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GABAA receptor

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The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. [1]

140 relations: Action potential, Active site, Adipiplon, Agonist, Alcohol (drug), Allosteric modulator, Allosteric regulation, Amentoflavone, Amnesia, Anesthetic, Anticonvulsant, Anxiety, Anxiolytic, Ataxia, Barbiturate, Benzodiazepine, Bicuculline, Bretazenil, Cancer, Carbamate, Carisoprodol, Cell growth, Cell membrane, Cell surface receptor, Central nervous system, Channel blocker, Chloride, Cicutoxin, CL-218,872, Convulsion, Dendrite, Depolarization, Diproqualone, Endocrine system, Endogeny (biology), Epigallocatechin gallate, Epiphyseal plate, Eszopiclone, Etaqualone, Ethanol, Etomidate, Euphoria, Flumazenil, GABA receptor, GABAA receptor negative allosteric modulator, GABAA receptor positive allosteric modulator, GABAA-rho receptor, GABAB receptor, Gabazine, Gaboxadol, ..., GABRA2, GABRA3, GABRA4, GABRA5, GABRA6, GABRB1, GABRB2, GABRB3, GABRD, GABRE, GABRG1, GABRG2, GABRG3, GABRP, GABRQ, GABRR1, GABRR2, GABRR3, Gamma-Aminobutyric acid, Gamma-aminobutyric acid receptor subunit alpha-1, Gephyrin, Glutethimide, Glycine receptor, Hallucinogen, Hypnotic, Imidazenil, Inhalational anaesthetic, Inhibitory postsynaptic potential, Inosine, International Union of Basic and Clinical Pharmacology, Ion, Ion channel, Isoguvacine, Kavalactone, L-838,417, Lanthanum, Leydig cell, Ligand (biochemistry), Ligand-gated ion channel, Lindane, Liver, Lorbamate, Membrane potential, Meprobamate, Methaqualone, Muscimol, Muscle relaxant, Neuron, Neurosteroid, Neurotransmission, Neurotransmitter, Niacin, Nicotinamide, Nicotinic acetylcholine receptor, Nomenclature, Nonbenzodiazepine, Nootropic, Oenanthotoxin, Pentylenetetrazol, Picrotoxin, Placenta, Progabide, Propofol, Protein, Protein isoform, QH-II-66, Quinazolinone, Receptor antagonist, Reversal potential, Riluzole, Ro15-4513, Sarmazenil, Sedation, Sedative, SL-651,498, Soma (biology), Stiripentol, Synapse, Thalamic reticular nucleus, Theanine, Thienodiazepine, Thujone, Translocator protein, Valerenic acid, White blood cell, Z-drug, Zinc, Zolpidem, 4-Iodopropofol, 5-HT3 receptor. Expand index (90 more) »

Action potential

In physiology, an action potential occurs when the membrane potential of a specific axon location rapidly rises and falls: this depolarisation then causes adjacent locations to similarly depolarise.

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Active site

In biology, the active site is the region of an enzyme where substrate molecules bind and undergo a chemical reaction.

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Adipiplon (NG2-73) is an anxiolytic drug developed by Neurogen Corporation.

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An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response.

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Alcohol (drug)

Alcohol, also known by its chemical name ethanol, is a psychoactive substance or drug that is the active ingredient in alcoholic beverages such as beer, wine, and distilled spirits (hard liquor).

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Allosteric modulator

In biochemistry and pharmacology, an allosteric modulator (allo- from the Greek meaning "other") is a substance which indirectly influences (modulates) the effects of a primary ligand that directly activates or deactivates the function of a target protein.

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Allosteric regulation

In biochemistry, allosteric regulation (or allosteric control) is the regulation of an enzyme by binding an effector molecule at a site other than the enzyme's active site.

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Amentoflavone is a biflavonoid (bis-apigenin coupled at 8 and 3' positions, or 3′,8′′-biapigenin) constituent of a number of plants including Ginkgo biloba, Chamaecyparis obtusa (hinoki), Hypericum perforatum (St. John’s Wort) and Xerophyta plicata.

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Amnesia is a deficit in memory caused by brain damage, disease, or psychological trauma.

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An anesthetic (or anaesthetic) is a drug to prevent pain during surgery, completely blocking any feeling as opposed to an analgesic.

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Anticonvulsants (also commonly known as antiepileptic drugs or as antiseizure drugs) are a diverse group of pharmacological agents used in the treatment of epileptic seizures.

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Anxiety is an emotion characterized by an unpleasant state of inner turmoil, often accompanied by nervous behaviour such as pacing back and forth, somatic complaints, and rumination.

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An anxiolytic (also antipanic or antianxiety agent) is a medication or other intervention that inhibits anxiety.

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Ataxia is a neurological sign consisting of lack of voluntary coordination of muscle movements that includes gait abnormality.

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A barbiturate is a drug that acts as a central nervous system depressant, and can therefore produce a wide spectrum of effects, from mild sedation to death.

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Benzodiazepines (BZD, BZs), sometimes called "benzos", are a class of psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring.

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Bicuculline is a phthalide-isoquinoline compound that is a light-sensitive competitive antagonist of GABAA receptors.

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Bretazenil (Ro16-6028) is an imidazopyrrolobenzodiazepine anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988.

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Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body.

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A carbamate is an organic compound derived from carbamic acid (NH2COOH).

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Carisoprodol, marketed under the brand name Soma among others, is a prescription drug marketed since 1959.

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Cell growth

The term cell growth is used in the contexts of biological cell development and cell division (reproduction).

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Cell membrane

The cell membrane (also known as the plasma membrane or cytoplasmic membrane, and historically referred to as the plasmalemma) is a biological membrane that separates the interior of all cells from the outside environment (the extracellular space).

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Cell surface receptor

Cell surface receptors (membrane receptors, transmembrane receptors) are receptors that are embedded in the membranes of cells.

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Central nervous system

The central nervous system (CNS) is the part of the nervous system consisting of the brain and spinal cord.

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Channel blocker

A channel blocker is the biological mechanism in which a particular molecule is used to prevent the opening of ion channels in order to produce a physiological response in a cell.

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The chloride ion is the anion (negatively charged ion) Cl−.

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Cicutoxin is a poisonous polyyne and alcohol found in various plants, such as the highly toxic water hemlock (Cicuta species).

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CL-218,872 is a sedative and hypnotic drug used in scientific research.

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A convulsion is a medical condition where body muscles contract and relax rapidly and repeatedly, resulting in an uncontrolled shaking of the body.

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Dendrites (from Greek δένδρον déndron, "tree"), also dendrons, are branched protoplasmic extensions of a nerve cell that propagate the electrochemical stimulation received from other neural cells to the cell body, or soma, of the neuron from which the dendrites project.

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In biology, depolarization is a change within a cell, during which the cell undergoes a shift in electric charge distribution, resulting in less negative charge inside the cell.

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Diproqualone is a quinazolinone class GABAergic and is an analogue of methaqualone developed in the late 1950s by a team at Nogentaise de Produits Chimique.

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Endocrine system

The endocrine system is a chemical messenger system consisting of hormones, the group of glands of an organism that carry those hormones directly into the circulatory system to be carried towards distant target organs, and the feedback loops of homeostasis that the hormones drive.

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Endogeny (biology)

Endogenous substances and processes are those that originate from within an organism, tissue, or cell.

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Epigallocatechin gallate

Epigallocatechin gallate (EGCG), also known as epigallocatechin-3-gallate, is the ester of epigallocatechin and gallic acid, and is a type of catechin.

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Epiphyseal plate

The epiphyseal plate (or epiphysial plate, physis, or growth plate) is a hyaline cartilage plate in the metaphysis at each end of a long bone.

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Eszopiclone, marketed by Sunovion under the brand-name Lunesta, is a nonbenzodiazepine hypnotic agent used in the treatment of insomnia.

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Etaqualone (Aolan, Athinazone, Ethinazone) is a quinazolinone-class GABAergic and is an analogue of methaqualone that was developed in the 1960s and marketed mainly in France and some other European countries.

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Ethanol, also called alcohol, ethyl alcohol, grain alcohol, and drinking alcohol, is a chemical compound, a simple alcohol with the chemical formula.

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Etomidate (USAN, INN, BAN) (marketed as Amidate) is a short-acting intravenous anaesthetic agent used for the induction of general anaesthesia and sedation for short procedures such as reduction of dislocated joints, tracheal intubation, and cardioversion.

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Euphoria is an affective state in which a person experiences pleasure or excitement and intense feelings of well-being and happiness.

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Flumazenil (also known as flumazepil, code name Ro 15-1788) is a selective benzodiazepine receptor antagonist available by injection and intranasal.

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GABA receptor

The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory compound in the mature vertebrate central nervous system.

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GABAA receptor negative allosteric modulator

A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel of the major inhibitory neurotransmitter γ-aminobutyric acid (GABA).

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GABAA receptor positive allosteric modulator

In pharmacology, GABAA receptor positive allosteric modulators are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system.

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GABAA-rho receptor

The GABAA-rho receptor (previously known as the GABAC receptor) is a subclass of GABAA receptors composed entirely of rho (ρ) subunits.

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GABAB receptor

GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) that are linked via G-proteins to potassium channels.

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Gabazine (SR-95531) is a drug that acts as an antagonist at GABAA receptors.

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Gaboxadol, also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP), is a conformationally constrained derivative of the alkaloid muscimol that was first synthesized in 1977 by the Danish chemist Povl Krogsgaard-Larsen.

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Gamma-aminobutyric acid receptor subunit alpha-2 is a protein in humans that is encoded by the GABRA2 gene.

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Gamma-aminobutyric acid receptor subunit alpha-3 is a protein that in humans is encoded by the GABRA3 gene.

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Gamma-aminobutyric acid receptor subunit alpha-4 is a protein that in humans is encoded by the GABRA4 gene.

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Gamma-aminobutyric acid (GABA) A receptor, alpha 5, also known as GABRA5, is a protein which in humans is encoded by the GABRA5 gene.

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Gamma-aminobutyric acid receptor subunit alpha-6 is a protein that in humans is encoded by the GABRA6 gene.

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Gamma-aminobutyric acid receptor subunit beta-1 is a protein that in humans is encoded by the GABRB1 gene.

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Gamma-aminobutyric acid receptor subunit beta-2 is a protein that in humans is encoded by the GABRB2 gene.

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Gamma-aminobutyric acid receptor subunit beta-3 is a protein that in humans is encoded by the GABRB3 gene.

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Gamma-aminobutyric acid receptor subunit delta is a protein that in humans is encoded by the GABRD gene.

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Gamma-aminobutyric acid receptor subunit epsilon is a protein that in humans is encoded by the GABRE gene.

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Gamma-aminobutyric acid receptor subunit gamma-1 is a protein that in humans is encoded by the GABRG1 gene.

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Gamma-aminobutyric acid receptor subunit gamma-2 is a protein that in humans is encoded by the GABRG2 gene.

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GABAA receptor-γ3, also known as GABRG3, is a protein which in humans is encoded by the GABRG3 gene.

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Gamma-aminobutyric acid receptor subunit pi is a protein that in humans is encoded by the GABRP gene.

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Gamma-aminobutyric acid receptor subunit theta is a protein that in humans is encoded by theGABRQ gene.

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Gamma-aminobutyric acid receptor subunit rho-1 is a protein that in humans is encoded by the GABRR1 gene.

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Gamma-aminobutyric acid receptor subunit rho-2 is a protein that in humans is encoded by the GABRR2 gene.

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Gamma-aminobutyric acid receptor subunit rho-3 is a protein that in humans is encoded by the GABRR3 gene.

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Gamma-Aminobutyric acid

gamma-Aminobutyric acid, or γ-aminobutyric acid, or GABA, is the chief inhibitory neurotransmitter in the mammalian central nervous system.

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Gamma-aminobutyric acid receptor subunit alpha-1

Gamma-aminobutyric acid receptor subunit alpha-1 is a protein that in humans is encoded by the GABRA1 gene.

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Gephyrin is a protein that in humans is encoded by the GPHN gene.

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Glutethimide is a hypnotic sedative that was introduced by Ciba in 1954 as a safe alternative to barbiturates to treat insomnia.

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Glycine receptor

The glycine receptor (abbreviated as GlyR or GLR) is the receptor of the amino acid neurotransmitter glycine.

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A hallucinogen is a psychoactive agent which can cause hallucinations, perceptual anomalies, and other substantial subjective changes in thoughts, emotion, and consciousness.

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Hypnotic (from Greek Hypnos, sleep) or soporific drugs, commonly known as sleeping pills, are a class of psychoactive drugs whose primary function is to induce sleep and to be used in the treatment of insomnia (sleeplessness), or surgical anesthesia.

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Imidazenil is an experimental anxiolytic drug which is derived from the benzodiazepine family, and is most closely related to other imidazobenzodiazepines such as midazolam, flumazenil, and bretazenil.

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Inhalational anaesthetic

An inhalational anaesthetic is a chemical compound possessing general anaesthetic properties that can be delivered via inhalation.

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Inhibitory postsynaptic potential

An inhibitory postsynaptic potential (IPSP) is a kind of synaptic potential that makes a postsynaptic neuron less likely to generate an action potential.

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Inosine is a nucleoside that is formed when hypoxanthine is attached to a ribose ring (also known as a ribofuranose) via a β-N9-glycosidic bond.

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International Union of Basic and Clinical Pharmacology

The International Union of Basic and Clinical Pharmacology (IUPHAR) is a voluntary, non-profit association representing the interests of scientists in pharmacology-related fields to facilitate Better Medicines through Global Education and Research around the world.

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An ion is an atom or molecule that has a non-zero net electrical charge (its total number of electrons is not equal to its total number of protons).

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Ion channel

Ion channels are pore-forming membrane proteins that allow ions to pass through the channel pore.

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Isoguvacine is a GABAA receptor agonist used in scientific research.

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Kavalactones are a class of lactone compounds found in the kava shrub.

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L-838,417 is an anxiolytic drug used in scientific research.

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Lanthanum is a chemical element with symbol La and atomic number 57.

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Leydig cell

Leydig cells, also known as interstitial cells of Leydig, are found adjacent to the seminiferous tubules in the testicle.

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Ligand (biochemistry)

In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose.

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Ligand-gated ion channel

Ligand-gated ion channels (LICs, LGIC), also commonly referred as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow ions such as Na+, K+, Ca2+, and/or Cl− to pass through the membrane in response to the binding of a chemical messenger (i.e. a ligand), such as a neurotransmitter.

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Lindane, also known as gamma-hexachlorocyclohexane (γ-HCCH), gammaxene, Gammallin and sometimes incorrectly called benzene hexachloride (BHC), is an organochlorine chemical variant of hexachlorocyclohexane that has been used both as an agricultural insecticide and as a pharmaceutical treatment for lice and scabies.

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The liver, an organ only found in vertebrates, detoxifies various metabolites, synthesizes proteins, and produces biochemicals necessary for digestion.

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Lorbamate (INN; Abbott-19,957) is a muscle relaxant and tranquilizer of the carbamate family which was never marketed.

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Membrane potential

The term "membrane potential" may refer to one of three kinds of membrane potential.

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Meprobamate — marketed as Miltown by Wallace Laboratories and Equanil by Wyeth, among others — is a carbamate derivative used as an anxiolytic drug.

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Methaqualone, sold under the brand name Quaalude (pronounced) and sometimes stylized "Quāālude" in the United States and Mandrax in the United Kingdom and South Africa, is a sedative and hypnotic medication.

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Muscimol (also known as agarin or pantherine) is one of the principal psychoactive constituents of Amanita muscaria and related species of mushroom.

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Muscle relaxant

A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone.

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A neuron, also known as a neurone (British spelling) and nerve cell, is an electrically excitable cell that receives, processes, and transmits information through electrical and chemical signals.

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Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors.

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Neurotransmission (Latin: transmissio "passage, crossing" from transmittere "send, let through"), also called synaptic transmission, is the process by which signaling molecules called neurotransmitters are released by the axon terminal of a neuron (the presynaptic neuron), and bind to and activate the receptors on the dendrites of another neuron (the postsynaptic neuron).

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Neurotransmitters are endogenous chemicals that enable neurotransmission.

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Niacin, also known as nicotinic acid, is an organic compound and a form of vitamin B3, an essential human nutrient.

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Nicotinamide (NAA), also known as niacinamide, is a form of vitamin B3 found in food and used as a dietary supplement and medication.

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Nicotinic acetylcholine receptor

Nicotinic acetylcholine receptors, or nAChRs, are receptor proteins that respond to the neurotransmitter acetylcholine.

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Nomenclature is a system of names or terms, or the rules for forming these terms in a particular field of arts or sciences.

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Nonbenzodiazepines (sometimes referred to colloquially as "Z-drugs") are a class of psychoactive drugs that are very benzodiazepine-like in nature.

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Nootropics, also known as smart drugs and cognitive enhancers, are drugs, supplements, and other substances that purport to improve cognitive function, particularly executive functions, memory, creativity, or motivation, in healthy individuals.

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Oenanthotoxin is a toxin extracted from hemlock water dropwort (Oenanthe crocata) and other plants of the genus Oenanthe.

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Pentylenetetrazol, also known as pentylenetetrazole, metrazol, pentetrazol (INN), pentamethylenetetrazol, Corazol, Cardiazol, deumacard or PTZ, is a drug formerly used as a circulatory and respiratory stimulant.

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Picrotoxin, also known as cocculin, is a poisonous crystalline plant compound.

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The placenta is an organ that connects the developing fetus to the uterine wall to allow nutrient uptake, thermo-regulation, waste elimination, and gas exchange via the mother's blood supply; to fight against internal infection; and to produce hormones which support pregnancy.

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Progabide (INN) (trade name Gabrene, Sanofi-Aventis) is an analogue and prodrug of γ-aminobutyric acid (GABA) used in the treatment of epilepsy.

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Propofol, marketed as Diprivan among others, is a short-acting medication that results in a decreased level of consciousness and lack of memory for events.

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Proteins are large biomolecules, or macromolecules, consisting of one or more long chains of amino acid residues.

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Protein isoform

A protein isoform, or "protein variant" is a member of a set of highly similar proteins that originate from a single gene or gene family and are the result of genetic differences.

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QH-II-66 (QH-ii-066) is a sedative drug which is a benzodiazepine derivative.

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Quinazolinone is a heterocyclic chemical compound, a quinazoline with a keto group.

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Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist.

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Reversal potential

In a biological membrane, the reversal potential (also known as the Nernst potential) of an ion is the membrane potential at which there is no net (overall) flow of that particular ion from one side of the membrane to the other.

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Riluzole (marketed as Rilutek and Teglutik) is a drug used to treat amyotrophic lateral sclerosis.

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Ro15-4513 is a weak partial inverse agonist of the benzodiazepine class of drugs, developed by Hoffmann–La Roche in the 1980s.

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Sarmazenil (Ro15-3505) is a drug from the benzodiazepine family.

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Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure.

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A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement.

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SL-651,498 is an anxiolytic and anticonvulsant drug used in scientific research, with a chemical structure most closely related to β-carboline derivatives such as abecarnil and gedocarnil.

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Soma (biology)

The soma (pl. somata or somas), perikaryon (pl. perikarya), neurocyton, or cell body is the bulbous, non-process portion of a neuron or other brain cell type, containing the cell nucleus.

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Stiripentol (marketed as Diacomit by Laboratoires Biocodex) is an anticonvulsant drug used in the treatment of epilepsy.

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In the nervous system, a synapse is a structure that permits a neuron (or nerve cell) to pass an electrical or chemical signal to another neuron or to the target efferent cell.

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Thalamic reticular nucleus

The thalamic reticular nucleus is part of the ventral thalamus that forms a capsule around the thalamus laterally.

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Theanine, also known as L-γ-glutamylethylamide and N5-ethyl-L-glutamine, is an amino acid analogue of the proteinogenic amino acids L-glutamate and L-glutamine and is found primarily in particular plant and fungal species.

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A thienodiazepine is a heterocyclic compound containing a diazepine ring fused to a thiophene ring.

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No description.

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Translocator protein

Translocator protein (TSPO) is an 18 kDa protein mainly found on the outer mitochondrial membrane.

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Valerenic acid

Valerenic acid is a sesquiterpenoid constituent of the essential oil of the Valerian plant.

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White blood cell

White blood cells (WBCs), also called leukocytes or leucocytes, are the cells of the immune system that are involved in protecting the body against both infectious disease and foreign invaders.

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Z-drugs are a group of nonbenzodiazepine drugs with effects similar to benzodiazepines, which are used in the treatment of trouble sleeping, and most of whose names start with the letter "Z".

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Zinc is a chemical element with symbol Zn and atomic number 30.

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Zolpidem, sold under the brand name Ambien, among others, is a sedative primarily used for the treatment of trouble sleeping.

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4-Iodopropofol is a drug derived from the commonly used sedative anaesthetic agent, propofol.

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5-HT3 receptor

The 5-HT3 receptor belongs to the Cys-loop superfamily of ligand-gated ion channels (LGICs) and therefore differs structurally and functionally from all other 5-HT receptors (5-hydroxytryptamine, or serotonin) receptors which are G protein-coupled receptors.

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BZ-sensitive GABAA receptor, Benzodiazepine receptor, Benzodiazepine receptors, Benzodiazepine site, GABA A receptor, GABA-A, GABA-A receptor, GABAA, GABAA receptors, GABAa receptor, GABAa receptors, Gaba a receptor, Receptors, gaba-a, Γ-Aminobutyric acid A receptor.


[1] https://en.wikipedia.org/wiki/GABAA_receptor

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