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Allosteric modulator

Index Allosteric modulator

In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimuli. [1]

Table of Contents

  1. 52 relations: Agonist, Alcohol (drug), Allosteric regulation, Alprazolam, AMPA receptor, AMPA receptor positive allosteric modulator, Aniracetam, Barbiturate, Benzodiazepine, Biochemistry, Calcium-sensing receptor, CCR5, Chemical specificity, Chlordiazepoxide, Cinacalcet, Concentration, Conformational isomerism, CX614, Cyclothiazide, Desensitization (medicine), Diazepam, Dipraglurant, Dopamine receptor D1, Dose–response relationship, Drug overdose, Evolution, Fenobam, GABAA receptor, GABAA receptor negative allosteric modulator, GABAA receptor positive allosteric modulator, Glutamic acid, Intrinsic activity, Ion channel, Ligand (biochemistry), Major depressive disorder, Maraviroc, Metabotropic glutamate receptor 5, Mevidalen, Mutation, Neurotransmitter, Nicotinic acetylcholine receptor, Partial agonist, PH, Pharmacology, Phenobarbital, Psychoactive drug, Raseglurant, Receptor (biochemistry), Receptor antagonist, Research chemical, ... Expand index (2 more) »

  2. Neuropharmacology

Agonist

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

See Allosteric modulator and Agonist

Alcohol (drug)

Alcohol, sometimes referred to by the chemical name ethanol, is one of the most widely used and abused psychoactive drugs in the world and falls under the depressant category.

See Allosteric modulator and Alcohol (drug)

Allosteric regulation

In the fields of biochemistry and pharmacology an allosteric regulator (or allosteric modulator) is a substance that binds to a site on an enzyme or receptor distinct from the active site, resulting in a conformational change that alters the protein's activity, either enhancing or inhibiting its function.

See Allosteric modulator and Allosteric regulation

Alprazolam

Alprazolam, sold under the brand name Xanax and others, is a fast-acting, potent tranquilizer of moderate duration within the triazolobenzodiazepine group of chemicals called benzodiazepines.

See Allosteric modulator and Alprazolam

AMPA receptor

The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor) is an ionotropic transmembrane receptor for glutamate (iGluR) and predominantly Na+ ion channel that mediates fast synaptic transmission in the central nervous system (CNS).

See Allosteric modulator and AMPA receptor

AMPA receptor positive allosteric modulator

AMPA receptor positive allosteric modulators are positive allosteric modulators (PAMs) of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPR), a type of ionotropic glutamate receptor which mediates most fast synaptic neurotransmission in the central nervous system.

See Allosteric modulator and AMPA receptor positive allosteric modulator

Aniracetam

Aniracetam (brand names Draganon, Sarpul, Ampamet, Memodrin, Referan), also known as N-anisoyl-2-pyrrolidinone, is a racetam which is sold in Europe as a prescription drug.

See Allosteric modulator and Aniracetam

Barbiturate

Barbiturates are a class of depressant drugs that are chemically derived from barbituric acid.

See Allosteric modulator and Barbiturate

Benzodiazepine

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

See Allosteric modulator and Benzodiazepine

Biochemistry

Biochemistry or biological chemistry is the study of chemical processes within and relating to living organisms.

See Allosteric modulator and Biochemistry

Calcium-sensing receptor

The calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ions.

See Allosteric modulator and Calcium-sensing receptor

CCR5

C-C chemokine receptor type 5, also known as CCR5 or CD195, is a protein on the surface of white blood cells that is involved in the immune system as it acts as a receptor for chemokines.

See Allosteric modulator and CCR5

Chemical specificity

Chemical specificity is the ability of binding site of a macromolecule (such as a protein) to bind specific ligands.

See Allosteric modulator and Chemical specificity

Chlordiazepoxide

Chlordiazepoxide, trade name Librium among others, is a sedative and hypnotic medication of the benzodiazepine class; it is used to treat anxiety, insomnia and symptoms of withdrawal from alcohol, benzodiazepines, and other drugs.

See Allosteric modulator and Chlordiazepoxide

Cinacalcet

Cinacalcet, sold under the brand name Sensipar among others, is a medication used to treat primary hyperparathyroidism, tertiary hyperparathyroidism and parathyroid carcinoma.

See Allosteric modulator and Cinacalcet

Concentration

In chemistry, concentration is the abundance of a constituent divided by the total volume of a mixture.

See Allosteric modulator and Concentration

Conformational isomerism

In chemistry, conformational isomerism is a form of stereoisomerism in which the isomers can be interconverted just by rotations about formally single bonds (refer to figure on single bond rotation).

See Allosteric modulator and Conformational isomerism

CX614

CX-614 is an ampakine drug developed by Cortex Pharmaceuticals.

See Allosteric modulator and CX614

Cyclothiazide

Cyclothiazide (Anhydron, Acquirel, Doburil, Fluidil, Renazide, Tensodiural, Valmiran), sometimes abbreviated CTZ, 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.

See Allosteric modulator and Cyclothiazide

Desensitization (medicine)

In medicine, desensitization is a method to reduce or eliminate an organism's negative reaction to a substance or stimulus.

See Allosteric modulator and Desensitization (medicine)

Diazepam

Diazepam, sold under the brand name Valium among others, is a medicine of the benzodiazepine family that acts as an anxiolytic.

See Allosteric modulator and Diazepam

Dipraglurant

Dipraglurant (INN) (code name ADX-48621) is a negative allosteric modulator of the mGlu5 receptor which is under development by Addex Therapeutics for the treatment of Parkinson's disease levodopa-induced dyskinesia (PD-LID).

See Allosteric modulator and Dipraglurant

Dopamine receptor D1

Dopamine receptor D1, also known as DRD1.

See Allosteric modulator and Dopamine receptor D1

Dose–response relationship

The dose–response relationship, or exposure–response relationship, describes the magnitude of the response of an organism, as a function of exposure (or doses) to a stimulus or stressor (usually a chemical) after a certain exposure time.

See Allosteric modulator and Dose–response relationship

Drug overdose

A drug overdose (overdose or OD) is the ingestion or application of a drug or other substance in quantities much greater than are recommended.

See Allosteric modulator and Drug overdose

Evolution

Evolution is the change in the heritable characteristics of biological populations over successive generations.

See Allosteric modulator and Evolution

Fenobam

Fenobam is an imidazole derivative developed by McNeil Laboratories in the late 1970s as a novel anxiolytic drug with an at-the-time-unidentified molecular target in the brain.

See Allosteric modulator and Fenobam

GABAA receptor

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

See Allosteric modulator and GABAA receptor

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).

See Allosteric modulator and GABAA receptor negative allosteric modulator

GABAA receptor positive allosteric modulator

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

See Allosteric modulator and GABAA receptor positive allosteric modulator

Glutamic acid

Glutamic acid (symbol Glu or E; the anionic form is known as glutamate) is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins.

See Allosteric modulator and Glutamic acid

Intrinsic activity

Intrinsic activity (IA) and efficacy refer to the relative ability of a drug-receptor complex to produce a maximum functional response.

See Allosteric modulator and Intrinsic activity

Ion channel

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

See Allosteric modulator and Ion channel

Ligand (biochemistry)

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

See Allosteric modulator and Ligand (biochemistry)

Major depressive disorder

Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive low mood, low self-esteem, and loss of interest or pleasure in normally enjoyable activities.

See Allosteric modulator and Major depressive disorder

Maraviroc

Maraviroc, sold under the brand names Selzentry (US) and Celsentri (EU), is an antiretroviral medication used to treat HIV infection.

See Allosteric modulator and Maraviroc

Metabotropic glutamate receptor 5

Metabotropic glutamate receptor 5 is an excitatory Gq-coupled G protein-coupled receptor predominantly expressed on the postsynaptic sites of neurons.

See Allosteric modulator and Metabotropic glutamate receptor 5

Mevidalen

Mevidalen (developmental code name LY-3154207) is a dopaminergic drug which is under development for the treatment of Lewy body disease, including those with Parkinson's disease.

See Allosteric modulator and Mevidalen

Mutation

In biology, a mutation is an alteration in the nucleic acid sequence of the genome of an organism, virus, or extrachromosomal DNA.

See Allosteric modulator and Mutation

Neurotransmitter

A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse.

See Allosteric modulator and Neurotransmitter

Nicotinic acetylcholine receptor

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

See Allosteric modulator and Nicotinic acetylcholine receptor

Partial agonist

In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist.

See Allosteric modulator and Partial agonist

PH

In chemistry, pH, also referred to as acidity or basicity, historically denotes "potential of hydrogen" (or "power of hydrogen").

See Allosteric modulator and PH

Pharmacology

Pharmacology is the science of drugs and medications, including a substance's origin, composition, pharmacokinetics, pharmacodynamics, therapeutic use, and toxicology.

See Allosteric modulator and Pharmacology

Phenobarbital

Phenobarbital, also known as phenobarbitone or phenobarb, sold under the brand name Luminal among others, is a medication of the barbiturate type.

See Allosteric modulator and Phenobarbital

Psychoactive drug

A psychoactive drug, mind-altering drug, or consciousness-altering drug is a chemical substance that changes brain function and results in alterations in perception, mood, consciousness, cognition, or behavior.

See Allosteric modulator and Psychoactive drug

Raseglurant

Raseglurant (INN) (code name ADX-10059) is a negative allosteric modulator of the mGlu5 receptor and derivative of MPEP which was under development by Addex Therapeutics for the treatment of migraine, gastroesophageal reflux disease, and dental anxiety.

See Allosteric modulator and Raseglurant

Receptor (biochemistry)

In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems.

See Allosteric modulator and Receptor (biochemistry)

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.

See Allosteric modulator and Receptor antagonist

Research chemical

Research chemicals are chemical substances scientists use for medical and scientific research purposes.

See Allosteric modulator and Research chemical

Schizophrenia

Schizophrenia is a mental disorder characterized by reoccurring episodes of psychosis that are correlated with a general misperception of reality.

See Allosteric modulator and Schizophrenia

Signs and symptoms

Signs and symptoms are the observed or detectable signs, and experienced symptoms of an illness, injury, or condition.

See Allosteric modulator and Signs and symptoms

See also

Neuropharmacology

References

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

Also known as Allosteric modulation, Negative allosteric modulation, Negative allosteric modulator, Negative allosteric modulators, Negative modulator, Negative modulators, Positive allosteric modulation, Positive allosteric modulator, Positive allosteric modulators, Positive modulator, Positive modulators.

, Schizophrenia, Signs and symptoms.