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Functional selectivity

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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. [1]

35 relations: Agonist, Agonist-antagonist, Arachidonic acid, Atypical antidepressant, Axiom, Effector (biology), Epiphenomenon, G protein, G protein–coupled receptor, Heteromer, Hypoventilation, Inositol trisphosphate, Inverse agonist, Μ-opioid receptor, Ligand (biochemistry), Lisuride, Lysergic acid diethylamide, Monoamine oxidase inhibitor, N,N-Dimethyltryptamine, Pharmacology, Phospholipase A2, Phospholipase C, Protein dimer, Psychedelic drug, Receptor (biochemistry), Receptor antagonist, Second messenger system, Selective serotonin reuptake inhibitor, Serotonin, Signal transduction, Tianeptine, 2,5-Dimethoxy-4-bromoamphetamine, 5-HT receptor, 5-HT2A receptor, 5-HT2C receptor.

Agonist

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

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Agonist-antagonist

In pharmacology the term agonist-antagonist or mixed agonist/antagonist is used to refer to a drug which under some conditions behaves as an agonist (a substance that fully activates the receptor that it binds to) while under other conditions, behaves as an antagonist (a substance that binds to a receptor but does not activate and can block the activity of other agonists).

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Arachidonic acid

Arachidonic acid (AA, sometimes ARA) is a polyunsaturated omega-6 fatty acid 20:4(ω-6).

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Atypical antidepressant

An atypical antidepressant is a type of antidepressant medication which acts in an atypical manner relative to most other antidepressants.

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Axiom

An axiom or postulate is a statement that is taken to be true, to serve as a premise or starting point for further reasoning and arguments.

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Effector (biology)

In biochemistry, an effector molecule is usually a small molecule that selectively binds to a protein and regulates its biological activity.

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Epiphenomenon

An epiphenomenon (plural: epiphenomena) is a secondary phenomenon that occurs alongside or in parallel to a primary phenomenon.

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G protein

G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell to its interior.

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G protein–coupled receptor

G protein–coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein–linked receptors (GPLR), constitute a large protein family of receptors that detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular responses.

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Heteromer

A heteromer is something that consists of different parts.

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Hypoventilation

Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (hypo meaning "below") to perform needed gas exchange.

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Inositol trisphosphate

Inositol trisphosphate or inositol 1,4,5-trisphosphate (also commonly known as triphosphoinositol; abbreviated InsP3 or Ins3P or IP3), together with diacylglycerol (DAG), is a secondary messenger molecule used in signal transduction and lipid signaling in biological cells.

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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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Μ-opioid receptor

The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins.

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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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Lisuride

Lisuride, sold under the brand names Dopergin, Proclacam, and Revanil, is an antiparkinson agent of the iso-ergoline class, chemically related to the dopaminergic ergoline Parkinson's drugs.

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Lysergic acid diethylamide

Lysergic acid diethylamide (LSD), also known as acid, is a psychedelic drug known for its psychological effects, which may include altered awareness of one's surroundings, perceptions, and feelings as well as sensations and images that seem real though they are not.

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Monoamine oxidase inhibitor

Monoamine oxidase inhibitors (MAOIs) are a class of drugs that inhibit the activity of one or both monoamine oxidase enzymes: monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B).

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N,N-Dimethyltryptamine

N,N-Dimethyltryptamine (DMT or N,N-DMT) is a tryptamine molecule which occurs in many plants and animals.

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Pharmacology

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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Phospholipase A2

Phospholipases A2 (PLA2s) are enzymes that release fatty acids from the second carbon group of glycerol.

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Phospholipase C

Phospholipase C (PLC) is a class of membrane-associated enzymes that cleave phospholipids just before the phosphate group (see figure).

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Protein dimer

In biochemistry, a protein dimer is a macromolecular complex formed by two protein monomers, or single proteins, which are usually non-covalently bound.

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Psychedelic drug

Psychedelics are a class of drug whose primary action is to trigger psychedelic experiences via serotonin receptor agonism, causing thought and visual/auditory changes, and altered state of consciousness.

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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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Second messenger system

Second messengers are intracellular signaling molecules released by the cell in response to exposure to extracellular signaling molecules—the first messengers.

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Selective serotonin reuptake inhibitor

Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that are typically used as antidepressants in the treatment of major depressive disorder and anxiety disorders.

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Serotonin

Serotonin or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter.

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Signal transduction

Signal transduction is the process by which a chemical or physical signal is transmitted through a cell as a series of molecular events, most commonly protein phosphorylation catalyzed by protein kinases, which ultimately results in a cellular response.

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Tianeptine

Tianeptine, sold under the brand names Stablon and Coaxil among others, is an atypical antidepressant which is used mainly in the treatment of major depressive disorder, although it may also be used to treat anxiety, asthma, and irritable bowel syndrome.

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2,5-Dimethoxy-4-bromoamphetamine

Dimethoxybromoamphetamine (DOB), also known as brolamfetamine (INN) and bromo-DMA, is a psychedelic drug and substituted amphetamine of the phenethylamine class of compounds.

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5-HT receptor

5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems.

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5-HT2A receptor

The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR).

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5-HT2C receptor

The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT).

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Biased agonist, Drug selectivity, Functional Selectivity, Functionally selective, Ligand bias, Nonselective, Selectivity (biochemistry).

References

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

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