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Receptor antagonist

Index 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. [1]

60 relations: Active site, Adrenaline, Adrenergic receptor, Agonist, Allosteric regulation, Alpha blocker, Alzheimer's disease, Analgesic, Antihistamine, Benzodiazepine, Beta blocker, Binding site, Buprenorphine, Calcium channel blocker, Cell surface receptor, Covalent bond, Cyclothiazide, Dose–response relationship, Drug, Efficacy, Enzyme inhibitor, Ethanol, Flumazenil, Functional selectivity, GlaxoSmithKline, Greek language, Growth factor receptor inhibitor, Heroin, Histamine, Histamine H1 receptor, Hormone, IC50, Intracellular receptor, Inverse agonist, Ligand (biochemistry), Memantine, Metabotropic glutamate receptor 1, Methadone, Mitochondrion, Morphine, Naloxone, NMDA receptor, Non-covalent interactions, Norepinephrine, Nuclear receptor, Opioid overdose, Opioid receptor, Pharmacology, Phenoxybenzamine, Physiological agonism and antagonism, ..., Potency (pharmacology), Protein, Receptor (biochemistry), Receptor antagonist, Receptor theory, Receptor–ligand kinetics, Ro15-4513, Schild regression, Selective receptor modulator, Vasodilation. Expand index (10 more) »

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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Adrenaline, also known as adrenalin or epinephrine, is a hormone, neurotransmitter, and medication.

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Adrenergic receptor

The adrenergic receptors (or adrenoceptors) are a class of G protein-coupled receptors that are targets of the catecholamines, especially norepinephrine (noradrenaline) and epinephrine (adrenaline).

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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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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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Alpha blocker

Alpha-blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors).

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Alzheimer's disease

Alzheimer's disease (AD), also referred to simply as Alzheimer's, is a chronic neurodegenerative disease that usually starts slowly and worsens over time.

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An analgesic or painkiller is any member of the group of drugs used to achieve analgesia, relief from pain.

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Antihistamines are drugs which treat allergic rhinitis and other allergies.

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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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Beta blocker

Beta blockers, also written β-blockers, are a class of medications that are particularly used to manage abnormal heart rhythms, and to protect the heart from a second heart attack (myocardial infarction) after a first heart attack (secondary prevention).

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Binding site

In biochemistry, a binding site is a region on a protein or piece of DNA or RNA to which ligands (specific molecules and/or ions) may form a chemical bond.

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Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid addiction, acute pain, and chronic pain.

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Calcium channel blocker

Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are several medications that disrupt the movement of calcium through calcium channels.

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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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Covalent bond

A covalent bond, also called a molecular bond, is a chemical bond that involves the sharing of electron pairs between atoms.

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Cyclothiazide (Anhydron, Acquirel, Doburil, Fluidil, Renazide, Tensodiural, Valmiran) is a benzothiadiazide (thiazide) diuretic and antihypertensive that was originally introduced in the United States in 1963 by Eli Lilly and was subsequently also marketed in Europe and Japan.

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Dose–response relationship

The dose–response relationship, or exposure–response relationship, describes the change in effect on an organism caused by differing levels of exposure (or doses) to a stressor (usually a chemical) after a certain exposure time, or to a food.

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A drug is any substance (other than food that provides nutritional support) that, when inhaled, injected, smoked, consumed, absorbed via a patch on the skin, or dissolved under the tongue causes a temporary physiological (and often psychological) change in the body.

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Efficacy is the ability to get a job done satisfactorily.

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Enzyme inhibitor

4QI9) An enzyme inhibitor is a molecule that binds to an enzyme and decreases its activity.

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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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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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Functional selectivity

Functional selectivity (or “agonist trafficking”, “biased agonism”, “biased signalling”, "ligand bias" and “differential engagement”) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor.

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GlaxoSmithKline plc (GSK) is a British pharmaceutical company headquartered in Brentford, London.

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Greek language

Greek (Modern Greek: ελληνικά, elliniká, "Greek", ελληνική γλώσσα, ellinikí glóssa, "Greek language") is an independent branch of the Indo-European family of languages, native to Greece and other parts of the Eastern Mediterranean and the Black Sea.

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Growth factor receptor inhibitor

Growth factor receptor inhibitors (growth factor inhibitors, growth factor receptor blockers, growth factor blockers, growth factor receptor antagonists, growth factor antagonists) are drugs that target the growth factor receptors of cells.

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Heroin, also known as diamorphine among other names, is an opioid most commonly used as a recreational drug for its euphoric effects.

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Histamine is an organic nitrogenous compound involved in local immune responses, as well as regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus.

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Histamine H1 receptor

The H1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors.

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A hormone (from the Greek participle “ὁρμῶ”, "to set in motion, urge on") is any member of a class of signaling molecules produced by glands in multicellular organisms that are transported by the circulatory system to target distant organs to regulate physiology and behaviour.

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The half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function.

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Intracellular receptor

Intracellular receptors are receptors located inside the cell rather than on its cell membrane.

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Inverse agonist

In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist.

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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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Memantine is used to treat moderate to severe Alzheimer's disease. It acts on the glutamatergic system by blocking NMDA receptors. It was first synthesized by Eli Lilly and Company in 1968 as a potential agent to treat diabetes; the NMDA activity was discovered in the 1980s.

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Metabotropic glutamate receptor 1

The glutamate receptor, metabotropic 1, also known as GRM1, is a human gene which encodes the metabotropic glutamate receptor 1 (mGluR1) protein.

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Methadone, sold under the brand name Dolophine among others, is an opioid used to treat pain and as maintenance therapy or to help with tapering in people with opioid dependence.

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The mitochondrion (plural mitochondria) is a double-membrane-bound organelle found in most eukaryotic organisms.

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Morphine is a pain medication of the opiate variety which is found naturally in a number of plants and animals.

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Naloxone, sold under the brandname Narcan among others, is a medication used to block the effects of opioids, especially in overdose.

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NMDA receptor

The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel protein found in nerve cells.

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Non-covalent interactions

A non-covalent interaction differs from a covalent bond in that it does not involve the sharing of electrons, but rather involves more dispersed variations of electromagnetic interactions between molecules or within a molecule.

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Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as a hormone and neurotransmitter.

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Nuclear receptor

In the field of molecular biology, nuclear receptors are a class of proteins found within cells that are responsible for sensing steroid and thyroid hormones and certain other molecules.

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Opioid overdose

An opioid overdose is toxicity due to excessive opioids.

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Opioid receptor

Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands.

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Pharmacology is the branch of biology concerned with the study of drug action, where a drug can be broadly defined as any man-made, natural, or endogenous (from within body) molecule which exerts a biochemical or physiological effect on the cell, tissue, organ, or organism (sometimes the word pharmacon is used as a term to encompass these endogenous and exogenous bioactive species).

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Phenoxybenzamine (marketed under the trade name Dibenzyline) is a non-selective, irreversible alpha blocker.

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Physiological agonism and antagonism

Physiological agonism describes the action of a substance which ultimately produces the same effects in the body as another substance—as if they were both agonists at the same receptor—without actually binding to the same receptor.

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Potency (pharmacology)

In the field of pharmacology, potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity.

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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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Receptor (biochemistry)

In biochemistry and pharmacology, a receptor is a protein molecule that receives chemical signals from outside a cell.

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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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Receptor theory

Receptor theory is the application of receptor models to explain drug behavior.

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Receptor–ligand kinetics

In biochemistry, receptor–ligand kinetics is a branch of chemical kinetics in which the kinetic species are defined by different non-covalent bindings and/or conformations of the molecules involved, which are denoted as receptor(s) and ligand(s).

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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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Schild regression

Schild regression analysis, named for Heinz Otto Schild, is a useful tool for studying the effects of agonists and antagonists on the cellular response caused by the receptor or on ligand-receptor binding.

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Selective receptor modulator

In the field of pharmacology, a selective receptor modulator or SRM is a type of drug that has different effects in different tissues.

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Vasodilation is the widening of blood vessels.

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

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