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 an increase in the extracellular concentrations of the neurotransmitter. 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).

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 an increase in the extracellular concentrations of the neurotransmitter. 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).

==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 ~~receptor~~, 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 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.

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.

==Selectivity==

Releasing agents act to varying extents on the monoamine neurotransmitters. Some will induce the release of all three monoamines, an example of this is [[MDMA]]. Others are more selective, [[methamphetamine]] is a potent releasing agent of dopamine and noradrenaline, but is a weak releaser of serotonin.

Releasing agents act to varying extents on the monoamine neurotransmitters. Some will induce the release of all three monoamines; an example of this is [[MDMA]]. Others are more selective as [[methamphetamine]] is a potent releasing agent of dopamine and noradrenaline, but is a weak releaser of serotonin.

==Neurotoxicity==

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*[[Agonist]]

*[[Antagonist]]

*[[Reuptake ~~Inhibitor~~]]

*[[Reuptake inhibitor]]

==References==

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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 an increase in the extracellular concentrations of the neurotransmitter. 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).
+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 an increase in the extracellular concentrations of the neurotransmitter. 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).
 ==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 receptor, 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 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.
 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.
 ==Selectivity==
-Releasing agents act to varying extents on the monoamine neurotransmitters. Some will induce the release of all three monoamines, an example of this is [[MDMA]]. Others are more selective, [[methamphetamine]] is a potent releasing agent of dopamine and noradrenaline, but is a weak releaser of serotonin.
+Releasing agents act to varying extents on the monoamine neurotransmitters. Some will induce the release of all three monoamines; an example of this is [[MDMA]]. Others are more selective as [[methamphetamine]] is a potent releasing agent of dopamine and noradrenaline, but is a weak releaser of serotonin.
 ==Neurotoxicity==
@@ Line 15: / Line 15: @@
 *[[Agonist]]
 *[[Antagonist]]
-*[[Reuptake Inhibitor]]
+*[[Reuptake inhibitor]]
 ==References==
 {{references}}