Reuptake inhibitor: Difference between revisions

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==Mechanism of action==

[[File:Reuptake inhibitor.png|350px|thumb|right|The effect of reuptake inhibitors on the presynaptic neurone]]

Standard reuptake inhibitors are believed to function by binding directly to the transporter protein of the [[neurotransmitter]] in question. ~~They occupy~~ the transporter ~~in place of the~~ respective neurotransmitter and ~~competitively block the neurotransmitter~~ from being transported from the synapse into the presynaptic neurone.

Standard reuptake inhibitors are believed to function by binding directly to the transporter protein of the [[neurotransmitter]] in question. By occupying the transporter, a reuptake inhibitor competitively blocks its respective neurotransmitter from binding to the transporter protein and thus prevents it from being transported from the synapse into the presynaptic neurone.

Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Several [[dissociative]] drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and [[dizocilpine]] (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.

@@ Line 5: / Line 5: @@
 ==Mechanism of action==
 [[File:Reuptake inhibitor.png|350px|thumb|right|The effect of reuptake inhibitors on the presynaptic neurone]]
-Standard reuptake inhibitors are believed to function by binding directly to the transporter protein of the [[neurotransmitter]] in question. They occupy the transporter in place of the respective neurotransmitter and competitively block the neurotransmitter from being transported from the synapse into the presynaptic neurone.
+Standard reuptake inhibitors are believed to function by binding directly to the transporter protein of the [[neurotransmitter]] in question. By occupying the transporter, a reuptake inhibitor competitively blocks its respective neurotransmitter from binding to the transporter protein and thus prevents it from being transported from the synapse into the presynaptic neurone.
 Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Several [[dissociative]] drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and [[dizocilpine]] (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.