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Reuptake Modulator
A reuptake modulator, or transporter modulator, is a type of drug which modulates the reuptake of one or more neurotransmitters via their respective neurotransmitter transporters. Examples of reuptake modulators include reuptake inhibitors (transporter blockers) and reuptake enhancers. See also * Releasing agent * Release modulator * Transporter substrate * Channel modulator * Enzyme modulator * Receptor modulator A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical receptors. They are ligands that can act on different parts of receptors and regulate activit ... References Drugs by mechanism of action Psychopharmacology {{pharmacology-stub ...
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Drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used ...
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Neuromodulation
Neuromodulation is the physiological process by which a given neuron uses one or more chemicals to regulate diverse populations of neurons. Neuromodulators typically bind to metabotropic, G-protein coupled receptors (GPCRs) to initiate a second messenger signaling cascade that induces a broad, long-lasting signal. This modulation can last for hundreds of milliseconds to several minutes. Some of the effects of neuromodulators include: alter intrinsic firing activity, increase or decrease voltage-dependent currents, alter synaptic efficacy, increase bursting activity and reconfiguration of synaptic connectivity. Major neuromodulators in the central nervous system include: dopamine, serotonin, acetylcholine, histamine, norepinephrine, nitric oxide, and several neuropeptides. Cannabinoids can also be powerful CNS neuromodulators. Neuromodulators can be packaged into vesicles and released by neurons, secreted as hormones and delivered through the circulatory system. A neuromodulator ...
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Reuptake
Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the pre-synaptic neuron at a synapse) or glial cell after it has performed its function of transmitting a neural impulse. Reuptake is necessary for normal synaptic physiology because it allows for the recycling of neurotransmitters and regulates the level of neurotransmitter present in the synapse, thereby controlling how long a signal resulting from neurotransmitter release lasts. Because neurotransmitters are too large and hydrophilic to diffuse through the membrane, specific transport proteins are necessary for the reabsorption of neurotransmitters. Much research, both biochemical and structural, has been performed to obtain clues about the mechanism of reuptake. Protein structure The first primary sequence of a reuptake protein was published in 1990. The technique for protein sequence determination relied upon the purification, ...
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Neurotransmitter
A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell. Neurotransmitters are released from synaptic vesicles into the synaptic cleft where they are able to interact with neurotransmitter receptors on the target cell. The neurotransmitter's effect on the target cell is determined by the receptor it binds. Many neurotransmitters are synthesized from simple and plentiful precursors such as amino acids, which are readily available and often require a small number of biosynthetic steps for conversion. Neurotransmitters are essential to the function of complex neural systems. The exact number of unique neurotransmitters in humans is unknown, but more than 100 have been identified. Common neurotransmitters include glutamate, GABA, acetylcholine, glycine and norepinephrine. Mechanism and cycle Synthes ...
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Neurotransmitter Transporter
Neurotransmitter transporters are a class of membrane transport proteins that span the cellular membranes of neurons. Their primary function is to carry neurotransmitters across these membranes and to direct their further transport to specific intracellular locations. There are more than twenty types of neurotransmitter transporters. Vesicular transporters move neurotransmitters into synaptic vesicles, regulating the concentrations of substances within them. Vesicular transporters rely on a proton gradient created by the hydrolysis of adenosine triphosphate (ATP) in order to carry out their work: v-ATPase hydrolyzes ATP, causing protons to be pumped into the synaptic vesicles and creating a proton gradient. Then the efflux of protons from the vesicle provides the energy to bring the neurotransmitter into the vesicle. Neurotransmitter transporters frequently use electrochemical gradients that exist across cell membranes to carry out their work. For example, some transporters use ...
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Reuptake Inhibitor
Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the pre-synaptic neuron at a synapse) or glial cell after it has performed its function of transmitting a neural impulse. Reuptake is necessary for normal synaptic physiology because it allows for the recycling of neurotransmitters and regulates the level of neurotransmitter present in the synapse, thereby controlling how long a signal resulting from neurotransmitter release lasts. Because neurotransmitters are too large and hydrophilic to diffuse through the membrane, specific transport proteins are necessary for the reabsorption of neurotransmitters. Much research, both biochemical and structural, has been performed to obtain clues about the mechanism of reuptake. Protein structure The first primary sequence of a reuptake protein was published in 1990. The technique for protein sequence determination relied upon the purification, se ...
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Reuptake Enhancer
A reuptake enhancer (RE), also sometimes referred to as a reuptake activator, is a type of reuptake modulator which enhances the plasmalemmal transporter-mediated reuptake of a neurotransmitter from the synapse into the pre-synaptic neuron, leading to a decrease in the extracellular concentrations of the neurotransmitter and therefore a decrease in neurotransmission. The antidepressant tianeptine was once claimed to be a ''(selective) serotonin reuptake enhancer'' (SRE or SSRE), but the role of serotonin reuptake in its mechanism is doubtful. Tianeptine has no affinity for the serotonin transporter, neither increases nor decreases extracellular levels of serotonin in cortico-limbic structures of conscious rats, and it didn't show any other long-term effect on the serotonin pathway. Thus, tianeptine's role as an SSRE may have been the coincidence of a yet unknown mechanism of action. Coluracetam is a choline-reuptake enhancer. The flavone luteoline as well as some of its deriv ...
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Releasing Agent
A monoamine releasing agent (MRA), or simply monoamine releaser, is a drug that induces the synapse, release of a monoamine neurotransmitter from the synapse, presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitter. Many drugs induce their effects in the body and/or brain via the release of monoamine neurotransmitters, e.g., trace amines, many substituted amphetamines, and related compounds. Types of MRAs MRAS can be classified by the monoamines they mainly release, although these drugs lie on a spectrum. * Selective for one neurotransmitter ** Serotonin releasing agent (SRA) ** Norepinephrine releasing agent (NRA) ** Dopamine releasing agent (DRA) * Non-selective, releasing two or more neurotransmitters ** Norepinephrine–dopamine releasing agent (NDRA) ** Serotonin–norepinephrine releasing agent (SNRA) ** Serotonin–dopamine releasing agent (SDRA) ** Serotonin–norepinephrine–dopamine releasing agent (SNDR ...
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Release Modulator
A release modulator, or neurotransmitter release modulator, is a type of drug that modulates the release of one or more neurotransmitters. Examples of release modulators include monoamine releasing agents such as the substituted amphetamines (which induce the release of norepinephrine, dopamine, and/or serotonin) and release inhibitors such as botulinum toxin A (which inhibits acetylcholine release by inactivating SNAP-25, thereby preventing exocytosis from occurring). See also * Reuptake modulator * Channel modulator * Enzyme modulator * Receptor modulator A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical receptors. They are ligands that can act on different parts of receptors and regulate activit ... References Drugs by mechanism of action Psychopharmacology {{pharmacology-stub ...
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Substrate (biochemistry)
In chemistry, the term substrate is highly context-dependent. Broadly speaking, it can refer either to a chemical species being observed in a chemical reaction, or to a surface on which other chemical reactions or microscopy are performed. In the former sense, a reagent is added to the ''substrate'' to generate a product through a chemical reaction. The term is used in a similar sense in synthetic and organic chemistry, where the substrate is the chemical of interest that is being modified. In biochemistry, an enzyme substrate is the material upon which an enzyme acts. When referring to Le Chatelier's principle, the substrate is the reagent whose concentration is changed. ;Spontaneous reaction : :*Where S is substrate and P is product. ;Catalysed reaction : :*Where S is substrate, P is product and C is catalyst. In the latter sense, it may refer to a surface on which other chemical reactions are performed or play a supporting role in a variety of spectroscopic and microscop ...
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Channel Modulator
A channel modulator, or ion channel modulator, is a type of drug which modulates ion channels. They include channel blockers and channel openers. Direct modulators Ion channels are typically categorised by gating mechanism and by the ion they conduct. Note that an ion channel may overlap between different categories. Some channels conduct multiple ion currents and some are gated by multiple mechanisms. Examples of targets for modulators include: Voltage gated ion channels * Calcium channel: see also Calcium channel blocker, Calcium channel opener * Potassium channel: see also Potassium channel blocker, Potassium channel opener * Sodium channel: see also Sodium channel blocker, Sodium channel opener * Chloride channel: see also Chloride channel blocker, Chloride channel opener * Transient receptor potential channel) Ligand gated ion channels * 5-HT3: see also 5-HT3 antagonist, * GABAA receptor: see also GABA receptor agonist, GABA receptor antagonist * Glutamate receptor: see ...
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Enzyme Modulator
An enzyme modulator is a type of drug which modulates enzymes. They include enzyme inhibitors and enzyme inducers. In an homogeneous assay, "an enzyme modulator ... is covalently linked to the ligand which competes with free ligand from the test sample for the available antibodies." See also * Channel modulator * Receptor modulator * Transporter modulator A reuptake modulator, or transporter modulator, is a type of drug which modulates the reuptake of one or more neurotransmitters via their respective neurotransmitter transporters. Examples of reuptake modulators include reuptake inhibitors (tran ... References Metabolism Enzyme inhibitors {{pharmacology-stub ...
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