Releasing agent: Difference between revisions

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A '''releasing agent''', or simply releaser, is a drug that induces the release of a [[neurotransmitter]] from the presynaptic [[~~neurone~~]] into the synapse, leading to a rise in the extracellular concentrations of the neurotransmitter, therefore resulting in increased neurotransmission. Many drugs use neurotransmitter release to exert their psychological and physiological effects, namely the [[amphetamines]] and related compounds. Virtually all currently known releasing agents affect the monoamine neurotransmitters [[serotonin]], [[noradrenaline]], and/or [[dopamine]], and as such, they are often referred to more formally as monoamine releasing agents (MRAs). MRAs may be selective for a particular neurotransmitter or non-selective and affect multiple neurotransmitters.

A '''releasing agent''', or simply releaser, is a drug that induces the release of a [[neurotransmitter]] from the presynaptic [[neuron]] into the synapse, leading to a rise in the extracellular concentrations of the neurotransmitter, therefore resulting in increased neurotransmission. Many drugs use neurotransmitter release to exert their psychological and physiological effects, namely the [[amphetamines]] and related compounds. Virtually all currently known releasing agents affect the monoamine neurotransmitters [[serotonin]], [[noradrenaline]], and/or [[dopamine]], and as such, they are often referred to more formally as monoamine releasing agents (MRAs). MRAs may be selective for a particular neurotransmitter or non-selective and affect multiple neurotransmitters.

==Mechanism of Action==

Releasing agents cause the release of neurotransmitters by first entering the presynaptic ~~neurone~~, primarily via membrane transporters. Some, such as [[amphetamine]] and [[methamphetamine]], can also diffuse directly across the cell membrane. Next, they inhibit vesicular uptake of the neurotransmitter by interfering with a vesicular transporter, and thus inhibit the repackaging of the neurotransmitter from the pre-synaptic ~~neurone~~ into vesicles. Finally, releasing agents reverse the action of reuptake receptors, allowing the neurotransmitter to flow out from the pre-synaptic ~~neurone~~ into the nerve terminal or synapse. The result is increased neurotransmission.

Releasing agents cause the release of neurotransmitters by first entering the presynaptic neuron, primarily via membrane transporters. Some, such as [[amphetamine]] and [[methamphetamine]], can also diffuse directly across the cell membrane. Next, they inhibit vesicular uptake of the neurotransmitter by interfering with a vesicular transporter, and thus inhibit the repackaging of the neurotransmitter from the pre-synaptic neuron into vesicles. Finally, releasing agents reverse the action of reuptake receptors, allowing the neurotransmitter to flow out from the pre-synaptic neuron into the nerve terminal or synapse. The result is increased neurotransmission.

The postsynaptic effect is enhanced due to the interaction with reuptake receptors; one method by which the action of neurotransmitters is terminated is via reuptake into the presynaptic neuron, and disruption of this process causes further increases in extracellular neurotransmitter concentration.

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-A '''releasing agent''', or simply releaser, is a drug that induces the release of a [[neurotransmitter]] from the presynaptic [[neurone]] into the synapse, leading to a rise in the extracellular concentrations of the neurotransmitter, therefore resulting in increased neurotransmission.  Many drugs use neurotransmitter release to exert their psychological and physiological effects, namely the [[amphetamines]] and related compounds. Virtually all currently known releasing agents affect the monoamine neurotransmitters [[serotonin]], [[noradrenaline]], and/or [[dopamine]], and as such, they are often referred to more formally as monoamine releasing agents (MRAs). MRAs may be selective for a particular neurotransmitter or non-selective and affect multiple neurotransmitters.
+A '''releasing agent''', or simply releaser, is a drug that induces the release of a [[neurotransmitter]] from the presynaptic [[neuron]] into the synapse, leading to a rise in the extracellular concentrations of the neurotransmitter, therefore resulting in increased neurotransmission.  Many drugs use neurotransmitter release to exert their psychological and physiological effects, namely the [[amphetamines]] and related compounds. Virtually all currently known releasing agents affect the monoamine neurotransmitters [[serotonin]], [[noradrenaline]], and/or [[dopamine]], and as such, they are often referred to more formally as monoamine releasing agents (MRAs). MRAs may be selective for a particular neurotransmitter or non-selective and affect multiple neurotransmitters.
 ==Mechanism of Action==
-Releasing agents cause the release of neurotransmitters by first entering the presynaptic neurone, primarily via membrane transporters. Some, such as [[amphetamine]] and [[methamphetamine]], can also diffuse directly across the cell membrane. Next, they inhibit vesicular uptake of the neurotransmitter by interfering with a vesicular transporter, and thus inhibit the repackaging of the neurotransmitter from the pre-synaptic neurone into vesicles. Finally, releasing agents reverse the action of reuptake receptors, allowing the neurotransmitter to flow out from the pre-synaptic neurone into the nerve terminal or synapse. The result is increased neurotransmission.
+Releasing agents cause the release of neurotransmitters by first entering the presynaptic neuron, primarily via membrane transporters. Some, such as [[amphetamine]] and [[methamphetamine]], can also diffuse directly across the cell membrane. Next, they inhibit vesicular uptake of the neurotransmitter by interfering with a vesicular transporter, and thus inhibit the repackaging of the neurotransmitter from the pre-synaptic neuron into vesicles. Finally, releasing agents reverse the action of reuptake receptors, allowing the neurotransmitter to flow out from the pre-synaptic neuron into the nerve terminal or synapse. The result is increased neurotransmission.
 The postsynaptic effect is enhanced due to the interaction with reuptake receptors; one method by which the action of neurotransmitters is terminated is via reuptake into the presynaptic neuron, and disruption of this process causes further increases in extracellular neurotransmitter concentration.