genes encoding the three major targets of conventional insecticides are: Rdl, which encodes a gamma-aminobutyric acid receptor subunit (RDL); para, which encodes a voltage-gated sodium channel (PARA); and Ace, which encodes insect acetylcholinesterase (AChE). Interestingly, despite the complexity of the encoded receptors or enzymes, very few amino acid residues are replaced in different resistant insects: one within RDL, two within PARA and three or more within AChE. Here we examine the possible reasons underlying this extreme conservation by looking at the aspects of receptor and/or enzyme function that may constrain replacements to such a limited number of residues. (+info)

Somatic recording of GABAergic autoreceptor current in cerebellar stellate and basket cells. (2/3892)

Patch-clamp recordings were performed from stellate and basket cells in rat cerebellar slices. Under somatic voltage clamp, short depolarizing pulses were applied to elicit action potentials in the axon. After the action potential, a bicuculline- and Cd2+-sensitive current transient was observed. A similar response was obtained when eliciting axonal firing by extracellular stimulation. With an isotonic internal Cl- solution, the peak amplitude of this current varied linearly with the holding potential, yielding an extrapolated reversal potential of -20 to 0 mV. Unlike synaptic or autaptic GABAergic currents obtained in the same preparation, the current transient had a slow rise-time and a low variability between trials. This current was blocked when 10 mM BAPTA was included in the recording solution. In some experiments, the current transient elicited axonal action potentials. The current transient was reliably observed in animals aged 12-15 d, with a mean amplitude of 82 pA at -70 mV, but was small and rare in the age group 29-49 d. Numerical simulations could account for all properties of the current transient by assuming that an action potential activates a distributed GABAergic conductance in the axon. The actual conductance is probably restricted to release sites, with an estimated mean presynaptic current response of 10 pA per site (-70 mV, age 12-15 d). We conclude that in developing rats, stellate and basket cell axons have a high density of GABAergic autoreceptors and that a sizable fraction of the corresponding current can be measured from the soma. (+info)

Peripheral-type benzodiazepine receptor (PBR) in human breast cancer: correlation of breast cancer cell aggressive phenotype with PBR expression, nuclear localization, and PBR-mediated cell proliferation and nuclear transport of cholesterol. (3/3892)

Aberrant cell proliferation and increased invasive and metastatic behavior are hallmarks of the advancement of breast cancer. Numerous studies implicate a role for cholesterol in the mechanisms underlying cell proliferation and cancer progression. The peripheral-type benzodiazepine receptor (PBR) is an Mr 18,000 protein primarily localized to the mitochondria. PBR mediates cholesterol transport across the mitochondrial membranes in steroidogenic cells. A role for PBR in the regulation of tumor cell proliferation has also been shown. In this study, we examined the expression, characteristics, localization, and function of PBR in a battery of human breast cancer cell lines differing in their invasive and chemotactic potential as well as in several human tissue biopsies. Expression of PBR ligand binding and mRNA was dramatically increased in the highly aggressive cell lines, such as MDA-231, relative to nonaggressive cell lines, such as MCF-7. PBR was also found to be expressed at high levels in aggressive metastatic human breast tumor biopsies compared with normal breast tissues. Subcellular localization with both antibodies and a fluorescent PBR drug ligand revealed that PBR from the MDA-231 cell line as well as from aggressive metastatic human breast tumor biopsies localized primarily in and around the nucleus. This localization is in direct contrast to the largely cytoplasmic localization seen in MCF-7 cells, normal breast tissue, and to the typical mitochondrial localization seen in mouse tumor Leydig cells. Pharmacological characterization of the receptor and partial nucleotide sequencing of PBR cDNA revealed that the MDA-231 PBR is similar, although not identical, to previously described PBR. Addition of high affinity PBR drug ligands to MDA-231 cells increased the incorporation of bromodeoxyuridine into the cells in a dose-dependent manner, suggesting a role for PBR in the regulation of MDA-231 cell proliferation. Cholesterol uptake into isolated MDA-231 nuclei was found to be 30% greater than into MCF-7 nuclei. High-affinity PBR drug ligands regulated the levels of cholesterol present in MDA-231 nuclei but not in MCF-7. In addition, the PBR-dependent MDA-231 cell proliferation was found to highly correlate (r = -0.99) with the PBR-mediated changes in nuclear membrane cholesterol levels. In conclusion, these data suggest that PBR expression, nuclear localization, and PBR-mediated cholesterol transport into the nucleus are involved in human breast cancer cell proliferation and aggressive phenotype expression, thus participating in the advancement of the disease. (+info)

Synaptic activation of GABAA receptors induces neuronal uptake of Ca2+ in adult rat hippocampal slices. (4/3892)

Synaptically evoked transmembrane movements of Ca2+ in the adult CNS have almost exclusively been attributed to activation of glutamate receptor channels and the consequent triggering of voltage-gated calcium channels (VGCCs). Using microelectrodes for measuring free extracellular Ca2+ ([Ca2+]o) and extracellular space (ECS) volume, we show here for the first time that synaptic stimulation of gamma-aminobutyric acid-A (GABAA) receptors can result in a decrease in [Ca2+]o in adult rat hippocampal slices. High-frequency stimulation (100-200 Hz, 0.4-0.5 s) applied in stratum radiatum close (+info)

Retinal input induces three firing patterns in neurons of the superficial superior colliculus of neonatal rats. (5/3892)

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

Postnatal development of hippocampal dentate granule cell gamma-aminobutyric acidA receptor pharmacological properties. (6/3892)

Postnatal development of hippocampal dentate granule cell gamma-aminobutyric acidA (GABAA) receptor pharmacological properties was studied. Granule cells were acutely isolated from hippocampi of 7- to 14- and 45- to 52-day-old rats, and whole cell patch-clamp recordings were obtained. The sensitivity of GABAA receptors to GABA and modulation of GABAA receptor currents by benzodiazepines (BZ), zinc, furosemide, and loreclezole was studied. Multiple changes in the pharmacological properties of dentate granule-cell GABAA receptors occurred during the first 52 days of postnatal development: GABA-evoked maximal current increased with postnatal age; GABAA receptors changed from BZ type 3 in young rats to BZ type 1 in adult rats; furosemide and zinc inhibited GABAA receptor currents in young rats but not in adult rats; the fraction of cells that expressed loreclezole-sensitive GABAA receptors increased with postnatal age. These findings suggest that dentate granule cells in young and adult animals express pharmacologically distinct GABAA receptors and that the postnatal development of these receptors is prolonged, lasting at least 45 days. Comparison with the previously reported pharmacological properties of GABAA receptors on dentate granule cells acutely isolated from hippocampi of 28- to 35-day-old rats suggests that receptors expressed at that age have properties intermediate between young and adult rats. (+info)

Dopamine receptor subtypes modulate olfactory bulb gamma-aminobutyric acid type A receptors. (7/3892)

The gamma-aminobutyric acid type A (GABAA) receptor is the predominant Cl- channel protein mediating inhibition in the olfactory bulb and elsewhere in the mammalian brain. The olfactory bulb is rich in neurons containing both GABA and dopamine. Dopamine D1 and D2 receptors are also highly expressed in this brain region with a distinct and complementary distribution pattern. This distribution suggests that dopamine may control the GABAergic inhibitory processing of odor signals, possibly via different signal-transduction mechanisms. We have observed that GABAA receptors in the rat olfactory bulb are differentially modulated by dopamine in a cell-specific manner. Dopamine reduced the currents through GABA-gated Cl- channels in the interneurons, presumably granule cells. This action was mediated via D1 receptors and involved phosphorylation of GABAA receptors by protein kinase A. Enhancement of GABA responses via activation of D2 dopamine receptors and phosphorylation of GABAA receptors by protein kinase C was observed in mitral/tufted cells. Decreasing or increasing the binding affinity for GABA appears to underlie the modulatory effects of dopamine via distinct receptor subtypes. This dual action of dopamine on inhibitory GABAA receptor function in the rat olfactory bulb could be instrumental in odor detection and discrimination, olfactory learning, and ultimately odotopic memory formation. (+info)

Regional differences in the inhibition of mouse in vivo [3H]Ro 15-1788 binding reflect selectivity for alpha 1 versus alpha 2 and alpha 3 subunit-containing GABAA receptors. (8/3892)

The benzodiazepines flunitrazepam, diazepam, and Ro 15-1788 and the beta-carboline DMCM bind with equivalent affinity to the benzodiazepine binding site of GABAA receptors containing different alpha subunits (i.e., alpha 1, alpha 2, alpha 3, or alpha 5); whereas, the triazolopyridazine CL 218,872 and imidazopyridine zolpidem have higher affinity for alpha 1 subunit-containing GABAA receptors. In the present study, the in vivo binding of [3H]Ro 15-1788 in mouse cerebellum and spinal cord was used to establish the occupancy of the benzodiazepine binding site of GABAA receptors containing primarily alpha 1 and alpha 2/alpha 3 subunits, respectively. Thus, the nonselective compounds flunitrazepam, diazepam, and DMCM all produced a similar inhibition of binding in cerebellum and spinal cord (respective ID50 values of 0.2 to 0.3 mg/kg, 2 mg/kg, and 10 mg/kg i.p.); whereas, the alpha 1 selective compounds CL 218,872 and zolpidem were more potent at inhibiting [3H]Ro 15-1788 binding in the cerebellum (ID50 values 4.5 mg/kg and 10 mg/kg i.p.) compared to the spinal cord (ID50 values 12 mg/kg and > 30 mg/kg i.p.). Thus, the reduction of in vivo f[3H]Ro 15-1788 binding in tissues containing alpha 1 and alpha 2/alpha 3 receptor populations reflects the in vitro affinities of subtype selective compounds and should help to interpret the behavioral profile of such compounds. (+info)

There are many different types of seizures, each with its own unique set of symptoms. Some common types of seizures include:

1. Generalized seizures: These seizures affect both sides of the brain and can cause a range of symptoms, including convulsions, loss of consciousness, and muscle stiffness.
2. Focal seizures: These seizures affect only one part of the brain and can cause more specific symptoms, such as weakness or numbness in a limb, or changes in sensation or vision.
3. Tonic-clonic seizures: These seizures are also known as grand mal seizures and can cause convulsions, loss of consciousness, and muscle stiffness.
4. Absence seizures: These seizures are also known as petit mal seizures and can cause a brief loss of consciousness or staring spell.
5. Myoclonic seizures: These seizures can cause sudden, brief muscle jerks or twitches.
6. Atonic seizures: These seizures can cause a sudden loss of muscle tone, which can lead to falls or drops.
7. Lennox-Gastaut syndrome: This is a rare and severe form of epilepsy that can cause multiple types of seizures, including tonic, atonic, and myoclonic seizures.

Seizures can be diagnosed through a combination of medical history, physical examination, and diagnostic tests such as electroencephalography (EEG) or imaging studies. Treatment for seizures usually involves anticonvulsant medications, but in some cases, surgery or other interventions may be necessary.

Overall, seizures are a complex and multifaceted symptom that can have a significant impact on an individual's quality of life. It is important to seek medical attention if you or someone you know is experiencing seizures, as early diagnosis and treatment can help to improve outcomes and reduce the risk of complications.

There are many different types of epilepsy, each with its own unique set of symptoms and characteristics. Some common forms of epilepsy include:

1. Generalized Epilepsy: This type of epilepsy affects both sides of the brain and can cause a range of seizure types, including absence seizures, tonic-clonic seizures, and atypical absence seizures.
2. Focal Epilepsy: This type of epilepsy affects only one part of the brain and can cause seizures that are localized to that area. There are several subtypes of focal epilepsy, including partial seizures with complex symptoms and simple partial seizures.
3. Tonic-Clonic Epilepsy: This type of epilepsy is also known as grand mal seizures and can cause a loss of consciousness, convulsions, and muscle stiffness.
4. Lennox-Gastaut Syndrome: This is a rare and severe form of epilepsy that typically develops in early childhood and can cause multiple types of seizures, including tonic, atonic, and myoclonic seizures.
5. Dravet Syndrome: This is a rare genetic form of epilepsy that typically develops in infancy and can cause severe, frequent seizures.
6. Rubinstein-Taybi Syndrome: This is a rare genetic disorder that can cause intellectual disability, developmental delays, and various types of seizures.
7. Other forms of epilepsy include Absence Epilepsy, Myoclonic Epilepsy, and Atonic Epilepsy.

The symptoms of epilepsy can vary widely depending on the type of seizure disorder and the individual affected. Some common symptoms of epilepsy include:

1. Seizures: This is the most obvious symptom of epilepsy and can range from mild to severe.
2. Loss of consciousness: Some people with epilepsy may experience a loss of consciousness during a seizure, while others may remain aware of their surroundings.
3. Confusion and disorientation: After a seizure, some people with epilepsy may feel confused and disoriented.
4. Memory loss: Seizures can cause short-term or long-term memory loss.
5. Fatigue: Epilepsy can cause extreme fatigue, both during and after a seizure.
6. Emotional changes: Some people with epilepsy may experience emotional changes, such as anxiety, depression, or mood swings.
7. Cognitive changes: Epilepsy can affect cognitive function, including attention, memory, and learning.
8. Sleep disturbances: Some people with epilepsy may experience sleep disturbances, such as insomnia or sleepiness.
9. Physical symptoms: Depending on the type of seizure, people with epilepsy may experience physical symptoms such as muscle weakness, numbness or tingling, and sensory changes.
10. Social isolation: Epilepsy can cause social isolation due to fear of having a seizure in public or stigma associated with the condition.

It's important to note that not everyone with epilepsy will experience all of these symptoms, and some people may have different symptoms depending on the type of seizure they experience. Additionally, some people with epilepsy may experience additional symptoms not listed here.

The diagnosis of absence epilepsy is typically made based on a combination of clinical findings, including:
-A history of recurrent brief loss of awareness or staring spells
-Normal neurological examination between episodes
-Abnormal EEG activity during seizures (spikes or sharp waves)

Treatment for absence epilepsy usually involves medication, such as ethosuximide, valproic acid, or lamotrigine. In some cases, surgery may be considered if medications are ineffective or have significant side effects.

It is important to note that absence epilepsy can be a challenging condition to diagnose and treat, as the spells can be difficult to distinguish from other conditions such as daydreaming or attention deficit hyperactivity disorder (ADHD).

There are two main types of status epilepticus:

1. Generalized status epilepticus: This type affects the entire brain and is characterized by severe convulsions, loss of consciousness, and muscle stiffness.
2. Focal status epilepticus: This type affects only one part of the brain and can cause more subtle symptoms, such as weakness or numbness in a limb, speech difficulties, or confusion.

The diagnosis of status epilepticus is based on clinical findings, medical history, and electroencephalography (EEG) recordings. Treatment typically involves prompt administration of anticonvulsant medications, such as benzodiazepines or barbiturates, to control seizures and prevent further brain damage. In severe cases, sedation, mechanical ventilation, or anesthesia may be required to support the patient's vital functions.

The prognosis for status epilepticus depends on several factors, including the underlying cause, the severity of the seizure, and the promptness and effectiveness of treatment. In general, the earlier the treatment is initiated, the better the outcome. However, long-term neurological and cognitive deficits can occur in some cases.

Preventive measures for status epilepticus include proper management of underlying conditions that may trigger seizures, such as epilepsy or head trauma, and avoiding triggers like alcohol or drugs. Additionally, prompt medical attention should be sought if seizure warning signs are present, such as changes in sensation, confusion, or convulsions.

1) They share similarities with humans: Many animal species share similar biological and physiological characteristics with humans, making them useful for studying human diseases. For example, mice and rats are often used to study diseases such as diabetes, heart disease, and cancer because they have similar metabolic and cardiovascular systems to humans.

2) They can be genetically manipulated: Animal disease models can be genetically engineered to develop specific diseases or to model human genetic disorders. This allows researchers to study the progression of the disease and test potential treatments in a controlled environment.

3) They can be used to test drugs and therapies: Before new drugs or therapies are tested in humans, they are often first tested in animal models of disease. This allows researchers to assess the safety and efficacy of the treatment before moving on to human clinical trials.

4) They can provide insights into disease mechanisms: Studying disease models in animals can provide valuable insights into the underlying mechanisms of a particular disease. This information can then be used to develop new treatments or improve existing ones.

5) Reduces the need for human testing: Using animal disease models reduces the need for human testing, which can be time-consuming, expensive, and ethically challenging. However, it is important to note that animal models are not perfect substitutes for human subjects, and results obtained from animal studies may not always translate to humans.

6) They can be used to study infectious diseases: Animal disease models can be used to study infectious diseases such as HIV, TB, and malaria. These models allow researchers to understand how the disease is transmitted, how it progresses, and how it responds to treatment.

7) They can be used to study complex diseases: Animal disease models can be used to study complex diseases such as cancer, diabetes, and heart disease. These models allow researchers to understand the underlying mechanisms of the disease and test potential treatments.

8) They are cost-effective: Animal disease models are often less expensive than human clinical trials, making them a cost-effective way to conduct research.

9) They can be used to study drug delivery: Animal disease models can be used to study drug delivery and pharmacokinetics, which is important for developing new drugs and drug delivery systems.

10) They can be used to study aging: Animal disease models can be used to study the aging process and age-related diseases such as Alzheimer's and Parkinson's. This allows researchers to understand how aging contributes to disease and develop potential treatments.

Epilepsy, temporal lobe can cause a variety of seizure types, including:

1. Partial seizures: These are seizures that affect only one part of the brain, such as the temporal lobe.
2. Simple partial seizures: These are seizures that do not involve convulsions or loss of consciousness.
3. Complex partial seizures: These are seizures that involve impaired awareness or altered perception, and may involve convulsions or muscle stiffness.
4. Tonic-clonic seizures (formerly known as grand mal seizures): These are seizures that involve convulsions, loss of consciousness, and muscle stiffness.

The symptoms of epilepsy, temporal lobe can vary depending on the location of the seizure focus within the temporal lobe and the individual's age, but may include:

1. Auras (sensory disturbances such as flashing lights or unusual smells)
2. Confusion or disorientation
3. Memory loss or difficulty with memory
4. Emotional changes (such as fear, anxiety, or euphoria)
5. Speech difficulties
6. Muscle stiffness or weakness
7. Coordination problems
8. Vision changes (such as blurred vision or double vision)
9. Hearing changes (such as ringing in the ears)
10. Numbness or tingling sensations

Epilepsy, temporal lobe is typically diagnosed using a combination of medical history, physical examination, and diagnostic tests such as electroencephalography (EEG) or magnetic resonance imaging (MRI). Treatment options may include medication, surgery, or lifestyle modifications.

There are several types of ataxia, each with different symptoms and causes. Some common forms of ataxia include:

1. Spinocerebellar ataxia (SCA): This is the most common form of ataxia and is caused by a degeneration of the cerebellum and spinal cord. It can cause progressive weakness, loss of coordination, and difficulty with speaking and swallowing.
2. Friedreich's ataxia: This is the second most common form of ataxia and is caused by a deficiency of vitamin E in the body. It can cause weakness in the legs, difficulty walking, and problems with speech and language.
3. Ataxia-telangiectasia (AT): This is a rare form of ataxia that is caused by a gene mutation. It can cause progressive weakness, loss of coordination, and an increased risk of developing cancer.
4. Acute cerebellar ataxia: This is a sudden and temporary form of ataxia that can be caused by a variety of factors such as infections, injuries, or certain medications.
5. Drug-induced ataxia: Certain medications can cause ataxia as a side effect.
6. Vitamin deficiency ataxia: Deficiencies in vitamins such as vitamin B12 or folate can cause ataxia.
7. Metabolic disorders: Certain metabolic disorders such as hypothyroidism, hyperthyroidism, and hypoglycemia can cause ataxia.
8. Stroke or brain injury: Ataxia can be a result of a stroke or brain injury.
9. Multiple system atrophy (MSA): This is a rare progressive neurodegenerative disorder that can cause ataxia, parkinsonism, and autonomic dysfunction.
10. Spinocerebellar ataxia (SCA): This is a group of rare genetic disorders that can cause progressive cerebellar ataxia, muscle wasting, and other signs and symptoms.

It's important to note that this is not an exhaustive list and there may be other causes of ataxia not mentioned here. If you suspect you or someone you know may have ataxia, it is important to consult a healthcare professional for proper diagnosis and treatment.

* Anxiety
* Depression
* Fatigue
* Insomnia
* Muscle and bone pain
* Nausea and vomiting
* Seizures (in severe cases)
* Sweating
* Tremors

The specific symptoms of substance withdrawal syndrome can vary depending on the substance being withdrawn from, but some common symptoms include:

* Alcohol: tremors, anxiety, insomnia, nausea and vomiting, headaches, and seizures
* Opioids: withdrawal symptoms can include anxiety, muscle aches, sweating, nausea and vomiting, diarrhea, and depression
* Benzodiazepines: withdrawal symptoms can include anxiety, insomnia, tremors, and seizures

The diagnosis of substance withdrawal syndrome is typically made based on the patient's history of substance use and the presence of withdrawal symptoms. A healthcare provider may also order laboratory tests to rule out other conditions that may be causing the symptoms. Treatment for substance withdrawal syndrome usually involves supportive care, such as rest, hydration, and pain management, as well as medication to manage withdrawal symptoms. In some cases, medical professionals may also recommend a gradual tapering of the substance over a period of time to minimize withdrawal symptoms.

It is important for individuals who are experiencing withdrawal symptoms to seek medical attention as soon as possible, as untreated withdrawal can lead to serious complications, such as seizures and dehydration. With appropriate treatment, most individuals with substance withdrawal syndrome can recover fully and successfully overcome their addiction.

The term "schizophrenia" was first used by the Swiss psychiatrist Eugen Bleuler in 1908 to describe the splitting of mental functions, which he believed was a key feature of the disorder. The word is derived from the Greek words "schizein," meaning "to split," and "phrenos," meaning "mind."

There are several subtypes of schizophrenia, including:

1. Paranoid Schizophrenia: Characterized by delusions of persecution and suspicion, and a tendency to be hostile and defensive.
2. Hallucinatory Schizophrenia: Characterized by hearing voices or seeing things that are not there.
3. Disorganized Schizophrenia: Characterized by disorganized thinking and behavior, and a lack of motivation or interest in activities.
4. Catatonic Schizophrenia: Characterized by immobility, mutism, and other unusual movements or postures.
5. Undifferentiated Schizophrenia: Characterized by a combination of symptoms from the above subtypes.

The exact cause of schizophrenia is still not fully understood, but it is believed to involve a combination of genetic, environmental, and neurochemical factors. It is important to note that schizophrenia is not caused by poor parenting or a person's upbringing.

There are several risk factors for developing schizophrenia, including:

1. Genetics: A person with a family history of schizophrenia is more likely to develop the disorder.
2. Brain chemistry: Imbalances in neurotransmitters such as dopamine and serotonin have been linked to schizophrenia.
3. Prenatal factors: Factors such as maternal malnutrition or exposure to certain viruses during pregnancy may increase the risk of schizophrenia in offspring.
4. Childhood trauma: Traumatic events during childhood, such as abuse or neglect, have been linked to an increased risk of developing schizophrenia.
5. Substance use: Substance use has been linked to an increased risk of developing schizophrenia, particularly cannabis and other psychotic substances.

There is no cure for schizophrenia, but treatment can help manage symptoms and improve quality of life. Treatment options include:

1. Medications: Antipsychotic medications are the primary treatment for schizophrenia. They can help reduce positive symptoms such as hallucinations and delusions, and negative symptoms such as a lack of motivation or interest in activities.
2. Therapy: Cognitive-behavioral therapy (CBT) and other forms of talk therapy can help individuals with schizophrenia manage their symptoms and improve their quality of life.
3. Social support: Support from family, friends, and support groups can be an important part of the treatment plan for individuals with schizophrenia.
4. Self-care: Engaging in activities that bring pleasure and fulfillment, such as hobbies or exercise, can help individuals with schizophrenia improve their overall well-being.

It is important to note that schizophrenia is a complex condition, and treatment should be tailored to the individual's specific needs and circumstances. With appropriate treatment and support, many people with schizophrenia are able to lead fulfilling lives and achieve their goals.

Hypothermia can be mild, moderate, or severe. Mild hypothermia is characterized by shivering and a body temperature of 95 to 97 degrees Fahrenheit (32 to 36.1 degrees Celsius). Moderate hypothermia has a body temperature of 82 to 94 degrees Fahrenheit (28 to 34 degrees Celsius), and the person may appear lethargic, drowsy, or confused. Severe hypothermia is characterized by a body temperature below 82 degrees Fahrenheit (28 degrees Celsius) and can lead to coma and even death if not treated promptly.

Treatment for hypothermia typically involves warming the person up slowly, using blankets or heating pads, and providing warm fluids to drink. In severe cases, medical professionals may use a specialized warm water bath or apply warm packs to specific areas of the body.

Preventing hypothermia is important, especially in cold weather conditions. This can be done by dressing appropriately for the weather, staying dry and avoiding wet clothing, eating regularly to maintain energy levels, and seeking shelter if you become stranded or lost. It's also essential to recognize the signs of hypothermia early on so that treatment can begin promptly.

Types of Malformations of Cortical Development:

There are several types of malformations of cortical development, including:

1. Cerebral palsy: a group of disorders that affect movement, balance, and posture, often resulting from brain damage during fetal development or birth.
2. Hydrocephalus: a condition in which there is an abnormal accumulation of cerebrospinal fluid (CSF) in the brain, leading to increased intracranial pressure and enlargement of the head.
3. Microcephaly: a condition in which the brain and skull are smaller than normal, often resulting in developmental delays, intellectual disability, and seizures.
4. Macrocephaly: a condition in which the brain and skull are larger than normal, often resulting from an overproduction of CSF or a brain tumor.
5. Cortical dysplasia: a condition in which there is abnormal development of the cerebral cortex, leading to problems with movement, cognition, and behavior.
6. Fetal alcohol spectrum disorders (FASD): a group of conditions that result from exposure to alcohol during fetal development, often causing malformations of the cerebral cortex and other brain structures.
7. Genetic mutations: some genetic mutations can lead to malformations of cortical development, such as those caused by maternal infection or exposure to certain medications.
8. Infections during pregnancy: certain infections, such as rubella or toxoplasmosis, can cause malformations of cortical development if contracted during pregnancy.
9. Traumatic brain injury: a head injury during fetal development or early childhood can disrupt normal cortical development and lead to developmental delays and cognitive impairments.
10. Exposure to toxins: exposure to certain toxins, such as lead or pesticides, during fetal development can damage the developing brain and result in malformations of cortical development.

These are just a few examples of conditions that can cause malformations of cortical development. It's important to note that many of these conditions can be diagnosed through imaging studies such as MRI or CT scans, and some may require specialized testing or monitoring throughout childhood. Early detection and intervention can help improve outcomes for children with these conditions.

Types of Hypothalamic Diseases:

1. Hypothalamic hamartoma: A benign tumor that develops in the hypothalamus and can cause a variety of symptoms such as seizures, obesity, and developmental delays.
2. Hypothalamic glioma: A malignant tumor that arises in the hypothalamus and can cause similar symptoms to hypothalamic hamartoma.
3. Hypothalamic malformations: Congenital abnormalities that affect the development of the hypothalamus, leading to various neurological symptoms such as seizures, intellectual disability, and behavioral problems.
4. Hypothalamic infarction: A condition where there is a lack of blood flow to the hypothalamus, leading to damage to the tissue and potentially causing a range of symptoms including stroke-like symptoms.
5. Hypothalamic lesions: Damage to the hypothalamus caused by traumatic brain injury, infection, or other factors, which can lead to a range of neurological symptoms.

Symptoms of Hypothalamic Diseases:

The symptoms of hypothalamic diseases can vary depending on the specific condition and the severity of the damage to the hypothalamus. Some common symptoms include:

* Seizures
* Headaches
* Vision problems
* Balance and coordination difficulties
* Weight changes (gain or loss)
* Sleep disturbances
* Mood changes (depression, anxiety)
* Behavioral problems (aggression, irritability)
* Intellectual disability

Diagnosis of Hypothalamic Diseases:

Diagnosing hypothalamic diseases can be challenging and may require a range of tests and evaluations. These may include:

1. Physical examination and medical history: A thorough evaluation of the patient's symptoms, medical history, and physical condition.
2. Imaging tests: Such as CT or MRI scans to visualize the brain and identify any structural abnormalities or lesions in the hypothalamus.
3. Blood tests: To check for hormone levels and other markers that can help diagnose specific conditions.
4. EEG and other neurological tests: To evaluate the patient's neurological function and identify any potential seizure activity or other abnormalities.
5. Genetic testing: If the condition is suspected to be inherited, genetic testing may be performed to identify mutations or variations in genes that can contribute to hypothalamic diseases.

Treatment of Hypothalamic Diseases:

The treatment of hypothalamic diseases depends on the specific condition and the severity of the symptoms. Some common treatments include:

1. Medications: Such as anticonvulsants, hormone replacement therapy, and pain management medications to control seizures, hormonal imbalances, and pain.
2. Hormone replacement therapy: To replace hormones that are deficient or imbalanced.
3. Surgery: May be necessary to remove a tumor or repair a structural abnormality in the hypothalamus.
4. Lifestyle modifications: Such as changes to diet, exercise, and sleep habits to manage symptoms and improve quality of life.
5. Rehabilitation therapy: To help regain lost functions and improve daily living skills.

Prognosis of Hypothalamic Diseases:

The prognosis for hypothalamic diseases varies depending on the specific condition and the severity of the symptoms. Some conditions may have a good prognosis with appropriate treatment, while others may have a poorer outcome. In general, early diagnosis and treatment can improve the chances of a better outcome.

Living with Hypothalamic Diseases:

Living with a hypothalamic disease can be challenging and may require significant lifestyle modifications and ongoing medical care. However, with the right treatment and support, many people are able to manage their symptoms and improve their quality of life. Some tips for living with a hypothalamic disease include:

1. Educate yourself about your condition and its management.
2. Work closely with your healthcare provider to develop a personalized treatment plan.
3. Make lifestyle modifications such as changes to diet, exercise, and sleep habits.
4. Join a support group to connect with others who are living with similar conditions.
5. Seek mental health support if needed to cope with the emotional impact of the condition.

In conclusion, hypothalamic diseases can have a significant impact on quality of life, but with early diagnosis and appropriate treatment, many people are able to manage their symptoms and improve their outcomes. It is important to work closely with a healthcare provider to develop a personalized treatment plan and make lifestyle modifications as needed. With the right support and resources, it is possible to live a fulfilling life with a hypothalamic disease.

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 ... GABA receptors influence neural function by coordinating with glutamatergic processes. A subclass of ionotropic GABA receptors ... Over-excitation of this receptor induces receptor remodeling and the eventual invagination of the GABA receptor. As a result, ...

https://en.wikipedia.org/wiki/GABA_receptor

GABA-α and GABA-ρ receptors produce sedative and hypnotic effects and have anti-convulsion properties. GABA-β receptors also ... A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative ... There are three receptors of the gamma-aminobutyric acid. The two receptors GABA-α and GABA-ρ are ion channels that are ... binding to GABA receptors and inhibiting neuronal signaling. Brohan J, Goudra BG (October 2017). "The Role of GABA Receptor ...

https://en.wikipedia.org/wiki/GABA_receptor_agonist

GABAA receptors GABAA-ρ receptors The GABAB receptor, a G protein-coupled receptor, is the only metabotropic GABA receptor and ... Ionotropic GABA receptors (iGABARs) are ligand-gated ion channel of the GABA receptors class which are activated by gamma- ... Thus, the iontropic GABA receptors consist of the GABAA receptor and the GABAA-ρ receptor. There are pharmacological ... The two types of GABA receptors are the GABAA and GABAB receptors. The pentameric GABAA receptors are ionotropic, meaning that ...

https://en.wikipedia.org/wiki/Ionotropic_GABA_receptor

... s are drugs that inhibit the action of GABA. In general these drugs produce stimulant and convulsant ... GABAA receptor negative allosteric modulators GABA+antagonists at the US National Library of Medicine Medical Subject Headings ... v t e (GABA receptor antagonists, Biochemistry, All stub articles, Nervous system drug stubs). ... Other agents which may have GABAA receptor antagonism include the antibiotic ciprofloxacin, tranexamic acid, thujone, ginkgo ...

https://en.wikipedia.org/wiki/GABA_receptor_antagonist

... is a protein that in humans is encoded by the GABARAPL1 gene. GRCh38: Ensembl ... "Entrez Gene: GABA type A receptor associated protein like 1". Retrieved 2017-12-21. Nemos C, Mansuy V, Vernier-Magnin S, ... "GEC1 interacts with the kappa opioid receptor and enhances expression of the receptor". J. Biol. Chem. 281 (12): 7983-93. doi: ... Chen Y, Chen C, Kotsikorou E, Lynch DL, Reggio PH, Liu-Chen LY (2009). "GEC1-kappa opioid receptor binding involves hydrophobic ...

https://en.wikipedia.org/wiki/Gaba_type_a_receptor_associated_protein_like_1

Dupont AG, Légat L (October 2020). "GABA is a mediator of brain AT1 and AT2 receptor-mediated blood pressure responses". ... where GABA can be recycled) and astrocytes (where GABA can be broken down). GABA Transporter 1 uses energy from the dissipation ... The GABA affinity (Km) of the mouse isoform of GAT1 is 8 μM. In the brain of a mature mammal, glutamate is converted to GABA by ... The stoichiometry for GABA Transporter 1 is 2 Na+: 1 Cl−: 1 GABA. The presence of a Cl−/Cl− exchange is also proposed because ...

https://en.wikipedia.org/wiki/GABA_transporter_type_1

GHB receptor agonists, GABA analogues, General anesthetics, Neurotransmitters, Drug culture, Euphoriants, Hydroxy acids, GABA, ... It is a precursor to GABA, glutamate, and glycine in certain brain areas. It acts on the GHB receptor and is a weak agonist at ... Other antipsychotics were tested and were not found to have an affinity for this receptor. GHB is a precursor to GABA, ... Allen MJ, Sabir S, Sharma S (2022). GABA Receptor. StatPearls. Treasure Island (FL): StatPearls Publishing. PMID 30252380. ...

https://en.wikipedia.org/wiki/Gamma-Hydroxybutyric_acid

GABA Receptor Agonists". Drugs and Diseases. Medccape. Retrieved 10 July 2005. Ralvenius WT, Acuña MA, Benke D, Matthey A, ... June 2000). "Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype". ... work by enhancing GABA-activated chloride influx at GABAA receptors, creating a hyperpolarizing, inhibitory postsynaptic ... The α1 subtype of the GABAA receptor, was shown to be responsible for the sedative effects of diazepam by McKernan et al. in ...

https://en.wikipedia.org/wiki/Clobazam

GABA(B)) receptors with truncated receptors and metabotropic glutamate receptor 4 supports the GABA(B) heterodimer as the ... "Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors". Nature. 386 (6622): 239-46. ... The GABA(B) receptor 1 gene is mapped to chromosome 6p21.3 within the HLA class I region close to the HLA-F gene. ... Couve A, Kittler JT, Uren JM, Calver AR, Pangalos MN, Walsh FS, Moss SJ (2001). "Association of GABA(B) receptors and members ...

https://en.wikipedia.org/wiki/GABBR1

"A pharmacological characterization of GABA, THIP and DS2 at binary α4β3 and β3δ receptors: GABA activates β3δ receptors via the ... Goetz T, Arslan A, Wisden W, Wulff P (2007). "GABAA receptors: Structure and function in the basal ganglia". GABA(A) receptors ... July 1987). "Sequence and functional expression of the GABA A receptor shows a ligand-gated receptor super-family". Nature. 328 ... GABA). GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts on the repertoire of GABAA receptors ...

https://en.wikipedia.org/wiki/GABRD

Benzodiazepines produce an anxiolytic response by modulating GABA and increasing its receptor binding. A third common treatment ... September 2011). "Ingestion of Lactobacillus strain regulates emotional behavior and central GABA receptor expression in a ... decreased GABA-ergic tone; allelic polymorphism of the catechol-O-methyltransferase (COMT) gene; increased adenosine receptor ... and a receptor gene for BDNF called NTRK2 was associated with anxiety in a large genome-wide investigation. The reason that ...

https://en.wikipedia.org/wiki/Anxiety

GABA-A receptors; (4) AMPA/kainate receptors; and (5) carbonic anhydrase isoenzymes. There is evidence that topiramate may ... Effects on specific GABA-A receptor isoforms could also contribute to the antiseizure activity of the drug. Topiramate ... AMPA receptor antagonists, Anticonvulsants, Carbonic anhydrase inhibitors, GABAA receptor positive allosteric modulators, ... Johnson & Johnson brands, Kainate receptor antagonists, Monosaccharide derivatives, Sodium channel blockers, Sulfamates, ...

https://en.wikipedia.org/wiki/Topiramate

GABA). They are closely related and similar to GABAA receptor antagonists. The effects of GABAA receptor NAMs are functionally ... A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ... Flumazenil is a competitive antagonist of the benzodiazepine site of the GABAA receptor and hence is a GABAA receptor NAM of ... GABAA receptor positive allosteric modulator AMPA receptor positive allosteric modulator List of investigational ...

https://en.wikipedia.org/wiki/GABAA_receptor_negative_allosteric_modulator

However, due to its antagonist effect on GABA receptors, it has been used as a central nervous system stimulant. It was also ... GABAA receptor negative allosteric modulators, GABAA-rho receptor negative allosteric modulators, Glycine receptor antagonists ... Other research suggests that the toxin acts instead as a non-competitive antagonist, or inhibitor, for GABA receptors. A study ... Newland CF, Cull-Candy SG (February 1992). "On the mechanism of action of picrotoxin on GABA receptor channels in dissociated ...

https://en.wikipedia.org/wiki/Picrotoxin

"GABA(A) receptors and alcohol". Pharmacology Biochemistry and Behavior. 90 (1): 90-4. doi:10.1016/j.pbb.2008.03.006. PMC ... and NMDA receptors, the glycine receptor, the nicotinic acetylcholine receptors, the serotonin 5-HT3 receptor, voltage-gated ... Nicotinic acetylcholine receptor positive allosteric modulator 5-HT3 receptor positive allosteric modulator Glycine reuptake ... to other actions AMPA receptor negative allosteric modulator Kainate receptor negative allosteric modulator Glycine receptor ...

https://en.wikipedia.org/wiki/Alcohol_(drug)

"Interaction of pitrazepin with the GABA/benzodiazepine receptor complex and with glycine receptors". European Journal of ... Sattelle DB, Pinnock RD, Wafford KA, David JA (January 1988). "GABA receptors on the cell-body membrane of an identified insect ... Murphy VF, Wann KT (November 1988). "The action of GABA receptor agonists and antagonists on muscle membrane conductance in ... Anthony NM, Harrison JB, Sattelle DB (1993). "GABA receptor molecules of insects". Exs. 63: 172-209. doi:10.1007/978-3-0348- ...

https://en.wikipedia.org/wiki/Pitrazepin

The GABAA receptor (GABAAR) is an ionotropic receptor activated by the inhibitory neurotransmitter γ-aminobutyric acid (GABA). ... The Cys-loop receptor superfamily includes inhibitory receptors (GABAA receptors, GABAC receptors, glycine receptors) and ... Sallard, Erwan; Letourneur, Diane; Legendre, Pascal (2021). "Electrophysiology of ionotropic GABA receptors". Cellular and ... "Human GABAA receptor α1-β2-γ2 subtype in complex with GABA plus propofol". RCSB PDB. doi:10.2210/pdb6X3T/pdb. S2CID 225185057. ...

https://en.wikipedia.org/wiki/Theories_of_general_anaesthetic_action

These changes rely on the precise timing of GABA receptors activation which in turn are dependent upon the release and ... The GABA transporter group consists of six different transporters: GABA transporter type 1 (GAT1; SLC6A1) GABA transporter type ... The GABA transporter help creates an equilibrium of GABA and will work in the reverse direction if needed to maintain the ... The GABA transmitters are not broken down but are cleared via GABA transporters through re-absorption from the synaptic cleft. ...

https://en.wikipedia.org/wiki/GABA_transporter

Wang H, Bedford FK, Brandon NJ, Moss SJ, Olsen RW (January 1999). "GABA(A)-receptor-associated protein links GABA(A) receptors ... Wang H, Bedford FK, Brandon NJ, Moss SJ, Olsen RW (January 1999). "GABA(A)-receptor-associated protein links GABA(A) receptors ... mediates neuronal inhibition by binding to GABA receptors. The type A GABA receptors are pentameric chloride channels assembled ... "Subunit specificity and interaction domain between GABA(A) receptor-associated protein (GABARAP) and GABA(A) receptors". ...

https://en.wikipedia.org/wiki/Gamma-aminobutyric_acid_receptor_subunit_gamma-2

GABAA receptor antagonists are drugs that bind to GABAA receptors but do not activate them and inhibit the action of GABA. Thus ... "GABA-A Receptor Antagonists - MeSH - NCBI". www.ncbi.nlm.nih.gov. Retrieved 2022-01-18. "GABAA Receptor Agonists - an overview ... 3-Mercaptopropionic acid Allylglycine Glycine receptor antagonists are drugs which inactivates the glycine receptors. ... "Acetylcholine receptor anatomy". www.openanesthesia.org. Retrieved 2022-01-18. Cooper, Kathryn (October 2014). "The chemical ...

https://en.wikipedia.org/wiki/Convulsant

... is a GABA receptor agonist. It was patented as an anticonvulsant by Merck but was never marketed. Imidazopyridine ... GABAA receptor agonists, Imidazopyridines, Abandoned drugs, All stub articles, Anticonvulsant stubs). ...

https://en.wikipedia.org/wiki/Bamaluzole

GABA agonist GABA antagonist GABA receptor López-Muñoz F, Ucha-Udabe R, Alamo C (Dec 2005). "The history of barbiturates a ... The GABAA receptors are made up of subunits which form a receptor complex. Humans have 19 receptor subunits and are classified ... Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-Aminobutyric acid (GABA) ... GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it triggers the GABAA receptor to open ...

https://en.wikipedia.org/wiki/GABAA_receptor_positive_allosteric_modulator

GABA. Muscimol binds to the same site on the GABAA receptor complex as GABA itself, as opposed to other GABAergic drugs such as ... Frølund B, Ebert B, Kristiansen U, Liljefors T, Krogsgaard-Larsen P (August 2002). "GABA(A) receptor ligands and their ... April 2019). "Extrasynaptic δ-GABAA receptors are high-affinity muscimol receptors". Journal of Neurochemistry. 149 (1): 41-53 ... "Muscimol as an ionotropic GABA receptor agonist". Neurochemical Research. 39 (10): 1942-1947. doi:10.1007/s11064-014-1245-y. ...

https://en.wikipedia.org/wiki/Muscimol

GABA Receptor Physiology and Pharmacology (6th ed.). American Society for Neurochemistry. Retrieved 2008-10-01. Itier V, ... Nicotinic acetylcholine receptors are the best-studied of the ionotropic receptors. Since nicotinic receptors help transmit ... The nicotinic receptors are considered cholinergic receptors, since they respond to acetylcholine. Nicotinic receptors get ... They possess similarities with GABAA receptors, glycine receptors, and the type 3 serotonin receptors (which are all ionotropic ...

https://en.wikipedia.org/wiki/Nicotinic_acetylcholine_receptor

Bormann J, Ferrero P, Guidotti A, Costa E (1985). "Neuropeptide modulation of GABA receptor C1- channels". Regulatory Peptides ... 1992). "The human "peripheral-type" benzodiazepine receptor: regional mapping of the gene and characterization of the receptor ... "Peripheral" benzodiazepine receptors are also found in the brain, although only at around a quarter the expression levels of ... YL-IPA08 Ro5-4864 - original ligand with which TSPO receptor was characterised, now less used due to inter-species differences ...

https://en.wikipedia.org/wiki/Translocator_protein

... rat or human GABA receptors is expected to be low for afoxolaner. Selectivity for insect over mammalian GABA-receptors has been ... Hosie AM, Aronstein K, Sattelle DB, ffrench-Constant RH (December 1997). "Molecular biology of insect neuronal GABA receptors ... GABA-receptors). Isoxazolines, among the chloride channel modulators, bind to a distinct and unique target site within the ... The selectivity might be explained by the number of pharmacological differences that exist between GABA-gated chloride channels ...

https://en.wikipedia.org/wiki/Afoxolaner

Watanabe M, Maemura K, Kanbara K, Tamayama T, Hayasaki H (2002). "GABA and GABA receptors in the central nervous system and ... NMDA receptors rely on the EPSC produced by AMPA receptors to open. NMDA receptors are permeable to Ca2+, which is an important ... 2009). "Metabotropic glutamate receptor subtype 4 selectively modulates both glutamate and GABA transmission in the striatum: ... Glutamate is the main excitatory and GABA the main inhibitory neurotransmitter in the mammalian cortex "Glutamate Receptors - ...

https://en.wikipedia.org/wiki/Glutamate_receptor

Alcohol also acts as a positive allosteric modulator of GABA receptors, specifically type GABAA. Upon activation, these GABA ... Schummers, J.; Browning, M. D. (2001). "Evidence for a role for GABA(A) and NMDA receptors in ethanol inhibition of long-term ... Hodge, C. W.; Cox, A. A. (1998). "The discriminative stimulus effects of ethanol are mediated by NMDA and GABA(A) receptors in ... Paul, S. M. (2006). "Alcohol-sensitive GABA receptors and alcohol antagonists". Proceedings of the National Academy of Sciences ...

https://en.wikipedia.org/wiki/Effects_of_alcohol_on_memory

These receptors have inhibitory functions comparable to those of the GABA receptors. Lastly, investigation into similar toxins ... Tutin is an antagonist of the GABA receptors. By inhibiting these receptors, the sedative effect of this neurotransmitter is ... Apart from GABA receptor inhibition, in vitro studies have also shown tutin to have an inhibitory effect on the glycine ... Glycine receptor antagonists, GABAA receptor antagonists, Spiro compounds, Sesquiterpene lactones, Neurotoxins). ...

https://en.wikipedia.org/wiki/Tutin_(toxin)

... gene and GABA receptors in the cerebellum of people with essential tremor. HAPT1 mutations have also been linked to ET, as well ... "Defective dentate nucleus GABA receptors in essential tremor". Brain. 135 (Pt 1): 105-16. doi:10.1093/brain/awr301. PMID ... Mally J, Stone TW (June 1991). "The effect of theophylline on essential tremor: the possible role of GABA". Pharmacology ...

https://en.wikipedia.org/wiki/Essential_tremor

5-HT6 receptor antagonist [22] BNC-210 (IW-2143) - "GABA modulator" / undefined mechanism of action[23] JNJ-42165279 - FAAH ... 5-HT1A receptor agonist, 5-HT2A receptor antagonist [4] Vilazodone (EMD-68843, SB-659746A; Viibryd) - 5-HT1A receptor partial ... 5-HT1A receptor agonist, 5-HT2A receptor antagonist [20] Vilazodone (EMD-68843, SB-659746A; Viibryd) - 5-HT1A receptor partial ... Agomelatine (AGO-178; Valdoxan) - melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist[1] Riluzole sublingual ( ...

https://en.wikipedia.org/wiki/List_of_investigational_anxiolytics

... role of GABA(A)/alpha1 receptors". Psychopharmacology. 165 (3): 209-15. doi:10.1007/s00213-002-1275-z. PMID 12420154. S2CID ... Most other benzodiazepines are unselective and bind to type1 GABAA receptors and type2 GABAA receptors. Type1 GABAA receptors ... Quazepam modulates specific GABAA receptors via the benzodiazepine site on the GABAA receptor. This modulation enhances the ... and long-acting benzodiazepine-receptor agonists with different receptor selectivity on motor coordination and muscle ...

https://en.wikipedia.org/wiki/Quazepam

GABA receptor antagonists, German inventions, Glycine receptor antagonists, Kappa-opioid receptor agonists, Morphinans, Mu- ... also acts as a glycine receptor antagonist and GABA receptor antagonist at very high concentrations. Levorphanol is 6 to 8 ... κ-opioid receptor (KOR), and the nociceptin receptor (NOP), as well as an NMDA receptor antagonist and a serotonin- ... opioid receptor agonists, NMDA receptor antagonists, Nociceptin receptor agonists, Phenols, Serotonin-norepinephrine reuptake ...

https://en.wikipedia.org/wiki/Levorphanol

The dependence induced by lormetazepam is related to changes in the sensitivity of the GABA-BZD receptor complex. Withdrawal ... Lormetazepam binds to the benzodiazepine receptor which in turn enhances the effect of the GABAA receptor producing its ... Lormetazepam appears to be more selective in the type of benzodiazepine receptor it binds to showing a higher affinity for the ... When lormetazepam binds to the benzodiazepine receptor sites in sufficient quantities it produces sedation which is used ...

https://en.wikipedia.org/wiki/Lormetazepam

An adenosine A1 receptor agonist has been shown to depress preBötC rhythmogenesis independent of the neurotransmitters GABA and ... 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 ... A lack of serotonin binding to the serotonin receptor 2 leads to the inability to autoresuscitation due to the lack of drive ...

https://en.wikipedia.org/wiki/Pre-Bötzinger_complex

... binds at a distinct binding site associated with a Cl− ionophore at the GABAA receptor, increasing the duration of ... The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. Symptoms of acute barbiturate poisoning ... GABAA receptor positive allosteric modulators, Allyl compounds, All stub articles, Sedative stubs). ...

https://en.wikipedia.org/wiki/Talbutal

GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated ... Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At ... Mu W, Cheng Q, Yang J, Burt DR (2002). "Alternative splicing of the GABA(A) receptor alpha 4 subunit creates a severely ... Kumar S, Sieghart W, Morrow AL (2002). "Association of protein kinase C with GABA(A) receptors containing alpha1 and alpha4 ...

https://en.wikipedia.org/wiki/GABRA4

The reduction in GABA receptors in the hypothalamus seen in chronic stress reduces the inhibition of stress hormone release ... Chronic mildly stressed rats display a reduction in inhibitory GABA receptors in the hypothalamus (increasing the release of ... Within the pedunculopontine tegmentum region, in the brainstem, reduced GABA imbibition of cholinergic neurons acts again in ... by the circadian rhythm but its effectiveness is increased by sleep itself as there is an increase in serum IL-6 receptors ...

https://en.wikipedia.org/wiki/Psychological_stress_and_sleep

April 2006). "The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol ... Filip M, Frankowska M, Przegaliński E (November 2007). "Effects of GABA(B) receptor antagonist, agonists and allosteric ... a positive allosteric modulator of the GABA(B) receptor". The Journal of Biological Chemistry. 279 (28): 29085-91. doi:10.1074/ ... Binet V, Brajon C, Le Corre L, Acher F, Pin JP, Prézeau L (July 2004). "The heptahelical domain of GABA(B2) is activated ...

https://en.wikipedia.org/wiki/CGP-7930

... because of H3 receptor-modulation of dopamine and GABA in the basal ganglia), schizophrenia and ADHD (again because of dopamine ... histamine receptor antagonists H3-receptor antagonist Histamine H1-receptor Histamine H2-receptor Histamine H4-receptor GRCh38 ... 1997 H3 receptors shown to modulate ischemic norepinephrine release in animals. 1999 H3 receptor cloned 2000 H3 receptors ... the H3 receptor is a G-protein coupled receptor. The H3 receptor is coupled to the Gi G-protein, so it leads to inhibition of ...

https://en.wikipedia.org/wiki/Histamine_H3_receptor

... in cortical inhibitory interneurons that release GABA and synaptic abnormalities associated with deficits in NMDA receptor ... Metabotropic glutamate receptors are known to act as modulators of (affect the activity of) other receptors. For example, group ... The metabotropic glutamate receptors, or mGluRs, are a type of glutamate receptor that are active through an indirect ... Receptor types are grouped based on receptor structure and physiological activity. The mGluRs are further divided into subtypes ...

https://en.wikipedia.org/wiki/Metabotropic_glutamate_receptor

... competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor ... After long-term exposure to benzodiazepines, GABAA receptors become down-regulated and uncoupled. Growth of new receptors and ... because they act via the benzodiazepine site of the GABA receptor - it has been used to successfully treat z-drug overdose. ... GABA(A) receptors". Biomedicine & Pharmacotherapy. 59 (7): 408-414. doi:10.1016/j.biopha.2005.02.003. PMID 16084060. Danka ...

https://en.wikipedia.org/wiki/Flumazenil

... one received directly from its receptor with a time delay and the other received from the adjacent receptor, are multiplied. ... This means that GABA at one area will be depolarizing and at another area hyperpolarizing, accounting for the spatial offset ... Both subunits have a receptor that can be stimulated by an input (light in the case of visual system). In each subunit, when an ... Further evidence suggests that starburst cells release inhibitory neurotransmitters, GABA onto each other in a delayed and ...

https://en.wikipedia.org/wiki/Motion_perception

GABA activates the GABAA receptor which is a Cl− ion channel. Cl− ions will enter the neuron causing hyperpolarization and ... Thus, GABA is an excitatory neurotransmitter during development. WNK1 has been implicated in the developmental switch from ... In the mature brain, the GABA neurotransmitter represents the major inhibitory signal used in neuronal signaling. ... excitatory to inhibitory GABA signaling via interaction with NKCC1 and KCCs. WNK1 phosphorylates SPAK/OSR1 which then ...

https://en.wikipedia.org/wiki/WNK1

These receptors sense the local environment, causing the growth cone to be attracted or repelled by various cellular elements, ... Because of their ubiquity, drugs that act on glutamate or GABA tend to have broad and powerful effects. Some general ... The axons of sensory receptor cells travel into the spinal cord or brain, where they transmit their signals to a first-order ... The tip of a growing axon consists of a blob of protoplasm called a growth cone, studded with chemical receptors. ...

https://en.wikipedia.org/wiki/Brain

G protein-coupled receptor - G3P - GABA - GABA receptor - GABA-A receptor - gag-onc fusion protein - galanin - gamete - gamma- ... interleukin receptor - interleukin-1 receptor - interleukin-2 receptor - interleukin-3 - interleukin-3 receptor - intermediate ... IgE receptor - IGF type 1 receptor - IGF type 2 receptor - IgG - IgM - immediate-early protein - immune cell - immune system - ... alpha adrenergic receptor - alpha helix - alpha-1 adrenergic receptor - alpha-2 adrenergic receptor - alpha-beta T-cell antigen ...

https://en.wikipedia.org/wiki/Index_of_biochemistry_articles

Specifically, it studied the muscarinic and gaba (benzodiazepine) receptors in the sensory-motor cortex and spinal cord. The ... The objective of this experiment was to determine the effects of spaceflight on neurotransmitter receptors of the brain and ...

https://en.wikipedia.org/wiki/Kosmos_2044

Alcohol produces a sedative effect by acting on receptors of the inhibitory neurotransmitter GABA. GABA receptors contain a ... When alcohol molecules bind to its site on the GABA receptor, they lengthen the time that the receptor's chloride ion pore ... When a GABA molecule attaches to its binding site, it activates the receptor, resulting in an inflow of chloride ions. The ... Alcohol's ability to alter behavior and decision-making stems from its impact on synaptic transmission at GABA receptors. ...

https://en.wikipedia.org/wiki/Alcohol_myopia

Braida D, Limonta V, Malabarba L, Zani A, Sala M (January 2007). "5-HT1A receptors are involved in the anxiolytic effect of ... GABA and glutamate. When using cannabidiol (CBD) results have indicated a weakened emotional response to traumatic memories. ... This effect is attributed to the presence of endocannabinoid receptors in the limbic system, including the amygdala, and the ... Pertwee RG (January 2008). "The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: delta9- ...

https://en.wikipedia.org/wiki/Cannabis_use_and_trauma

2002). "Subunit specificity and interaction domain between GABA(A) receptor-associated protein (GABARAP) and GABA(A) receptors ... 2005). "Identification of significant association and gene-gene interaction of GABA receptor subunit genes in autism". Am. J. ... 2009). "An immunohistochemical study of GABA A receptor gamma subunits in Alzheimer's disease hippocampus: relationship to ... Gamma-aminobutyric acid receptor subunit gamma-1 is a protein that in humans is encoded by the GABRG1 gene. The protein encoded ...

https://en.wikipedia.org/wiki/GABRG1

H1 receptor antagonist) Vilazodone (atypical antidepressant) Agomelatine (antidepressant, MT1/2 receptor agonist, 5HT2c ... Citalopram Fluoxetine Sertraline Fluvoxamine Benzodiazepines Clonazepam Lorazepam Diazepam GABA analogs Pregabalin[excessive ... SSRIs increase serotonin levels through inhibition of serotonin reuptake receptors. FDA approved SSRIs used for this purpose ... and also implicated in neurotransmitters and neurotransmitter receptors known to be involved in anxiety disorders. More ...

https://en.wikipedia.org/wiki/Generalized_anxiety_disorder

This suggests that in schizophrenia, the alpha-2 adrenergic receptor, a presynaptic inhibitory receptor, may be less sensitive ... serotonin and GABA transporters. A single-nucleotide polymorphism (SNP) is a genetic variation in which a genome sequence is ... compared to normally functioning alpha-2 receptors and thus relate to elevated NE levels in the disorder. In addition to ...

https://en.wikipedia.org/wiki/Norepinephrine_transporter

... they function via the benzodiazepine receptor of neurotransmitter GABA. The best-known cyclopyrrolone derivatives are zopiclone ...

https://en.wikipedia.org/wiki/Cyclopyrrolones

Rainesalo S, Keränen T, Saransaari P, Honkaniemi J (November 2005). "GABA and glutamate transporters are expressed in human ... "Differential synaptic localization of the glutamate transporter EAAC1 and glutamate receptor subunit GluR2 in the rat ...

https://en.wikipedia.org/wiki/Excitatory_amino_acid_transporter_3

... is linked to receptors for several brain chemicals including glutamate, dopamine and GABA. An experiment with ... cell receptor-induced calcineurin activation regulates T helper type 2 cell development by modifying the interleukin 4 receptor ... When an antigen-presenting cell interacts with a T cell receptor on T cells, there is an increase in the cytoplasmic level of ... 5-trisphosphate receptor-FKBP12 complex modulates Ca2+ flux". Cell. 83 (3): 463-72. doi:10.1016/0092-8674(95)90124-8. PMID ...

https://en.wikipedia.org/wiki/Calcineurin

Ticku MK, Burch TP, Davis WC (1983). "The interactions of ethanol with the benzodiazepine-GABA receptor-ionophore complex". ... In a New Zealand study (2003) of 200 deaths, Zopiclone, a benzodiazepine receptor agonist, had similar overdose potential as ... Flumazenil (Romazicon) is a competitive benzodiazepine receptor antagonist that can be used as an antidote for benzodiazepine ... Benzodiazepines bind to a specific benzodiazepine receptor, thereby enhancing the effect of the neurotransmitter gamma- ...

https://en.wikipedia.org/wiki/Benzodiazepine_overdose

It is therefore possible that this protein also acts as a neuropeptide to modulate the action of the GABA receptor. ACBP is a ... recognition site located on the GABA type A receptor. ...

https://en.wikipedia.org/wiki/Acyl-CoA-binding_protein

... nociception is dependent upon GABA-B receptor signaling since both were abolished by treatment with a GABA-B receptor ... Specific regulation of mechanical nociception by Gβ5 involves GABA-B receptors Mritunjay Pandey 1 , Jian-Hua Zhang 1 , Poorni R ... Specific regulation of mechanical nociception by Gβ5 involves GABA-B receptors Mritunjay Pandey et al. JCI Insight. 2023. . ... without and with the systemic administration of the GABA-B receptor antagonist 2-hydroxysaclofen (2HS). (A) Hot plate testing ( ...

https://www.ncbi.nlm.nih.gov/pubmed/37219953

... is associated with GABA receptor activation. Fmr1 KO mice exhibit decreased levels of GABAA and GABAB receptors, indicating ... The effect of a GABA receptor agonist on sleep deficiency in a Fragile X syndrome mouse model. Thursday, September 14, 2017. - ... that GABA pathways are affected in FXS. Our previous studies have shown that a GABAB receptor agonist, R-baclofen, reverses ...

https://researchfestival.nih.gov/2017/posters/effect-gaba-receptor-agonist-sleep-deficiency-fragile-x-syndrome-mouse

Like benzodiazepines, barbiturates bind to the gamma-aminobutyric acid (GABA) receptor, enhancing the actions of GABA by ... These agents bind to the gamma-aminobutyric acid (GABA) receptor, thereby enhancing the actions of GABA. ... GABA) neurotransmission resulting from binding at the benzodiazepine site of the GABA-A receptor. Diazepam intranasal is ... GABA Receptor Positive Modulators. Class Summary. Precise mechanism is unknown, but anticonvulsant effects are thought to ...

https://emedicine.medscape.com/article/1184846-medication

... receptors play a central role in fast inhibitory neurotransmission in insects. Several classes of insecticide ... GABA receptor. Abstract: Background: γ-Aminobutyric acid (GABA) receptors play a central role in fast inhibitory ... Since some GABA receptor modulators act on L-glutamate-gated chloride channels, some comparisons are included. ... Since some GABA receptor modulators act on L-glutamate-gated chloride channels, some comparisons are included. ...

https://www.eurekaselect.com/article/84038

... receptor subunits, GABA(B1) and GABA(B2). In addition, to investigate the relationship between GABA(B) receptors and ... Double labeling for GABA(B) receptor subunits and vesicular glutamate transporters revealed that labeling for both GABA(B1) and ... the data indicate that GABA may also affect the excitability of striatal neurons via postsynaptic GABA(B) receptors. ... Immunolabeling for GABA(B1) and GABA(B2) was widely and similarly distributed in the striatum, with immunogold particles ...

https://www.dpag.ox.ac.uk/publications/330499

WL 385 85EP-1 Epilepsy and GABA receptor agonists : WL 385 85OD Epilepsies of childhood / WL 385 91AU Guidelines for ... Epilepsy and GABA receptor agonists : basic and therapeutic research / editors, G. Bartholini ... [et al.] Contributor(s): ...

https://kohahq.searo.who.int/cgi-bin/koha/opac-detail.pl?biblionumber=30507&shelfbrowse_itemnumber=53690

Nanoscale alterations in GABAB receptors and GIRK channel organization on the hippocampus of APP/PS1 mice. ... Nanoscale alterations in GABA,sub,B,/sub, receptors and GIRK channel organization on the h ... Texto completo: Disponível Coleções: Bases de dados internacionais Base de dados: MEDLINE Assunto principal: Receptores de GABA ... Texto completo: Disponível Coleções: Bases de dados internacionais Base de dados: MEDLINE Assunto principal: Receptores de GABA ...

https://pesquisa.bvsalud.org/portal/resource/pt/mdl-36131327

We find that simulated binding impulses to varying clusters of GABA binding site residues produce channel opening, and that ... We have performed a parallel tempering crankshaft motion Monte Carlo simulation on a model of the GABA type A receptor with the ... equivalent impulses to single GABA sites produce partial opening. ... Functional movements of the GABA type A receptor. Physical ... We have performed a parallel tempering crankshaft motion Monte Carlo simulation on a model of the GABA type A receptor with the ...

https://hal-pasteur.archives-ouvertes.fr/pasteur-03341745

Here we show that sleep is regulated by GABA in Drosophila and that a mutant GABAA receptor, RdlA302S, specifically decreases ... Pharmacological manipulation of these receptors has differential effects on sleep onset and sleep maintenance insomnia. ... uncouple the regulation of sleep latency from that of sleep duration and suggest that the kinetics of GABAA receptor signaling ... Many lines of evidence indicate that GABA and GABAA receptors make important contributions to human sleep regulation. ...

https://www.nature.com/articles/nn2046?error=cookies_not_supported&code=c65c5d00-71c0-41fb-b879-b0a3ab94c7bb

How do they do it? By acting on GABA receptors.. Dr. Paul, having been trained by the incredible Nobel-prize winning NIMH ... Subsequent research showed that there were several naturally produced neurosteroids that all work through GABA receptors, some ... Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor. Science, 232, 1004-1007. ... Stress-induced elevations of y-aminobutyric acid type A receptor-active steroids in the rat brain. Proceedings of the National ...

https://www.nimh.nih.gov/about/director/messages/2019/a-bench-to-bedside-story-the-development-of-a-treatment-for-postpartum-depression.shtml

GABA ion channel; GABA B; glutamatergic, glycine site; metabotropic glutamate subtypes and other glutamate receptor subtypes; ... Receptor interacting proteins, trafficking proteins; *Transporters: vesicular ACh; GABA; glutamate; glycine; glutamine; NET; ... coupled receptors, such as the dopamine receptor, an indirect site of action for cocaine and amphetamine, or ligand gated ion ... nicotinic receptor subunits; NMDA subunits; opioid receptors: mu, delta, kappa; serotonin: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5- ...

http://grants.nih.gov/grants/guide/pa-files/PAR-14-234.html

... crowd of transmembrane proteins and the rich cytoskeletal environment may constitute obstacles to the diffusion of receptors ... The flux of neurotransmitter receptors in and out of synapses depends on receptor interaction with scaffolding molecules. ... As shown for GABA(A)R, the excitatory glutamate receptor 2 subunit (GluA2) of the α-amino-3-hydroxy-5-methyl-4- ... To address this question, we studied the membrane diffusion of the γ-aminobutyric acid type A receptor (GABA(A)R) subunits ...

https://pubmed.ncbi.nlm.nih.gov/22912780/?dopt=Abstract

... ... Allosteric positive interaction of thymol with the GABA-A receptor in primary cultures of mouse cortical neurons; Pergamon- ... Thymol enhanced GABA-induced (5 μM) chloride influx at concentrations lower than those exhibiting direct activity in the ... In the present work, we more closely examined the pharmacological action of thymol on the native GABAA receptor by using ...

https://repositorioslatinoamericanos.uchile.cl/handle/2250/1907136

This antihyperalgesia occurs mainly through GABA A receptors (GABA A Rs) containing 2 subunits (2-GABA A Rs). Previous work ... This antihyperalgesia occurs mainly through GABA A receptors (GABA A Rs) containing 2 subunits (2-GABA A Rs). Previous work ... This antihyperalgesia occurs mainly through GABA A receptors (GABA A Rs) containing 2 subunits (2-GABA A Rs). Previous work ... This antihyperalgesia occurs mainly through GABA A receptors (GABA A Rs) containing 2 subunits (2-GABA A Rs). Previous work ...

https://experts.illinois.edu/en/publications/antihyperalgesia-by-2-gaba-a-receptors-occurs-via-a-genuine-spina

... of the GABAA receptor protein. The GABAA receptor acts as a channel. that allows negatively charged chlorine atoms (chloride ... Mutations in GABAA receptor subunit genes lead to production of altered subunit proteins that cannot form functional receptors ... Hirose S. Mutant GABA(A) receptor subunits in genetic (idiopathic) epilepsy. Prog Brain Res. 2014;213:55-85. doi: 10.1016/B978- ... When associated with mutations in GABAA receptor or calcium channel genes, it seems to follow an autosomal dominant inheritance ...

https://medlineplus.gov/genetics/condition/childhood-absence-epilepsy/

GABAA receptor αl subunit is the most widely expressed in the brain among at least 17 known subunits. This single fact implies ... GABAA receptor αl subunit is the most widely expressed in the brain among at least 17 known subunits. This single fact implies ... The construction of a targeting vector for GABA̳A receptor [alpha]1 subunit gene disruption. by Hei-Yin Yip THESIS 1998 ... GABAA receptors mediate the major inhibitory synaptic transmission in the central nervous system, and form a number of binding ...

https://lbezone.hkust.edu.hk/bib/b603958

... and low affinity DA receptors; estrogen; GABA A subunits; GABA ion channel; GABA B; glutaminergic; glycine site; metabotropic ... o Transporters: vesicular ACh; GABA glutamate; NET; SERT. o Enzymes: choline acetyltransferase; dopamine beta-hydroxylase; GABA ... nicotinic receptor subunits: alpha 7 & alpha 4 beta 2; NMDA subunits; opioid receptors: mu, delta, kappa; serotonin: 5-HT1A, 5- ... o Receptors: adenosine; adrenergic: alpha 1, alpha 2; cannabinoid: CB1, CB2; corticotropin releasing hormone: CRH R1, CRH R2; ...

http://grants2.nih.gov/grants/guide/pa-files/PA-03-112.html

... low affinity DA receptors; estrogen; GABA A subunits; GABA ion channel; GABA B; glutaminergic; glycine site; metabotropic ... Development of selective hormone receptor radioligands (e.g., for estrogen receptor ß, corticosteroid hormone receptors, and ... Transporters: vesicular ACh; GABA glutamate; NET; SERT *Enzymes: choline acetyltransferase; dopamine beta-hydroxylase; GABA ... nicotinic receptor subunits: alpha 7 & alpha 4 beta 2; NMDA subunits; opioid receptors: mu, delta, kappa; serotonin: 5-HT1A, 5- ...

http://grants2.nih.gov/grants/guide/pa-files/PA-06-018.html

... and it binds primarily to 2 major classes of receptors: GABA-A and GABA-B. GABA-A receptors are coupled to chloride (negative ... at least 6 alpha subunits and 3 beta and gamma subunits exist for the GABA-A receptor complex. A complete GABA-A receptor ... The thalamic relay neurons have GABA-B receptors in the cell body and receive tonic activation by GABA released from the NRT ... IPSPs are mediated mainly by the release of GABA in the synaptic cleft with postsynaptic activation of GABA-A receptors. ...

https://www.medscape.com/article/1184846-overview

Spatola M, Petit-Pedrol M, Simabukuro MM, Armangue T, Castro FJ, Barcelo Artigues MI, et al. Investigations in GABAA receptor ... Endres D, Rauer S, Kern W, Venhoff N, Maier SJ, Runge K, et al. Psychiatric presentation of Anti-NMDA receptor encephalitis. ... Anti-NMDA receptor encephalitis after TdaP-IPV booster vaccination: cause or coincidence? J Neurol. 2011;258:500-1. DOIPubMed ... Anti-NMDA receptor encephalitis and vaccination. Int J Mol Sci. 2017;18:. E193. . DOIPubMedGoogle Scholar ...

https://wwwnc.cdc.gov/eid/article/27/6/20-4170

... reduced the number of GABAA receptors and decreased the strength of electrical currents generated by synaptic GABAA receptor ... Shisa7 is a GABAA receptor auxiliary subunit controlling benzodiazepine actions. Science, October 10, 2019 DOI: 10.1126/science ... Before this study, it was thought that benzodiazepines worked alone to boost the nerve calming responses of GABAA receptors. Dr ... Electrical recordings showed that Shisa7 hastened receptor responses to the transmitter GABA and nearly doubled the size of ...

https://www.nih.gov/news-events/news-releases/sticky-gene-may-help-valium-calm-nerves

It appears to act on NMDA and GABA receptors. NIAAA is providing consultation on methodology and trial design to pharmaceutical ... NMDA subtype of glutamate receptor, the GABAA receptor, and other serotonin receptors. The effect of alcohol on these receptors ... Recently, a study identified one precise serotonin receptor subtype, 5-HT1B , that is involved in regulating the consumption of ... This was accomplished by genetically removing the serotonin receptor, 5-HT1B , and observing increases in alcohol consumption. ...

https://www.niaaa.nih.gov/about-niaaa/our-funding/congressional-testimony/niaaa-directors-statement-house-committee-appropriations-subcommittee-labor-health-and-human

GABA-A Receptors Mediate Tonic Inhibition and Neurosteroid Sensitivity in the Brain. Vitam Horm. 2018;107:177-191. doi: 10.1016 ... Genetic and Molecular Regulation of Extrasynaptic GABA-A Receptors in the Brain: Therapeutic Insights for Epilepsy. J Pharmacol ... Pressly B, Nguyen HM, Wulff H. GABAA receptor subtype selectivity of the proconvulsant rodenticide TETS. Arch Toxicol. 2018 Feb ... Oscillatory Synchronous Inhibition in the Basolateral Amygdala and its Primary Dependence on NR2A-containing NMDA Receptors. ...

https://www.ninds.nih.gov/current-research/trans-agency-activities/counteract-program/counteract-publications/counteract-publications-2018

GABA receptor bioassay; Metabolite; LC-MS-MS; Antibody; Immunoassay; Screening; Sensor ...

http://www2a.cdc.gov/nioshtic-2/BuildQyr.asp?s1=surveillance%2A&f1=KW&Startyear=&terms=3&Adv=1&ct=&B1=Search&Limit=500&Sort=DP+DESC&whichdate=DP&D1=10&EndYear=&PageNo=102&RecNo=1018&View=f&

... screening offer the ability to quickly and cheaply estimate the affinity and binding mode of a ligand for the protein receptor ... was found to inhibit both GLIC and GABAA receptors, suggesting that the GLIC receptor may be a plausible model system for GABAA ... The active compounds were further tested on GABAA receptors. One of the compounds, like propofol, ... a bacterial homolog of GABAA receptors, to search for compounds that bind to the same site as the anesthetic propofol. Among a ...

https://www.mdpi.com/1420-3049/19/7/10150/htm

Specific regulation of mechanical nociception by Gβ5 involves GABA-B receptors.. Pandey M, Zhang JH, Adikaram PR, Kittock C, ...

https://www.niddk.nih.gov/about-niddk/staff-directory/biography/simonds-william/publications

Receptors, GABA/chemistry; Receptors, GABA/metabolism*; Voltage-Dependent Anion Channels/metabolism ...

https://tools.niehs.nih.gov/portfolio/index.cfm?do=portfolio.publicationDetail&id=3943280

... partly via ionotropic type-A receptors (GABA,sub,A,/sub,Rs). Pharmacological properties of ρ-type GABA,sub,A,/sub,Rs are ... GABA) drives critical inhibitory processes in and beyond the nervous system, ... Keywords: Cys-loop receptor; GABA(A) receptors; GABA(C) receptors; cryo-EM; ligand-gated ion channel; ρ1 GABA(A) receptor. ... Structure and dynamics of differential ligand binding in the human ρ-type GABAA receptor John Cowgill 1 , Chen Fan 1 , Nandan ...

https://pubmed.ncbi.nlm.nih.gov/37659407/

The important resistant to dieldrin GABA receptor subunit (RDL) has been used to investigate insecticide sites of action using radioligands, electrophysiology and site-directed mutagenesis. (eurekaselect.com)
Although this important subunit readily forms robust functional homomeric receptors when expressed, alternative splicing and RNA A-to-I editing can generate diverse forms of the receptor. (eurekaselect.com)
However, the subunit composition of native GABA receptors remains unknown and studies to clarify this are needed. (eurekaselect.com)
These observations indicate that the blocking drugs can produce allosteric changes in GABA A receptors, at least those containing this mutated β2 subunit. (jneurosci.org)
Finally, both gabazine and bicuculline act as weak agonists for GABA A receptors containing the β2(Y157S) mutated subunit. (jneurosci.org)
As shown for GABA(A)R, the excitatory glutamate receptor 2 subunit (GluA2) of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) had lower mobility in both excitatory and inhibitory synapses but a higher residency time at excitatory synapses. (nih.gov)
These drugs facilitate the function of pentameric GABA A receptors that exhibit widespread expression in all brain regions and large structural and pharmacological heterogeneity as a result of composition from a repertoire of 19 subunit variants. (aspetjournals.org)
Most drugs, in long-term use and during withdrawal, have been associated with important modulations of the receptor subunit expression in brain-region-specific manner, participating in the mechanisms of tolerance and dependence. (aspetjournals.org)
GABA A receptor αl subunit is the most widely expressed in the brain among at least 17 known subunits. (edu.hk)
The present thesis work aimed at the construction of a replacement type of vector for a targeted disruption of the GABA A receptor αl subunit in mice. (edu.hk)
The success of this construction will facilitate the ablation of αl subunit gene and provide a mouse model for the in vivo studies on GABA A receptor αl subunit. (edu.hk)
For the construction of the targeting vector, a 13-kb DNA fragment containing the first two exons of mouse GABA A receptor al subunit was obtained from screening of a λ2001 based 129/Sv mouse genomic library. (edu.hk)
Therefore, mice generated from these cell lines will have ablated GABA A receptor αl subunit. (edu.hk)
Mutations in GABA A receptor subunit genes lead to production of altered subunit proteins that cannot form functional receptors, so fewer GABA A receptors are available. (medlineplus.gov)
Influence of subunit configuration on the interaction of picrotoxin-site ligands with recombinant GABA(A) receptors. (bvsalud.org)

We have studied the ability of alphaxalone (an anesthetic steroid) and pentobarbital (an anesthetic barbiturate) to directly activate recombinant GABA A receptors containing the α1, β2, and γ2L subunits. (jneurosci.org)
Steroid gating was not affected when either of two mutated β2 subunits [β2(Y157S) and β2(Y205S)] are incorporated into the receptors, although these subunits greatly reduce the affinity of GABA binding. (jneurosci.org)
Finally, at receptors containing α1β2(Y157S)γ2L subunits, both bicuculline and gabazine showed weak agonist activity and actually potentiated responses to alphaxalone. (jneurosci.org)
To address this question, we studied the membrane diffusion of the γ-aminobutyric acid type A receptor (GABA(A)R) subunits clustered (γ2) or not (α5) at inhibitory synapses in rat hippocampal dissociated neurons. (nih.gov)
This antihyperalgesia occurs mainly through GABA A receptors (GABA A Rs) containing 2 subunits (2-GABA A Rs). (illinois.edu)
One key step to extend drug development related to GABA A receptors is likely to require deeper understanding of the adaptational mechanisms of neurons, receptors themselves with interacting proteins, and finally receptor subunits during drug action and in neuropsychiatric disease processes. (aspetjournals.org)
Several genes associated with childhood absence epilepsy provide instructions for making pieces (subunits) of the GABA A receptor protein. (medlineplus.gov)
Hirose S. Mutant GABA(A) receptor subunits in genetic (idiopathic) epilepsy. (medlineplus.gov)
Its application in the case of brain mRNAs for the GABAA receptor is illustrated, including the production of receptor subunits and its chloride channel with characteristic pharmacology. (xenbase.org)

Lancel, M. Role of GABAA receptors in the regulation of sleep: initial sleep responses to peripherally administered modulators and agonists. (nature.com)
One of the main problems in clinical use of GABA A receptor agonists is the development of tolerance. (aspetjournals.org)

Background: γ-Aminobutyric acid (GABA) receptors play a central role in fast inhibitory neurotransmission in insects. (eurekaselect.com)
Furthermore, using a gephyrin dominant-negative approach, we showed that the increased residency time of γ2 at inhibitory synapses was due to receptor-scaffold interactions. (nih.gov)
The γ-aminobutyric acid (GABA) type A receptor system, the main fast-acting inhibitory neurotransmitter system in the brain, is the pharmacological target for many drugs used clinically to treat, for example, anxiety disorders and epilepsy, and to induce and maintain sedation, sleep, and anesthesia. (aspetjournals.org)
GABA A receptors mediate the major inhibitory synaptic transmission in the central nervous system, and form a number of binding sites for clinically important drugs such as benzodiazepines. (edu.hk)
[5] Gamma-aminobutyric acid (GABA) and glycine, conversely, serve as the major inhibitory neurotransmitters. (nih.gov)
GABA, for example, can account for approximately 40% of the inhibitory processing in the brain. (nih.gov)
The day after drinking we get what we call a glutamate storm - so you've got much more glutamate binding and working in the brain and not enough of the inhibitory, calming brain chemical, gaba," Professor Currie said. (beyondblue.org.au)

Baclofen, a gamma-aminobutyric acid 'B-receptor' agonist, has long been used to treat spasticity from neurological diseases, at a dose of 30-90 mg/day. (clinicaltrials.gov)
Investigation of gamma-aminobutyric acid (GABA) A receptors genes and migraine susceptibility. (cdc.gov)

Methods: We have reviewed studies on native and recombinant insect GABA-gated chloride channels, their interactions with ligands acting at orthosteric and allosteric sites and their interactions with insecticides. (eurekaselect.com)

In the present work, we more closely examined the pharmacological action of thymol on the native GABAA receptor by using primary cultures of cortical neurons. (uchile.cl)

The flux of neurotransmitter receptors in and out of synapses depends on receptor interaction with scaffolding molecules. (nih.gov)
Functional expression in the Xenopus oocyte of messenger ribonucleic acids encoding brain neurotransmitter receptors: further characterisation of the implanted GABA receptor. (xenbase.org)

Several classes of insecticides targeting insect GABA-gated chloride channels have been developed. (eurekaselect.com)
Since some GABA receptor modulators act on L-glutamate-gated chloride channels, some comparisons are included. (eurekaselect.com)
Results: The actions on GABA-gated chloride channels of polychlorocycloalkanes, cyclodienes, macrocyclic lactones, phenylpyrazoles, isoxazolines, and metadiamides are described and the mechanisms of action of members of these insecticide classes are addressed. (eurekaselect.com)
Toxicity issues relating to insecticides targeting GABA-gated chloride channels are also addressed. (eurekaselect.com)
An overview of all major insecticide classes targeting insect GABA-gated chloride channels has enhanced our understanding of these important receptors and their insecticide binding sites. (eurekaselect.com)
GABA-A receptors control chloride channels formed by the receptor complex itself. (bvsalud.org)

Recent studies have reported enhanced GABAA receptor-operated chloride channel activity and increased binding affinity of [3H]flunitrazepam in the presence of thymol. (uchile.cl)
This direct effect was inhibited by competitive and non-competitive GABAA receptor antagonists. (uchile.cl)
These results confirm that thymol is a positive allosteric modulator of the GABAA receptor. (uchile.cl)

However, the crowd of transmembrane proteins and the rich cytoskeletal environment may constitute obstacles to the diffusion of receptors within the synapse. (nih.gov)
GABA-B receptors act through G-proteins on several effector systems, are insensitive to bicuculline, and have a high affinity for L-baclofen. (bvsalud.org)

The data are consistent with a model in which both gabazine and bicuculline act as allosteric inhibitors of channel opening for the GABA A receptor after binding to the GABA-binding site. (jneurosci.org)

We conclude that the sites for binding steroids and barbiturates do not overlap with the GABA-binding site. (jneurosci.org)
In particular, steroids and barbiturates are each able to directly gate the GABA A receptor channel (in the absence of GABA), and they can also enhance the activation produced by low concentrations of GABA. (jneurosci.org)
These data indicate that steroids and barbiturates do not bind to the GABA-binding site when they directly gate the channel of the GABA A receptor. (jneurosci.org)

Smith, G.B. & Olsen, R.W. Functional domains of GABAA receptors. (nature.com)

We find that simulated binding impulses to varying clusters of GABA binding site residues produce channel opening, and that equivalent impulses to single GABA sites produce partial opening. (archives-ouvertes.fr)
Accordingly, we have examined the ability of alphaxalone to gate mutated GABA A receptors, and we found that residues that are important in determining the binding affinity of GABA do not affect activation by steroids. (jneurosci.org)

Pharmacological manipulation of these receptors has differential effects on sleep onset and sleep maintenance insomnia. (nature.com)
More knowledge has been obtained on the mechanisms of GABA A receptor trafficking and cell surface expression and the processes that may contribute to tolerance, although their possible pharmacological regulation is not known. (aspetjournals.org)

Thymol enhanced GABA-induced (5 μM) chloride influx at concentrations lower than those exhibiting direct activity in the absence of GABA (EC50 = 12 μM and 135 μM, respectively). (uchile.cl)

For the sites involved in potentiation, however, the steroid-binding site and the barbiturate-binding site are distinct from each other and are also distinct from the GABA-binding site ( Macdonald and Olsen, 1993 ). (jneurosci.org)
Previous work indicates that potentiation of these receptors in the spinal cord evokes profound antihyperalgesia also after systemic administration, but possible synergistic or antagonistic actions of supraspinal 2-GABA A Rs on spinal antihyperalgesia have not yet been addressed. (illinois.edu)

When associated with mutations in GABA A receptor or calcium channel genes, it seems to follow an autosomal dominant inheritance pattern, which means one copy of the altered gene in each cell is sufficient to increase the likelihood of the disorder. (medlineplus.gov)

Chemical synaptic transmission primarily through the release of neurotransmitters from presynaptic neural cells to postsynaptic receptors. (nih.gov)

Gottesmann, C. GABA mechanisms and sleep. (nature.com)

Many lines of evidence indicate that GABA and GABA A receptors make important contributions to human sleep regulation. (nature.com)
These experiments uncouple the regulation of sleep latency from that of sleep duration and suggest that the kinetics of GABA A receptor signaling dictate sleep latency. (nature.com)

Various other compounds also bind to the GABA A receptor and can gate the channel or modulate channel function ( Macdonald and Olsen, 1993 ). (jneurosci.org)
Zinc and copper modulate differentially the P2X receptor. (cdc.gov)

The Xenopus oocyte is the only system currently available for the full expression of mRNAS encoding membrane receptors and ion channels. (xenbase.org)

Using a pharmacophoric model that includes a hydrogen bond donor group as well as an aromatic ring with two aliphatic substituents, we propose to demonstrate the molecular essential features of these compounds to interact with GABAA receptors. (uchile.cl)

We have performed a parallel tempering crankshaft motion Monte Carlo simulation on a model of the GABA type A receptor with the aim of exploring a wide variety of local conformational space. (archives-ouvertes.fr)

Here we generated two lines of GABA A R-mutated mice, which either lack 2-GABA A Rs specifically from the spinal cord, or, which express only benzodiazepine-insensitive 2-GABA A Rs at this site. (illinois.edu)
However, antihyperalgesia by systemic HZ166 was reduced in both mutated mouse lines by about 60% and was virtually indistinguishable from that of global point-mutated mice, in which all 2-GABA A Rs were benzodiazepine insensitive. (illinois.edu)

The major (2-dependent) component of GABA A R-mediated antihyperalgesia was therefore exclusively of spinal origin, whereas supraspinal 2-GABA A Rs had neither synergistic nor antagonistic effects on antihyperalgesia. (illinois.edu)

GABA activates a ligand-gated ion channel (the GABA A receptor), which underlies most rapid inhibition in the brain. (jneurosci.org)
Alcohol targets two receptors in the brain, which send messages to our nervous system. (beyondblue.org.au)

Figure 6: CBZ specifically increases RDL desensitization and the A302S mutation prevents CBZ effects ( a ) Response to 90-s application of 100 μM GABA with variable doses of CBZ, recorded from oocytes expressing RDL held at −60 mV under voltage clamp. (nature.com)
It is not known whether the same sites are involved in producing direct gating and in potentiating the effects of GABA. (jneurosci.org)

Our data further reveal that the confinement and the dwell time but not the diffusion coefficient report on the synapse specific sorting, trapping and accumulation of receptors. (nih.gov)

We are interested in defining the sites on the GABA A receptor that are involved in direct gating by anesthetics, and we have initiated studies of channel activation by alphaxalone (an anesthetic steroid analog) and pentobarbital (an anesthetic barbiturate). (jneurosci.org)

It is a competitive antagonist for GABA-A receptors. (curehunter.com)

Here we show that sleep is regulated by GABA in Drosophila and that a mutant GABA A receptor, Rdl A302S , specifically decreases sleep latency. (nature.com)

Anatomy53

Organisms14

Diseases8

Chemicals and Drugs136

Analytical, Diagnostic and Therapeutic Techniques and Equipment13

Psychiatry and Psychology5

Phenomena and Processes25

Disciplines and Occupations2

Health Care1

Why are there so few resistance-associated mutations in insecticide target genes? (1/3892)

Somatic recording of GABAergic autoreceptor current in cerebellar stellate and basket cells. (2/3892)

Peripheral-type benzodiazepine receptor (PBR) in human breast cancer: correlation of breast cancer cell aggressive phenotype with PBR expression, nuclear localization, and PBR-mediated cell proliferation and nuclear transport of cholesterol. (3/3892)

Synaptic activation of GABAA receptors induces neuronal uptake of Ca2+ in adult rat hippocampal slices. (4/3892)

Retinal input induces three firing patterns in neurons of the superficial superior colliculus of neonatal rats. (5/3892)

Postnatal development of hippocampal dentate granule cell gamma-aminobutyric acidA receptor pharmacological properties. (6/3892)

Dopamine receptor subtypes modulate olfactory bulb gamma-aminobutyric acid type A receptors. (7/3892)

Regional differences in the inhibition of mouse in vivo [3H]Ro 15-1788 binding reflect selectivity for alpha 1 versus alpha 2 and alpha 3 subunit-containing GABAA receptors. (8/3892)

No images available that match "receptors gaba a"

GABA Agonists

GABA Antagonists

GABA Agents

gamma-Aminobutyric Acid

GABA Modulators

Receptors, GABA-A

GABA Plasma Membrane Transport Proteins

Receptors, GABA-B

GABA Uptake Inhibitors

GABA-A Receptor Antagonists

GABA-A Receptor Agonists

Baclofen

Muscimol

Bicuculline

Nipecotic Acids

GABA-B Receptor Agonists

Picrotoxin

Phosphinic Acids

4-Aminobutyrate Transaminase

GABA-B Receptor Antagonists

Neural Inhibition

Glutamate Decarboxylase

Neurons

Inhibitory Postsynaptic Potentials

Patch-Clamp Techniques

Pyridazines

Synaptic Transmission

Diazepam

Vigabatrin

Vesicular Inhibitory Amino Acid Transport Proteins

Rats, Sprague-Dawley

Isonicotinic Acids

Pregnanolone

Hippocampus

Glutamic Acid

Aminobutyrates

Synapses

Benzodiazepines

GABAergic Neurons

Protein Subunits

Organic Anion Transporters

Interneurons

Sodium Oxybate

Flunitrazepam

Neurotransmitter Uptake Inhibitors

Membrane Potentials

Strychnine

Glycine

Neurotransmitter Agents

Electrophysiology

Flumazenil

Presynaptic Terminals

Crotonates

Dose-Response Relationship, Drug

Excitatory Postsynaptic Potentials

Rats, Wistar

Receptors, Glycine

Excitatory Amino Acid Antagonists

Convulsants

Glycine Agents

Chlorides

Electric Stimulation

Action Potentials

Animals, Newborn

3-Mercaptopropionic Acid

Pyramidal Cells

Cerebral Cortex

Xenopus laevis

Pregnanediones

Carbolines

6-Cyano-7-nitroquinoxaline-2,3-dione

Cerebellum

Etomidate

Anti-Anxiety Agents

Organophosphorus Compounds

Sodium Potassium Chloride Symporter Inhibitors

Ethanol

Solute Carrier Family 12, Member 2

Isoxazoles

Receptors, Presynaptic